(Q43851506)

27 November 2017

title

The importance of plasma protein binding in drug discovery (English)

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27 November 2017

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George L Trainor

1

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27 November 2017

language of work or name

English

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publication date

1 January 2007

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Expert Opinion on Drug Discovery

27 November 2017

number of pages

14

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based on heuristic

inferred from page(s)

published in

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27 November 2017

volume

2

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27 November 2017

issue

1

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27 November 2017

page(s)

51-64

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Fewer new drugs from the pharmaceutical industry

27 November 2017

cites work

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The chimpanzee (Pan troglodytes) as a pharmacokinetic model for selection of drug candidates: model characterization and application

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Strategy of utilizing in vitro and in vivo ADME tools for lead optimization and drug candidate selection

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QT prolongation through hERG K(+) channel blockade: current knowledge and strategies for the early prediction during drug development

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Idiosyncratic drug hepatotoxicity

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Do preclinical testing strategies help predict human hepatotoxic potentials?

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Tissue distribution and pharmacodynamics: a complicated relationship

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Antiretrovirals, part 1: overview, history, and focus on protease inhibitors

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Protein binding of human immunodeficiency virus protease inhibitor KNI-272 and alteration of its in vitro antiretroviral activity in the presence of high concentrations of proteins

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Weak Binding of VX-478 to Human Plasma Proteins and Implications for Anti-Human Immunodeficiency Virus Therapy

21 January 2018

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Relevance of plasma protein binding to antiviral activity and clinical efficacy of inhibitors of human immunodeficiency virus protease

21 January 2018

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Does protein binding modulate the effect of angiotensin II receptor antagonists?

21 January 2018

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Albumin: biochemical properties and therapeutic potential

21 January 2018

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Human alpha-1-glycoprotein and its interactions with drugs

21 January 2018

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Methods of determining plasma and tissue binding of drugs. Pharmacokinetic consequences

21 January 2018

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Early Absorption and Distribution Analysis of Antitumor and Anti-AIDS Drugs: Lipid Membrane and Plasma Protein Interactions

21 January 2018

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DPC 681 and DPC 684: potent, selective inhibitors of human immunodeficiency virus protease active against clinically relevant mutant variants

21 January 2018

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Synthesis, antiviral activity and pharmacokinetics of P1/P1' substituted 3-aminoindazole cyclic urea HIV protease inhibitors

21 January 2018

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A simple method for predicting serum protein binding of compounds from IC(50) shift analysis for in vitro assays

21 January 2018

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Intracellular concentration of the HIV protease inhibitors indinavir and saquinavir in human endothelial cells

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Intracellular accumulation of human immunodeficiency virus protease inhibitors

21 January 2018

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Intracellular and plasma pharmacokinetics of efavirenz in HIV-infected individuals

21 January 2018

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Therapeutic drug monitoring in saliva. An update

21 January 2018

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Influence of nonspecific brain and plasma binding on CNS exposure: implications for rational drug discovery

21 January 2018

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Relationship between exposure and nonspecific binding of thirty-three central nervous system drugs in mice.

21 January 2018

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Improving the in vitro prediction of in vivo central nervous system penetration: integrating permeability, P-glycoprotein efflux, and free fractions in blood and brain.

21 January 2018

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Plasma and CSF levels of dizocilplne (MK-801) required for neuroprotection in the quinolinate-injected rat striatum

21 January 2018

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Receptor occupancy of nonpeptide corticotropin-releasing factor 1 antagonist DMP696: correlation with drug exposure and anxiolytic efficacy

21 January 2018

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The technique of intracerebral microdialysis

21 January 2018

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Microdialysis in the study of drug transporters in the CNS.

21 January 2018

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GF120918, a P-glycoprotein modulator, increases the concentration of unbound amprenavir in the central nervous system in rats

21 January 2018

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Protein binding in antiretroviral therapies

21 January 2018

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Alpha1-acid glycoprotein expressed in the plasma of chronic myeloid leukemia patients does not mediate significant in vitro resistance to STI571.

21 January 2018

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Binding of imatinib by alpha(1)-acid glycoprotein

21 January 2018

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Relationship between elevated levels of the alpha 1 acid glycoprotein in chronic myelogenous leukemia in blast crisis and pharmacological resistance to imatinib (Gleevec) in vitro and in vivo.

21 January 2018

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Review of UCN-01 development: a lesson in the importance of clinical pharmacology

21 January 2018

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Alpha 1-acid glycoprotein levels in human immunodeficiency virus-infected subjects on antiretroviral regimens

21 January 2018

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Evidence for differences in the binding of drugs to the two main genetic variants of human alpha 1-acid glycoprotein

21 January 2018

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Distinct glycoforms of human alpha1-acid glycoprotein have comparable synthesis rates: a [13C]valine-labelling study in healthy humans

21 January 2018

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alpha1-acid glycoprotein fucosylation as a marker of carcinoma progression and prognosis

21 January 2018

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Steady-state pharmacokinetics of indinavir in cerebrospinal fluid and plasma among adults with human immunodeficiency virus type 1 infection

21 January 2018

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Harnessing chaperones to generate small-molecule inhibitors of amyloid beta aggregation

21 January 2018

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Clinical relevance of P-glycoprotein in drug therapy

21 January 2018

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Efflux transporters and their clinical relevance

21 January 2018

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Drug uptake systems in liver and kidney

21 January 2018

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Role of organic anion transporter OATP1B1 (OATP-C) in hepatic uptake of irinotecan and its active metabolite, 7-ethyl-10-hydroxycamptothecin: in vitro evidence and effect of single nucleotide polymorphisms.

21 January 2018

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Intracellular transport of formaldehyde-treated serum albumin in liver endothelial cells after uptake via scavenger receptors

21 January 2018

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Membrane binding proteins are the major determinants for the hepatocellular transmembrane flux of long-chain fatty acids bound to albumin

21 January 2018

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The role of plasma-binding proteins in the cellular uptake of lipophilic vitamins and steroids

21 January 2018

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Increased antitumor activity, intratumor paclitaxel concentrations, and endothelial cell transport of cremophor-free, albumin-bound paclitaxel, ABI-007, compared with cremophor-based paclitaxel

21 January 2018

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https://api.crossref.org/works/10.1517%2F17460441.2.1.51

Effect of albumin on phenytoin and tolbutamide metabolism in human liver microsomes: an impact more than protein binding

21 January 2018

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https://api.crossref.org/works/10.1517%2F17460441.2.1.51

Endocytosis of alpha 1-acid glycoprotein variants and of neoglycoproteins containing mannose derivatives by a mouse hybridoma cell line (2C11-12). Comparison with mouse peritoneal macrophages

21 January 2018

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https://api.crossref.org/works/10.1517%2F17460441.2.1.51

Role of site-specific binding to plasma albumin in drug availability to brain

21 January 2018

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https://api.crossref.org/works/10.1517%2F17460441.2.1.51

AZ 242, a novel PPARalpha/gamma agonist with beneficial effects on insulin resistance and carbohydrate and lipid metabolism in ob/ob mice and obese Zucker rats

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4-(2-[2-(2(R)-methylpyrrolidin-1-yl)ethyl]benzofuran-5-yl)benzonitrile and related 2-aminoethylbenzofuran H3 receptor antagonists potently enhance cognition and attention

21 January 2018

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SAR and inhibitor complex structure determination of a novel class of potent and specific Aurora kinase inhibitors

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Discovery and characterization of aminopiperidinecoumarin melanin concentrating hormone receptor 1 antagonists

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9-hydroxyazafluorenes and their use in thrombin inhibitors

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Discovery of 1-(3'-aminobenzisoxazol-5'-yl)-3-trifluoromethyl-N-[2-fluoro-4- [(2'-dimethylaminomethyl)imidazol-1-yl]phenyl]-1H-pyrazole-5-carboxyamide hydrochloride (razaxaban), a highly potent, selective, and orally bioavailable factor Xa inhibitor

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3-Aminopyrazole inhibitors of CDK2/cyclin A as antitumor agents. 2. Lead optimization

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3-Aminopyrazole inhibitors of CDK2/cyclin A as antitumor agents. 1. Lead finding

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Discovery of novel and potent thiazoloquinazolines as selective Aurora A and B kinase inhibitors

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Design of a potent, soluble glucokinase activator with excellent in vivo efficacy.

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Synthesis and antibacterial activity of 3-substituted-6-(3-ethyl-4-methylanilino)uracils

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Discovery, structure-activity relationship, and pharmacological evaluation of (5-substituted-pyrrolidinyl-2-carbonyl)-2-cyanopyrrolidines as potent dipeptidyl peptidase IV inhibitors.

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(2S,3S)-3-Amino-4-(3,3-difluoropyrrolidin-1-yl)-N,N-dimethyl-4-oxo-2-(4-[1,2,4]triazolo[1,5-a]-pyridin-6-ylphenyl)butanamide: a selective alpha-amino amide dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes

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In vitro and in vivo characterization of 3-[2-[6-(2-tert-butoxyethoxy)pyridin-3-yl]-1H-imidazol-4-yl]benzonitrile hydrochloride salt, a potent and selective NPY5 receptor antagonist

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Computational prediction of the plasma protein-binding percent of diverse pharmaceutical compounds

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In silico ADME modelling 2: computational models to predict human serum albumin binding affinity using ant colony systems.

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21 January 2018

Identifiers

DOI

10.1517/17460441.2.1.51

1 reference

27 November 2017

1 reference