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Titlebook: Optimization in Drug Discovery; Zhengyin Yan,Gary W. Caldwell Book 2004 Humana Press 2004

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發(fā)表于 2025-3-21 17:58:08 | 只看該作者 |倒序?yàn)g覽 |閱讀模式
書目名稱Optimization in Drug Discovery
編輯Zhengyin Yan,Gary W. Caldwell
視頻videohttp://file.papertrans.cn/704/703246/703246.mp4
概述Includes supplementary material:
叢書名稱Methods in Pharmacology and Toxicology
圖書封面Titlebook: Optimization in Drug Discovery;  Zhengyin Yan,Gary W. Caldwell Book 2004 Humana Press 2004
描述Recent analyses of drug attrition rates reveal that a significant number of drug candidates fail in the later stage of clinical development owing to absorption, distribution, metabolism, elimination (ADME), and toxicity issues. Lead optimization in drug discovery, a process attempting to uncover and correct these defects of drug candidates, is highly beneficial in lowering the cost and time to develop therapeutic drugs by reducing drug candidate failures in development. At present, parallel synthesis combining with high-throughput screening has made it easier to generate highly potent compounds (i. e. , hits). However, to be a potential drug, a hit must have drug-like characteristics in addition to potency, which include optimal physicochemical properties, reasonable ph- macokinetic parameters, and good safety profiles. Therefore, research tools must be available in drug discovery to rapidly screen for compounds with favorable drug-like properties, and thus adequate resources can be directed to projects with high potential. Optimization in Drug Discovery: In Vitro Methods is a compilation of detailed experimental protocols necessary for setting up a variety of assays important in c
出版日期Book 2004
版次1
doihttps://doi.org/10.1385/1592598005
isbn_softcover978-1-61737-499-9
isbn_ebook978-1-59259-800-7Series ISSN 1557-2153 Series E-ISSN 1940-6053
issn_series 1557-2153
copyrightHumana Press 2004
The information of publication is updating

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Use of Caco-2 Cell Monolayers to Study Drug Absorption and Metabolism,nd dietary chemicals. The Food and Drug Administration (FDA) recognized the model system as useful in classifying a compound’s absorption characteristics in the Biopharmaceutics Classification System. In addition to its usefulness as an absorption model, the Caco-2 cells are useful for studying the
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Absorption Screening Using the PAMPA Approach,earliest absorption, distribution, metabolism, and excretion (ADME) primary screening of research compounds. PAMPA’s popularity in the industry has risen rapidly. This chapter focuses on state-of-the-art PAMPA methods. Evidence will be cited demonstrating that as far as predicting passive permeabili
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In Vitro Permeation Study With Bovine Brain Microvessel Endothelial Cells, lines such as Caco-2, MDCK, MDCKII, and LLC-PK have been used to predict in vivo intestinal absorption of drugs. However, there are no well-characterized cell lines available representing the blood-brain barrier. In this chapter, the authors describe the primary culture of bovine brain microvessel
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Isothermal Titration Calorimetry Characterization of Drug-Binding Energetics to Blood Proteins,les. In this chapter, the authors describe the use of isothermal titration calorimetry (ITC) to measure the binding energetics of drugs bound to blood proteins (i.e., human serum albumin [HSA] and α-acid glycoprotein [AGP]). The stoichiometry (.), the association-binding constant (..), and the entha
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Metabolic Stability Assessed by Liver Microsomes and Hepatocytes,c stability assays, the typical test systems are liver microsomes, liver S9, or hepatocytes (plated or suspended), depending on the goal of the assay. To determine the metabolic stability of a new chemical entity, quantification of the drug candidate from incubate supernatants is required and usuall
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