(Q34413630)

2 August 2017

1 reference

title

The discovery of the CCR5 receptor antagonist, UK-427,857, a new agent for the treatment of HIV infection and AIDS. (English)

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2 August 2017

Anthony Wood

1

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2 August 2017

Duncan Armour

series ordinal

2

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2 August 2017

language of work or name

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1 January 2005

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Progress in medicinal chemistry

2 August 2017

published in

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2 August 2017

volume

43

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2 August 2017

page(s)

239-271

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Isolation of a T-Lymphotropic Retrovirus from a Patient at Risk for Acquired Immune Deficiency Syndrome (AIDS)

2 August 2017

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7 January 2021

HIV and AIDS: 20 years of science

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7 January 2021

Twenty years of therapy for HIV-1 infection.

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7 January 2021

Toxicity of antiretroviral therapy and implications for drug development

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7 January 2021

Failure to maintain long-term adherence to highly active antiretroviral therapy: the role of lipodystrophy

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7 January 2021

Adherence to HAART among patients with HIV: breakthroughs and barriers

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7 January 2021

Antiretroviral-drug resistance among patients recently infected with HIV.

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7 January 2021

HIV Type 1 Isolates from 200 Untreated Individuals in Ho Chi Minh City (Vietnam): ANRS 1257 Study. Large Predominance of CRF01_AE and Presence of Major Resistance Mutations to Antiretroviral Drugs

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7 January 2021

Resistance to antiretroviral drugs in patients with primary HIV-1 infection. Investigators of the Quebec Primary Infection Study.

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7 January 2021

HIV coreceptors: role of structure, posttranslational modifications, and internalization in viral-cell fusion and as targets for entry inhibitors

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7 January 2021

The entry of entry inhibitors: a fusion of science and medicine

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7 January 2021

A small molecule HIV-1 inhibitor that targets the HIV-1 envelope and inhibits CD4 receptor binding

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7 January 2021

The bicyclam AMD3100 story

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7 January 2021

Homozygous defect in HIV-1 coreceptor accounts for resistance of some multiply-exposed individuals to HIV-1 infection

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7 January 2021

The role of viral phenotype and CCR-5 gene defects in HIV-1 transmission and disease progression

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7 January 2021

The chemokine receptor, CCR5

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7 January 2021

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7 January 2021

Potent inhibition of HIV-1 infectivity in macrophages and lymphocytes by a novel CCR5 antagonist.

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7 January 2021

Potent, broad-spectrum inhibition of human immunodeficiency virus type 1 by the CCR5 monoclonal antibody PRO 140

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7 January 2021

Antagonists of the human CCR5 receptor as anti-HIV-1 agents. part 1: discovery and initial structure-activity relationships for 1 -amino-2-phenyl-4-(piperidin-1-yl)butanes

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7 January 2021

Multiple charged and aromatic residues in CCR5 amino-terminal domain are involved in high affinity binding of both chemokines and HIV-1 Env protein.

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7 January 2021

Naturally occurring CCR5 extracellular and transmembrane domain variants affect HIV-1 Co-receptor and ligand binding function

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7 January 2021

CCR5 antagonists: bicyclic isoxazolidines as conformationally constrained N-1-substituted pyrrolidines

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7 January 2021

Molecular complexity and its impact on the probability of finding leads for drug discovery

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7 January 2021

Is there a difference between leads and drugs? A historical perspective

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7 January 2021

Experimental and computational approaches to estimate solubility and permeability in drug discovery and development settings

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7 January 2021

The maximal affinity of ligands

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7 January 2021

Methods for drug discovery: development of potent, selective, orally effective cholecystokinin antagonists

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7 January 2021

Recognition of privileged structures by G-protein coupled receptors

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7 January 2021

Discovery of novel, potent, and selective small-molecule CCR5 antagonists as anti-HIV-1 agents: synthesis and biological evaluation of anilide derivatives with a quaternary ammonium moiety

1 reference

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7 January 2021

Discovery of 4-[(Z)-(4-bromophenyl)- (ethoxyimino)methyl]-1'-[(2,4-dimethyl-3- pyridinyl)carbonyl]-4'-methyl-1,4'- bipiperidine N-oxide (SCH 351125): an orally bioavailable human CCR5 antagonist for the treatment of HIV infection

1 reference

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7 January 2021

Piperazine-based CCR5 antagonists as HIV-1 inhibitors. II. Discovery of 1-[(2,4-dimethyl-3-pyridinyl)carbonyl]-4- methyl-4-[3(S)-methyl-4-[1(S)-[4-(trifluoromethyl)phenyl]ethyl]-1-piperazinyl]- piperidine N1-oxide (Sch-350634), an orally bioavailabl

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7 January 2021

Lead generation--enhancing the success of drug discovery by investing in the hit to lead process

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7 January 2021

Substrate interaction with cytochrome P-450.

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7 January 2021

P450 interaction with HIV protease inhibitors: relationship between metabolic stability, inhibitory potency, and P450 binding spectra

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7 January 2021

Novel approach to predicting P450-mediated drug metabolism: development of a combined protein and pharmacophore model for CYP2D6

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7 January 2021

The application of non-combinatorial chemistry to lead discovery.

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7 January 2021

Nomenclature for human CYP2D6 alleles.

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7 January 2021

A refined substrate model for human cytochrome P450 2D6

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7 January 2021

Structural and mechanistic studies of galactoside acetyltransferase, the Escherichia coli LacA gene product

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7 January 2021

Molecular and cellular mechanisms of cardiac arrhythmias

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7 January 2021

The impact of drug-induced QT interval prolongation on drug discovery and development

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7 January 2021

Antagonists of human CCR5 receptor containing 4-(pyrazolyl)piperidine side chains. Part 3: SAR studies on the benzylpyrazole segment

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7 January 2021

A structural basis for drug-induced long QT syndrome

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7 January 2021

Toward a pharmacophore for drugs inducing the long QT syndrome: insights from a CoMFA study of HERG K(+) channel blockers

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7 January 2021

Structural determinants of HERG channel block by clofilium and ibutilide.

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7 January 2021

The influence of peptide structure on transport across Caco-2 cells

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7 January 2021

Predicting oral absorption and bioavailability

1 reference

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7 January 2021

Polar molecular surface properties predict the intestinal absorption of drugs in humans.

1 reference

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7 January 2021

Polar molecular surface as a dominating determinant for oral absorption and brain penetration of drugs

1 reference

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7 January 2021

Synthetic and enzyme inhibition studies of pepstatin analogues containing hydroxyethylene and ketomethylene dipeptide isosteres

1 reference

https://api.crossref.org/works/10.1016%2FS0079-6468%2805%2943007-6

7 January 2021

Property-based design: optimization of drug absorption and pharmacokinetics

1 reference

https://api.crossref.org/works/10.1016%2FS0079-6468%2805%2943007-6

7 January 2021

Interactions among drugs for HIV and opportunistic infections

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7 January 2021

Chemokine receptors: gateways to inflammation and infection

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7 January 2021

Chemokine receptor-directed agents as novel anti-HIV-1 therapies

1 reference

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7 January 2021

Small-molecule antagonists of CCR5 and CXCR4: a promising new class of anti-HIV-1 drugs

1 reference

https://api.crossref.org/works/10.1016%2FS0079-6468%2805%2943007-6

7 January 2021

A small-molecule, nonpeptide CCR5 antagonist with highly potent and selective anti-HIV-1 activity

1 reference

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7 January 2021

https://api.crossref.org/works/10.1016%2FS0079-6468%2805%2943007-6

1 reference

7 January 2021

Novel low molecular weight spirodiketopiperazine derivatives potently inhibit R5 HIV-1 infection through their antagonistic effects on CCR5.

1 reference

https://api.crossref.org/works/10.1016%2FS0079-6468%2805%2943007-6

7 January 2021

Cloning and functional expression of CC CKR5, a human monocyte CC chemokine receptor selective for MIP-1(alpha), MIP-1(beta), and RANTES

1 reference

https://api.crossref.org/works/10.1016%2FS0079-6468%2805%2943007-6

7 January 2021

10.1016/S0079-6468(05)43007-6

Identifiers

DOI

1 reference

2 August 2017

1 reference