Patents and Publications
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Terry Clayton is a chemist who has authored or co-authored numerous patents and publications related to GABAergic agents and their use in treating memory deficits. He has synthesized novel ligands for GABAA receptors containing the 留5 subunit. Clayton has also given many presentations on his research at national conferences. His research focuses on developing subtype selective ligands to treat memory impairments.
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Publication_DDe_2009DIBYENDU DE
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This document lists the publications, patents, and presentations of Dibyendu De, Ph.D. It includes 11 patents on novel compounds, 2 book chapters, 17 peer-reviewed publications, and 10 national and international conference presentations related to antimalarial drug development and medicinal chemistry. The publications span from 1990-2007 and focus on the synthesis and evaluation of aminoquinoline derivatives to overcome drug resistance in malaria parasites.fnmol-08-00024
fnmol-08-00024Niloo Karunaweera
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This document discusses how plant polyphenols may help treat Alzheimer's disease by inhibiting NF-虜B induced cytokine production. It first provides background on Alzheimer's disease and chronic neuroinflammation. It then describes the role of NF-虜B in inflammation and how plant polyphenols could prevent the expression of pro-inflammatory genes regulated by NF-虜B. The document proposes that plant polyphenols, due to their anti-inflammatory properties, have the potential to slow Alzheimer's disease progression by inhibiting NF-虜B signaling in the brain.Ecology2 Complete
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The document discusses genetic and environmental polymorphism, which refers to differences in DNA sequences or phenotypes induced by environmental factors. It provides examples of various types of genetic polymorphism, including phenotypic, biochemical, immunological, chromosomal, and DNA polymorphisms. The manifestation of these polymorphisms can include variations in traits, proteins, antigens, blood groups, length of chromosomes, and DNA sequences. The importance of polymorphism studies is also highlighted for applications like forensics, transplantation, epidemiology, taxonomy, and understanding susceptibility to environmental factors and drugs.Spontaneous mutations in microorganisms
Spontaneous mutations in microorganismsprasanna1017
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Griffith's experiment in 1928 showed that bacteria can undergo transformation through uptake of DNA. He found that non-lethal heat-killed bacteria, when mixed with live harmless bacteria, could make the mixture lethal. Later it was found the "transforming principle" was DNA, which could be taken up by other bacteria and confer new traits like capsule formation and virulence. This provided early evidence that DNA carries genetic information that can be transferred between bacteria.Nucleotide chemotherapy
Nucleotide chemotherapyJosephJaphet
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Chemotherapeutic enzymes target the nucleotide biosynthetic pathway by inhibiting enzymes involved in DNA and RNA synthesis. Nucleotides are essential for cell survival and proliferation, and tumor cells have high concentrations of nucleotide metabolites. Chemotherapeutic drugs work by blocking DNA synthesis, causing lethal events in rapidly dividing cancer cells and arresting tumor progression. Specifically, antimetabolites like methotrexate and 6-mercaptopurine interfere with folate and purine metabolism, halting cancer cell division. By targeting nucleotide biosynthesis, chemotherapy aims to stop uncontrolled tumor cell growth.Publication HS
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This document lists 41 publications authored or co-authored by Himadri Samanta from 1977 to 2007. The publications cover research conducted by Samanta and collaborators on topics including thymineless death in Escherichia coli, radiation response of thymine starved bacteria, interferon action and the enzymology of interferon pathways, expression of hepatitis B virus antigens, characterization of recombinant enzymes expressed in cell lines, analysis of drug-resistant HIV strains, and discovery of new classes of HIV integrase inhibitors.Mutation
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Mutations can be caused by errors during DNA replication or by environmental mutagens. There are two main types of mutations: germline mutations, which can be inherited, and somatic mutations, which cannot. Mutations can involve changes to a single nucleotide (point mutation) or larger structural changes to chromosomes. DNA repair systems help fix errors, with mechanisms like base excision repair, nucleotide excision repair, and mismatch repair that recognize and correct damage. Unrepaired mutations can lead to genetic disorders if they occur in germline cells or cause cancer if they happen in other body cells.Identification of a CpG Island Methylator Phenotype that Defines a Distinct S...
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This document discusses mutations, which are heritable changes in an organism's genome. Mutations can occur spontaneously during DNA replication due to errors, or can be induced by mutagens like UV radiation or chemicals. Mutations provide genetic variation and are the raw material for evolution, though they are generally harmful. They can result in the formation of new alleles and allow organisms to evolve and adapt to their environments. The document covers different types of mutations and their molecular basis.Effect of Environmental Chemical Exposures on Epigenetics of Diseases: A Syst...
Effect of Environmental Chemical Exposures on Epigenetics of Diseases: A Syst...SSR Institute of International Journal of Life Sciences
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This document summarizes the effects of environmental chemical exposures on epigenetics and disease. It finds that environmental pollutants like air pollution and chemicals like arsenic and aluminum can cause epigenetic changes including DNA methylation, histone modifications, and microRNA expression. These epigenetic alterations have been linked to various diseases. The document provides a table listing specific epigenetic changes found for different environmental chemicals and the diseases studied. It concludes that while many reports link environmental exposures to epigenetic changes, most have not been directly associated with disease outcomes, and more research is still needed.Genes and mutations
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The document discusses how various classes of biomolecules are affected by diseases, emphasizing the rapid or slow biochemical alterations that can occur. It outlines genetic disorders, including chromosomal, monogenic, and multifactorial types, and highlights the significance of inborn errors of metabolism. Additionally, it explores gene therapy approaches, gene expression in diagnostics, and treatment strategies for genetic diseases.Epigenetics
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This document summarizes different types of mutagens and how they cause mutations. There are three main types of mutagens: chemical mutagens, radiation, and biological mutagens. Chemical mutagens include base analogs, alkylating agents, and intercalating agents. They cause mutations by getting incorporated into DNA during replication or by modifying DNA bases. Radiation like UV and ionizing radiation also cause mutations by damaging DNA bases. The document provides examples of specific mutagens and how they induce transitions or transversions.Genetic variation and its role in health and pharmacology
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The document discusses genetic variation, which refers to the differences in genes among individuals in a population and plays a crucial role in evolution and natural selection. It outlines the causes of genetic variation, such as DNA mutations, gene flow, and sexual reproduction, and emphasizes its significance in health and pharmacology, including the implications for disease susceptibility and drug efficacy. Ultimately, genetic diversity is important for adaptation and survival of species, influencing both evolutionary processes and medical outcomes.Mutation
MutationShri Shankaracharya College, Bhilai,Junwani
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This document discusses mutations, which are sudden heritable changes in genetic material. Mutations can be classified in several ways, including by direction (forward or reverse), cause (spontaneous or induced), and tissue of origin (somatic or germinal). Spontaneous mutations occur randomly due to environmental mutagens or natural chemical changes in DNA bases. Induced mutations are caused by chemical or physical mutagens. The Ames test is commonly used to detect mutations. While most mutations are harmful, some can be beneficial by introducing genetic variation.Wing Lam CV Feb-2016
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Wing Lam is a research scientist at Yale University specializing in herbal medicine and cancer pharmacology. He has over 15 years of experience identifying active compounds from herbs to treat diseases like cancer, metabolic disorders, and viral infections. Some of his accomplishments include developing the herbal formulation PHY906 to reduce chemotherapy side effects and enhance cancer treatment, identifying compounds that activate Wnt signaling for tissue regeneration, and developing nucleoside analogs for cancer and viral infections. He has published over 30 papers in peer-reviewed journals and presented at international conferences on topics related to herbal medicine and cancer chemotherapy.Keith publications 2015
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This document lists 20 research publications that involve Kevin Porter as an author. The publications cover a range of topics including studies of genes associated with insulin resistance and diabetes, genetic defects related to reproductive disorders, and various analyses involving DNA sequencing and mapping of human chromosomes. Kevin Porter has contributed to research involving the molecular characterization of genes and chromosomal abnormalities.Ayyappan et al., PLoS One
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This research article describes a genome-wide analysis of histone modifications (H3K9me2 and H4K12ac) and gene expression in common bean (Phaseolus vulgaris L.) leaves inoculated with the fungal pathogen Uromyces appendiculatus, which causes bean rust disease. ChIP-Seq was used to identify differentially methylated and acetylated regions between inoculated and mock-inoculated leaves at 0, 12 and 84 hours after inoculation. RNA-Seq was used to identify differentially expressed genes. Key defense genes and transcription factors involved in the bean-rust interaction were identified. The study provides insights into epigenomic regulation of gene expression during biotic stress in commonCV_Edmiston
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This CV summarizes the academic and professional background of Paul L. Edmiston. He received his B.S. in Chemistry from Pepperdine University in 1993 and Ph.D. in Chemistry from the University of Arizona in 1997. He is currently a Professor of Chemistry at the College of Wooster where he conducts research exclusively with undergraduate students. He has founded a company, ABS Materials, and his research focuses on developing new hybrid organic-inorganic materials for applications including water treatment. He has received significant research funding and awards for his work developing swellable organosilica materials.Lecture 4, gene mutation.ppt
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The document discusses various types of mutations and how they are induced. It describes three main types of mutations: chromosome mutations, genome mutations, and single-gene mutations. Single-gene mutations can be further divided into point mutations, deletions, additions, transitions, and transversions. Mutations can occur spontaneously due to errors in DNA replication or be induced by environmental mutagens like chemicals, radiation, and viruses. Mutations provide genetic variation but can also cause genetic disorders and diseases.Abbas Morovvati
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This document discusses genetic manipulation of carotenoid biosynthesis. It defines genetic engineering as the direct manipulation of an organism's genes using techniques like recombinant DNA and gene splicing. It explains that genetic manipulation can be used to alter existing species' characteristics or induce mutations to produce desirable traits. Specific techniques discussed include site-directed mutagenesis, protoplast fusion, and using shuttle and expression vectors. Carotenoids are described as pigments that protect plant structures and have health benefits when consumed by humans as antioxidants and for vitamin A activity. The locations and functions of carotenoid pigments are summarized.Molecular mechanism of spontaneous mutations
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Spontaneous mutations arise from errors in DNA replication and spontaneous DNA damage. Errors in replication can result in base substitutions if an incorrect base pairs with another. Spontaneous DNA damage includes depurination, in which bases are lost from DNA, and deamination of cytosine to uracil. Large deletions and duplications can also occur spontaneously. These replication errors and lesions generate the genetic variation that allows organisms to evolve in response to environmental changes. Spontaneous mutations are the ultimate source of natural genetic variation seen within populations and are responsible for certain human genetic diseases when they disrupt important genes.Mutations
MutationsBaijayantiSahoo2
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Mutations are changes in DNA sequence that may occur naturally during DNA replication or be caused by mutagens. There are two types of mutations: somatic mutations, which occur in somatic cells and are not inherited, and germline mutations, which occur in gametes and are passed to offspring. Mutations can be caused by physical mutagens like radiation or chemical mutagens like mustard gas. Chromosomal mutations include deletions, inversions, translocations, duplications, and aneuploidy. Gene mutations include frameshift, substitution, insertion, and deletion mutations. Several databases track somatic mutations in cancer genomes, including COSMIC, ICGC, and TCGA.Mutation 2
Mutation 2BHU
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Mutagens are agents that cause mutations and can be physical, chemical, or biological. Physical mutagens include ionizing radiation like X-rays and gamma rays. These high energy radiations can directly damage DNA through ionization, producing reactive ions that cause breaks in DNA strands. Ionizing radiation is especially harmful to rapidly dividing cells. Ultraviolet light is also mutagenic through formation of pyrimidine dimers in DNA, though it does not ionize. The type and amount of radiation exposure determines the mutagenic effect.4d gene mutations
4d gene mutationsJessi Dildy
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Gene mutations occur when the sequence of nitrogen bases that make up a gene changes. There are three types of mutations: substitutions replace one base with another, additions insert an extra base, and deletions remove a base. Mutations can have positive, negative, or neutral effects on an organism's chances of survival. Mutagens like viruses, smoke, radiation, and chemicals cause DNA mutations and sometimes lead to cancer. Gene therapy aims to correct mutations by replacing the mutated gene with a healthy copy delivered via inactive viruses, though it remains experimental.Mutation
MutationAhmad Ali
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Mutations are genetic changes that result in alternative gene forms. There are two main types of mutations: gene mutations that change gene chemistry and chromosomal aberrations that affect chromosome structure and number. Most mutations are random, recessive, harmful, and non-adaptive, but can provide raw material for evolution by creating genetic variation. Mutations occur spontaneously due to errors in DNA replication or can be induced. They play a role in forming new alleles and allowing adaptability to environmental changes. There are different types of mutations, including somatic, germinal, hereditary, acquired, silent, neutral, missense, and nonsense mutations.Mdj Qpackage General V2
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MDJ provides owner's representative services to help clients successfully complete building and renovation projects. They have a senior level team with experience across various project types, sizes, and industries. Their services include managing project teams, budgets, schedules, and issues to keep projects on track and deliverables met. MDJ is accountable for ultimate project success and values quality, integrity, and commitment in their work.Branding2
Branding2St marys college
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This document discusses branding for an acoustic music artist targeting teenagers. The branding aims to create a consistent image across three products - a music video, album cover, and magazine advertisement. Specifically, the branding uses a simple black and white logo and font style throughout the products to clearly convey who the artist is and appeal to the target audience. Memory clips from the music video are also used in black and white on the album cover to link the two products under the same brand image.More Related Content
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This document discusses mutations, which are heritable changes in an organism's genome. Mutations can occur spontaneously during DNA replication due to errors, or can be induced by mutagens like UV radiation or chemicals. Mutations provide genetic variation and are the raw material for evolution, though they are generally harmful. They can result in the formation of new alleles and allow organisms to evolve and adapt to their environments. The document covers different types of mutations and their molecular basis.Effect of Environmental Chemical Exposures on Epigenetics of Diseases: A Syst...
Effect of Environmental Chemical Exposures on Epigenetics of Diseases: A Syst...SSR Institute of International Journal of Life Sciences
油
This document summarizes the effects of environmental chemical exposures on epigenetics and disease. It finds that environmental pollutants like air pollution and chemicals like arsenic and aluminum can cause epigenetic changes including DNA methylation, histone modifications, and microRNA expression. These epigenetic alterations have been linked to various diseases. The document provides a table listing specific epigenetic changes found for different environmental chemicals and the diseases studied. It concludes that while many reports link environmental exposures to epigenetic changes, most have not been directly associated with disease outcomes, and more research is still needed.Genes and mutations
Genes and mutationsSridevi Ravi
油
This document discusses genes, mutations, and how genetic information flows from DNA to protein. It defines key terms like gene, RNA, transcription, translation, and genetic code. It explains that genes code for proteins, and information flows from DNA to RNA to protein but not vice versa. It describes the three main types of RNA and the multi-step processes of transcription and translation. It also defines different types of mutations like substitutions, insertions, deletions, and expansions that can occur at the gene and chromosome level and cause genetic disorders.Genetic disesase
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The document discusses how various classes of biomolecules are affected by diseases, emphasizing the rapid or slow biochemical alterations that can occur. It outlines genetic disorders, including chromosomal, monogenic, and multifactorial types, and highlights the significance of inborn errors of metabolism. Additionally, it explores gene therapy approaches, gene expression in diagnostics, and treatment strategies for genetic diseases.Epigenetics
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The document discusses epigenetics and its role in environmental diseases. It defines epigenetics as mechanisms that regulate gene expression without changing DNA sequence. Environmental factors can cause epigenetic changes through pathways like DNA methylation and histone modification. Abnormal epigenetic changes have been implicated in diseases like cancer, aging, and neurodevelopmental disorders. Certain environmental exposures are also linked to epigenetic alterations, though causal relationships are difficult to establish.Gtc presentation
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Hemanthemant150893
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This document summarizes different types of mutagens and how they cause mutations. There are three main types of mutagens: chemical mutagens, radiation, and biological mutagens. Chemical mutagens include base analogs, alkylating agents, and intercalating agents. They cause mutations by getting incorporated into DNA during replication or by modifying DNA bases. Radiation like UV and ionizing radiation also cause mutations by damaging DNA bases. The document provides examples of specific mutagens and how they induce transitions or transversions.Genetic variation and its role in health and pharmacology
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The document discusses genetic variation, which refers to the differences in genes among individuals in a population and plays a crucial role in evolution and natural selection. It outlines the causes of genetic variation, such as DNA mutations, gene flow, and sexual reproduction, and emphasizes its significance in health and pharmacology, including the implications for disease susceptibility and drug efficacy. Ultimately, genetic diversity is important for adaptation and survival of species, influencing both evolutionary processes and medical outcomes.Mutation
MutationShri Shankaracharya College, Bhilai,Junwani
油
This document discusses mutations, which are sudden heritable changes in genetic material. Mutations can be classified in several ways, including by direction (forward or reverse), cause (spontaneous or induced), and tissue of origin (somatic or germinal). Spontaneous mutations occur randomly due to environmental mutagens or natural chemical changes in DNA bases. Induced mutations are caused by chemical or physical mutagens. The Ames test is commonly used to detect mutations. While most mutations are harmful, some can be beneficial by introducing genetic variation.Wing Lam CV Feb-2016
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Wing Lam is a research scientist at Yale University specializing in herbal medicine and cancer pharmacology. He has over 15 years of experience identifying active compounds from herbs to treat diseases like cancer, metabolic disorders, and viral infections. Some of his accomplishments include developing the herbal formulation PHY906 to reduce chemotherapy side effects and enhance cancer treatment, identifying compounds that activate Wnt signaling for tissue regeneration, and developing nucleoside analogs for cancer and viral infections. He has published over 30 papers in peer-reviewed journals and presented at international conferences on topics related to herbal medicine and cancer chemotherapy.Keith publications 2015
Keith publications 2015Keith Porter
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This document lists 20 research publications that involve Kevin Porter as an author. The publications cover a range of topics including studies of genes associated with insulin resistance and diabetes, genetic defects related to reproductive disorders, and various analyses involving DNA sequencing and mapping of human chromosomes. Kevin Porter has contributed to research involving the molecular characterization of genes and chromosomal abnormalities.Ayyappan et al., PLoS One
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This research article describes a genome-wide analysis of histone modifications (H3K9me2 and H4K12ac) and gene expression in common bean (Phaseolus vulgaris L.) leaves inoculated with the fungal pathogen Uromyces appendiculatus, which causes bean rust disease. ChIP-Seq was used to identify differentially methylated and acetylated regions between inoculated and mock-inoculated leaves at 0, 12 and 84 hours after inoculation. RNA-Seq was used to identify differentially expressed genes. Key defense genes and transcription factors involved in the bean-rust interaction were identified. The study provides insights into epigenomic regulation of gene expression during biotic stress in commonCV_Edmiston
CV_EdmistonPaul Edmiston
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This CV summarizes the academic and professional background of Paul L. Edmiston. He received his B.S. in Chemistry from Pepperdine University in 1993 and Ph.D. in Chemistry from the University of Arizona in 1997. He is currently a Professor of Chemistry at the College of Wooster where he conducts research exclusively with undergraduate students. He has founded a company, ABS Materials, and his research focuses on developing new hybrid organic-inorganic materials for applications including water treatment. He has received significant research funding and awards for his work developing swellable organosilica materials.Lecture 4, gene mutation.ppt
Lecture 4, gene mutation.pptMannat Mughal
油
The document discusses various types of mutations and how they are induced. It describes three main types of mutations: chromosome mutations, genome mutations, and single-gene mutations. Single-gene mutations can be further divided into point mutations, deletions, additions, transitions, and transversions. Mutations can occur spontaneously due to errors in DNA replication or be induced by environmental mutagens like chemicals, radiation, and viruses. Mutations provide genetic variation but can also cause genetic disorders and diseases.Abbas Morovvati
Abbas Morovvatiabbasmorovvati
油
This document discusses genetic manipulation of carotenoid biosynthesis. It defines genetic engineering as the direct manipulation of an organism's genes using techniques like recombinant DNA and gene splicing. It explains that genetic manipulation can be used to alter existing species' characteristics or induce mutations to produce desirable traits. Specific techniques discussed include site-directed mutagenesis, protoplast fusion, and using shuttle and expression vectors. Carotenoids are described as pigments that protect plant structures and have health benefits when consumed by humans as antioxidants and for vitamin A activity. The locations and functions of carotenoid pigments are summarized.Molecular mechanism of spontaneous mutations
Molecular mechanism of spontaneous mutationsPromila Sheoran
油
Spontaneous mutations arise from errors in DNA replication and spontaneous DNA damage. Errors in replication can result in base substitutions if an incorrect base pairs with another. Spontaneous DNA damage includes depurination, in which bases are lost from DNA, and deamination of cytosine to uracil. Large deletions and duplications can also occur spontaneously. These replication errors and lesions generate the genetic variation that allows organisms to evolve in response to environmental changes. Spontaneous mutations are the ultimate source of natural genetic variation seen within populations and are responsible for certain human genetic diseases when they disrupt important genes.Mutations
MutationsBaijayantiSahoo2
油
Mutations are changes in DNA sequence that may occur naturally during DNA replication or be caused by mutagens. There are two types of mutations: somatic mutations, which occur in somatic cells and are not inherited, and germline mutations, which occur in gametes and are passed to offspring. Mutations can be caused by physical mutagens like radiation or chemical mutagens like mustard gas. Chromosomal mutations include deletions, inversions, translocations, duplications, and aneuploidy. Gene mutations include frameshift, substitution, insertion, and deletion mutations. Several databases track somatic mutations in cancer genomes, including COSMIC, ICGC, and TCGA.Mutation 2
Mutation 2BHU
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Mutagens are agents that cause mutations and can be physical, chemical, or biological. Physical mutagens include ionizing radiation like X-rays and gamma rays. These high energy radiations can directly damage DNA through ionization, producing reactive ions that cause breaks in DNA strands. Ionizing radiation is especially harmful to rapidly dividing cells. Ultraviolet light is also mutagenic through formation of pyrimidine dimers in DNA, though it does not ionize. The type and amount of radiation exposure determines the mutagenic effect.4d gene mutations
4d gene mutationsJessi Dildy
油
Gene mutations occur when the sequence of nitrogen bases that make up a gene changes. There are three types of mutations: substitutions replace one base with another, additions insert an extra base, and deletions remove a base. Mutations can have positive, negative, or neutral effects on an organism's chances of survival. Mutagens like viruses, smoke, radiation, and chemicals cause DNA mutations and sometimes lead to cancer. Gene therapy aims to correct mutations by replacing the mutated gene with a healthy copy delivered via inactive viruses, though it remains experimental.Mutation
MutationAhmad Ali
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Mutations are genetic changes that result in alternative gene forms. There are two main types of mutations: gene mutations that change gene chemistry and chromosomal aberrations that affect chromosome structure and number. Most mutations are random, recessive, harmful, and non-adaptive, but can provide raw material for evolution by creating genetic variation. Mutations occur spontaneously due to errors in DNA replication or can be induced. They play a role in forming new alleles and allowing adaptability to environmental changes. There are different types of mutations, including somatic, germinal, hereditary, acquired, silent, neutral, missense, and nonsense mutations.Effect of Environmental Chemical Exposures on Epigenetics of Diseases: A Syst...
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This document discusses branding for an acoustic music artist targeting teenagers. The branding aims to create a consistent image across three products - a music video, album cover, and magazine advertisement. Specifically, the branding uses a simple black and white logo and font style throughout the products to clearly convey who the artist is and appeal to the target audience. Memory clips from the music video are also used in black and white on the album cover to link the two products under the same brand image.BELAJAR BERSAMA LIKA (ahLI logiKA)
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The document summarizes a student's work on a music video project. The student edited, filmed, and created a magazine advert and album back cover. The music video was for an acoustic song and used conventions like black and white performance clips. It challenged conventions by using slow motion black and white memories from the artist's perspective. Feedback showed the choices worked effectively. The album cover and advert used traditional conventions like the artist name/image and release date with a brick background to match the acoustic genre.Branding
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Branding involves using a particular brand on a product to increase sales through extensive advertising. The document discusses how branding is important for musicians to help sell their product and portray a particular image to their target audience. It describes how the artist's brand was created to appeal to typical teenagers interested in alternative, acoustic music. Logos and fonts were designed to be simple yet eye-catching and match across all products in order to effectively brand the artist.Pulsars
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Pulsar 犖犖劇賢 犖犖橿犖迦犢犖÷犢犖犖ム犖犖犖ム険犖犖犖項 (Highly magnetised) 犖犖犖 犖犖迦硯犖犖巌硯犖犖犖犖犖犖謹犖犢犖犖巌犖犖迦犖犖迦牽犖∇幻犖犖犖園硯犖犖犖犖犖迦硯 犖犖朽犖÷元犖÷硯犖ム検犖迦犖犖о犖迦犖о犖犖迦犖巌犖∇Cook2010web
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The document provides an overview of computational chemistry methods for structure-activity relationship analysis, pharmacophore modeling, and protein-ligand docking. It discusses topics like SAR, QSAR, molecular alignment, conformational analysis, homology modeling of protein targets, and docking programs. Examples are given of applying these methods to study benzodiazepine ligands and GABA receptor subtypes.Final Defence
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The document describes the development of pharmacophore models and selective ligands for the 5 subtypes of GABAA/benzodiazepine receptors. Key points include:
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Patents and Publications
- 1. terry_clayton@sbcglobal.net Terry S. Clayton 262-641-0536 Patents Cook, J.M.; Han, D.; Clayton, T. Imidazobenzodiazepines as gabaergic agents to treat memory deficits and their preparation. U.S. Pat 7,595,395 B2; September 29, 2009. Cook, J.M.; Clayton, T.; Jain, H.D.; Teng, Y.; Yang, J. Selective Anticonvulsant Agents and Their Uses. U.S. Pat. Appl. No. 61/038,184; Filed March 2008. Barndt, J.A.; Barton, R.H.; Clayton, T.S.; Rose, M.J.; Volz, P.G. Printing Using Color Changeable Material. WO 2009/094063 A1. Pub. July 30, 2009. Graushar, W.T; Barndt, J.A.; Barton, R.H.; Clayton, T.S..; Ablative Printing. US 2009/0128860 A1; Pub. May 21, 2009. Roth, B.; Clayton, T. Device, method, and composition for reducing the incidence of tobacco smoking. U.S. Pat. Appl. 20060130857; Filed September 30, 2005. Publications Miroslav M Savic, Ph.D.; Samarpan Majumder; Shengming Huang; Rahul V Edwankar; Roman Furtm端ller; Sran Joksimovi; Terry Clayton Sr; Joachim Ramerstorfer; Marija M Milinkovi; Bryan L Roth; Werner Sieghart; James M Cook Novel positive allosteric modulators of GABAA receptors: Do subtle differences in activity at a1 plus a5 versus a2 plus a3 subunits account for dissimilarities in behavioral effects in rats? Progress in Neuro-Psychopharmacology & Biological Psychiatry. Accepted in January 2010. Grant, J.A., Bonnick, T., Gossell-Williams, M., Clayton, T., Cook, J.M., Jackson, Y.A., Synthesis, pharmacological studies and molecular modeling of some tetracyclic 1,3-diazepinium chlorides. Bioorg. Med. Chem. xxx (2009) xxxxxx. Available online. Takahashi, A.; Yap, J.J.; Bohager, D.Z.; Faccidomo, S.; Clayton, T.; Cook, J.M.; Miczek, K.A Glutamatergic and GABAergic Modulations of Ultrasonic Vocalizations During Maternal Separation Distress in Mouse Pups. Psychopharmacol. (Berlin, Ger.) , 204, pp 61-71 (2009). Han, D., Forsterling, H.F., Li, X., Deschamps, J.R., Parrish, D., Cao, H., Rallapalli, S., Clayton, T. , Teng, Y., Majumder, S., Sankar, S., Roth, B.L., Sieghart, W., Furtmuller, R., J.K. , Weed, M.R., Cook, J.M. A Study of the Structure-activity Relationship of GABAA-benzodiazepine Receptor Bivalent Ligands by Conformational Analysis with low Temperature NMR and X-ray Analysis, Bioorg. and Med. Chem., 16, 8853-8862 (2008). Savic, M.M.; Milinkovic, M.M.; Clayton, T.; Rallapalli, R.; Joksimovic, Van linn, M.; Cook, J.M.; The differential role of 留1 and 留5 containing GABAA receptors in mediating diazepam effects on spontaneous locomotor activity and water maze learning and memory in rats. International Journal of Neuropsychopharmacology, 12, pp 1179-1193 (2009). Savic, M. M.; Clayton, T.; Furtmuller, R.; Gavrilovic, I.; Samardzic, J.; Savic, S.; Huck, S.; Sierhart,
- 2. terry_clayton@sbcglobal.net Terry S. Clayton 262-641-0536 W.; Cook, J. M.; PWZ-029, A compound with moderate inverse agonist functional selectivity at GABAA receptors containing 留5 subunits, improves passive, but not active, avoidance learning in rats. Brain Research, 2008,1208, pp 150-159. Danni Harris, Terry Clayton, James Cook, Robert Halliwell, Peyman Sahbaie, Roman Furtmuller, Sigismund Huck, Werner Sieghart,Timothy M. DeLorey; Selective Influence on Contextual Memory: Physiochemical Properties Associated with Selectivity of Benzodiazepine Ligands at GABAA Receptors Containing the 留5 Subunit. J. Med. Chem., 2008, 51 (13), pp 37883803. T. Clayton, J.L. Chen, M. Ernst, L. Richter, B.A. Cromer, C.J. Morton, H. Ng, C.C. Kaczorowski, F.J. Helmstetter, R. Furtm端ller, G. Ecker, M.W. Parker, W. Sieghart and J.M. Cook.; Analysis of the Benzodiazepine Binding Site on 粒-Aminobutyric acidA Receptors: Correlation of Experimental Data with Pharmacophore and Comparative Models, Current Medicinal Chemistry; vol. 14, number 26, Pp. 2755-2775; 2007. Savic, M.M., Huang, S., Furtm端eller, R., Clayton, T., Huck, S., Obradovi, D.I., Ugre邸i, N.D., Sieghart, W., Bokonji, D.R., Cook, J.M.; Are GABAA Receptors Containing 留5 Subunits Contributing to the Sedative Properties of Benzodiazepine Site Agonists? Neuropsychopharmacology, 2008, 33, pp 332339. Presentations Clayton, Terry; Synthesis of subtype selective ligands and molecular modeling for alpha-5 containing GABAA/Bz receptors to treat memory deficits. 235th ACS National Meeting, New Orleans, LA United States, April 6-10th , 2008. J. A. Grant, Y. A. Jackson, M. Gossell-Williams, T. Bonnick, T. Clayton and J. M. Cook; Synthesis, Pharmacological Studies and Molecular Modeling of Novel Tetracyclic 1,3- nd Diazepinium Chlorides The 22 Mona Symposium on Natural Products and Medicinal Chemistry, Mona Jamaica, January 7-10 (2008). James M. Cook, Harry June, Elise Weerts, Micheal L. Van Linn, Donna Platt, Tim DeLorey, Miroslav Savic, Terry Clayton. Serendipity rediscovered an oxymoron or rational drug design: Studies on subtype selective BzR/GABAergic ligands. Division of Medicinal Chemistry-234th ACS National Meeting Boston, MA August 19-23, 2007. Clayton, T.; Synthesis of Subtype Selective Ligands for Alpha 5-Containing GABAA/Bz Receptors to Treat Memory Deficits. 233rd ACS National Meeting, Chicago, IL, United States, March 25-29th, 2007. Huang, Shengming; Savic, Miroslav; Furtmuller, Roman; Duke, Angela; Clayton, Terry; Sieghart, Werner; Rowlett, James K.; Cook, James M. Design and synthesis of stereoenantiomeric benzodiazepine receptor ligands. Abstract of Papers, 233rd ACS National Meeting, Chicago, IL, United States, March 25-29th, 2007.
- 3. terry_clayton@sbcglobal.net Terry S. Clayton 262-641-0536 Platt, D.M.; Cook, J.M.; Van Linn, M.L.; Clayton, T.S.; GABA-A/alpha5 Receptor Mechanisms in the Discriminative Stimulus Effects of GABA-A Modulators. CPDD Meeting, Quebec, Canada. June 16-21, 2007. M. Weed, T. Clayton, J.M. Cook, Ry-023, a Selective Inverse Agonist at the Benzodiazepine Binding Site on the GABA-A 留5 Receptor, Improves Performance in a Delayed-Match-to-Sample Task in Rhesus Monkeys. 46th American College of Neuropsychopharmacology, December 9-13, Boca Raton, FL, Abst. #158 (2007). Faccidomo, S.; Maggin, J.G.; Melief, S.; Clayton, T.S.; Cook, J.M.; Miczek, K.A. Modulation of Alcohol-Heightened Aggression in Mice by a5-Containing GABAA Receptors; Society for Neuroscience, Atlanta, GA October, 2006. Grant, J.A..; Jackson, Y.A.; Gossel-Williams, M.; Clayton, T.; Cook, J.M.; Synthesis, Pharmacological Studies, and Molecular Modeling of Novel 1,3-Diazipinium Chlorides. In Latest Trends in Organic Synthesis, Brock University, St. Catherines, Ontario, 2006. Clayton, T.; Sanker, S.; Delorey, T.; Sieghart, W.; Furtmueller, R.; Wenger, G.; Cook, J.M.; Synthesis of Subtype Selective Ligands for 留5-Containing GABA /Bz Receptors to Treat Memory Deficits. A ACS, Milwaukee, WI, May, 2006. S. Huang, T. Clayton, M. Dai, W. Yin, J. Ma, R. Edwankar, C. Sawant, M. Van Linn, Y. Teng, M. Johnson, H. F. Forsterling, and J. M. Cook; The SAR Study of Benzodiazepine Receptor Bivalent th Ligands by Low Temperature NMR Spectroscopy and X-Ray Analysis , Abstracts, 37 Great Lakes Regional Meeting of the American Chemical Society, Milwaukee, WI May 31 June 2, 2006, GLRM-155. S. Huang, T. Clayton, M. Dai, R. Edwankar, C. Sawant, J. M. Cook Synthesis of Optically Active nd Subtype Selective BZR Ligands,, Abstracts of Papers, 232 ACS National Meeting, San Francisco, CA, Sept. 10-14, 2006, MEDI-502. Clayton, T., Prodrug Design and Synthesis, Graduate Seminar, Milwaukee, WI 2004. Clayton, T., Stripping Potentiometry Studies of Inorganic Arsenic Oxyanions at Trace Levels, Awards Day Finalist, Milwaukee, WI, 2003. Clayton, T.; Chemistry and Art. National Chemistry Week. Discovery World, ACS - Milwaukee Section, Milwaukee, WI, 2001.