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Advances in bioactivation r...
I have always been interested in chemistry and biology. My undergraduate, graduate, and postdoctoral trainings in pharmacy, medicinal chemistry and pharmacology, respectively, have strengthened this interest and led me to realize that significant advances in medicine have frequently been realized because of research at the chem- try-biology interface. I am hoping that this comprehensive volume on recent advances in bioactivation research will stimulate pharmacologists, medicinal chemists, phar- ceutical scientists, and graduate students in these fields and related areas to consider and use bioactivation research when they explore and chart new frontiers in drug design and drug development and when they consider ways to reduce the side effects of existing drugs by making prodrugs. As for the toxicologists and environmental health scientists, I hope this volume will help them generate the knowledge needed to understand better mechanisms of toxicity to improve human risk assessments and intervention methods after occupational or environmental exposure to various hazardous chemicals. Adnan A. Elfarra, Ph. D. vii Part I General Concepts and Basic Mechanisms 1 Metabolic Concerns in Drug Design Jeffrey P. Jones Department of Chemistry, Washington State University, Pullman, WA 99164, USA e-mail: jpj@wsu. edu Keywords: Cytochrome P450 Aldehyde Oxidase Drug-Drug Interactions Mechanism-based Virtual Screening ADMET Regioselectivity 1. 1. Introduction Due to recent technological innovations, such as genomics, combinatorial chemistry, and high-throughput screening, the identification of disease targets and of compounds that are active against these targets (''leads'') can now be carried out efficiently
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monografia Rebiun34949900 https://catalogo.rebiun.org/rebiun/record/Rebiun34949900 m o d cr |n||||||||| 080805s2008 nyua ob 001 0 eng c 2008934609 GBA817621 bnb 458110009 587268945 646814011 656245851 666990568 767204958 777968734 880325203 994821516 1005813050 1034886022 1035705054 1044200600 1048135635 1056326144 1066453778 1078859538 1087022120 1097305073 1097327593 1102276196 1111016728 1112572586 1152992042 1320891882 9780387773001 electronic bk.) 0387773002 electronic bk.) 9780387772998 hbk. ; alk. paper) 0387772995 hbk. ; alk. paper) 9781282291829 MyiLibrary) 1282291823 10.1007/978-0-387-77300-1 doi AU@ 000048719545 AU@ 000058376399 AU@ 000060544775 DEBSZ 43075325X HEBIS 215110536 NLGGC 322015685 NLGGC 326380647 NZ1 13533084 11752172 978-0-387-77299-8 Springer http://www.springerlink.com COO eng pn COO N$T CUS GW5XE PUL OCLCQ STF OCLCQ UBY E7B IDEBK EBLCP YDXCP OCLCQ OCLCF BEDGE OCLCQ SLY N$T NLGGC DEBSZ NUI OCLCQ TXI OCLCQ Z5A OTZ OCLCQ UAB ESU OCLCQ VT2 OCLCO OCLCA OCLCQ CEF U3W OCLCQ WYU CANPU CNTRU OCLCO AUD OCLCQ DCT ERF OCLCQ OCLCA OCLCO OCLCQ OCLCO OCLCL EZC TUS INARC CAUOI pcc MED 108000 bisacsh MMG. bicssc 610.284 22 44.38 bcl Q493 clc VS 5450 rvk 610 sdnb Advances in bioactivation research [editor], Adnan A. Elfarra New York Springer Arlington, VA AAPS Press 2008 New York Arlington, VA New York Springer Arlington, VA AAPS Press 1 online resource (vii, 503 pages) illustrations 1 online resource (vii, 503 pages) Text txt rdacontent computer c rdamedia online resource cr rdacarrier text file PDF rda Biotechnology : pharmaceutical aspects v. 9 Includes bibliographical references and index General Concepts and Basic Mechanisms -- Metabolic Concerns in Drug Design -- Role of Bioactivation in Idiosyncratic Drug Toxicity: Structure#x2013;Toxicity Relationships -- Michael Addition#x2013;Elimination Reactions: Roles in Toxicity and Potential New Therapeutic Applications -- Induction of Drug-Metabolizing Enzymes: Contrasting Roles in Detoxification and Bioactivation of Drugs and Xenobiotics -- Mechanism-Based Inactivation of Cytochrome P450 2A and 2B Enzymes -- CYP2E1 #x2013; Biochemical and Toxicological Aspects and Role in Alcohol-Induced Liver Injury -- One- and Two-Electron-Mediated Reduction of Quinones: Enzymology and Toxicological Implications -- Lipoxidation-Derived Electrophiles as Biological Reactive Intermediates -- Bioactivation and Protein Modification Reactions of Unsaturated Aldehydes -- Tissue-Specific Features and Risk Assessment Applications -- Adaptive Responses and Signal Transduction Pathways in Chemically Induced Mitochondrial Dysfunction and Cell Death -- Hepatic Bioactivation and Drug-Induced Liver Injury -- Role of Cysteine S-Conjugate #x03B2;-Lyases in the Bioactivation of Renal Toxicants -- Bioactivation of Xenobiotics in Lung: Role of CYPs and FMOs -- Generation of Reactive Metabolites and Associated DNA Adducts from Benzene, Butadiene, and PAH in Bone Marrow. Their Effects on Hematopoiesis and Impact on Human Health -- Butadiene-Mediated Mutagenesis and Carcinogenesis -- Pharmacogenetics of Drug Bioactivation Pathways -- Human Phenanthrene Metabolites as Probes for the Metabolic Activation and Detoxification of Carcinogenic Polycyclic Aromatic Hydrocarbons I have always been interested in chemistry and biology. My undergraduate, graduate, and postdoctoral trainings in pharmacy, medicinal chemistry and pharmacology, respectively, have strengthened this interest and led me to realize that significant advances in medicine have frequently been realized because of research at the chem- try-biology interface. I am hoping that this comprehensive volume on recent advances in bioactivation research will stimulate pharmacologists, medicinal chemists, phar- ceutical scientists, and graduate students in these fields and related areas to consider and use bioactivation research when they explore and chart new frontiers in drug design and drug development and when they consider ways to reduce the side effects of existing drugs by making prodrugs. As for the toxicologists and environmental health scientists, I hope this volume will help them generate the knowledge needed to understand better mechanisms of toxicity to improve human risk assessments and intervention methods after occupational or environmental exposure to various hazardous chemicals. Adnan A. Elfarra, Ph. D. vii Part I General Concepts and Basic Mechanisms 1 Metabolic Concerns in Drug Design Jeffrey P. Jones Department of Chemistry, Washington State University, Pullman, WA 99164, USA e-mail: jpj@wsu. edu Keywords: Cytochrome P450 Aldehyde Oxidase Drug-Drug Interactions Mechanism-based Virtual Screening ADMET Regioselectivity 1. 1. Introduction Due to recent technological innovations, such as genomics, combinatorial chemistry, and high-throughput screening, the identification of disease targets and of compounds that are active against these targets (''leads'') can now be carried out efficiently Biotransformation (Metabolism) Drug activation Biotransformation Biotransformation (Métabolisme) Médicaments- Activation MEDICAL- Instruments & Supplies. Drug activation. Biotransformation. Biotransformation (Metabolism) Biomédecine. Sciences de la vie. Biotransformation (Metabolism) Drug activation. dissertations. Academic theses. Academic theses. Thèses et écrits académiques. Elfarra, Adnan A. Print version Advances in bioactivation research. New York : Springer ; Arlington, VA : AAPS Press, 2008 9780387772998 (DLC) 2008934609 (OCoLC)192027297 Biotechnology (Arlington, Va.) v. 9