Literature DB >> 12788340

Recent progress in discovery of small-molecule CCR5 chemokine receptor ligands as HIV-1 inhibitors.

Wieslaw Kazmierski1, Neil Bifulco, Hanbiao Yang, Larry Boone, Felix DeAnda, Chris Watson, Terry Kenakin.   

Abstract

This review addresses key pharmacology and virology issues relevant in discovery and development of CCR5 antagonists as anti-HIV drugs, such as target validation, receptor internalization, allosterism, viral resistance and tropism. Recent progress in the discovery and development of CCR5 antagonists, SAR and clinical status are reviewed. Finally, modeling-based structure of CCR5 is discussed in the context of a small-molecule antagonism of the CCR5 receptor.

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Year:  2003        PMID： 12788340     DOI： 10.1016/s0968-0896(03)00161-5

Source DB:  PubMed          Journal:  Bioorg Med Chem        ISSN： 0968-0896            Impact factor:   3.641


  15 in total

Review 1.  Emerging drug targets for antiretroviral therapy.

Authors:  Jacqueline D Reeves; Andrew J Piefer
Journal:  Drugs       Date:  2005       Impact factor: 9.546

2.  Investigation of substituent effect of 1-(3,3-diphenylpropyl)-piperidinyl phenylacetamides on CCR5 binding affinity using QSAR and virtual screening techniques.

Authors:  Antreas Afantitis; Georgia Melagraki; Haralambos Sarimveis; Panayiotis A Koutentis; John Markopoulos; Olga Igglessi-Markopoulou
Journal:  J Comput Aided Mol Des       Date:  2006-05-09       Impact factor: 3.686

3.  Binding modes of CCR5-targetting HIV entry inhibitors: partial and full antagonists.

Authors:  Ting Wang; Yong Duan
Journal:  J Mol Graph Model       Date:  2007-12-17       Impact factor: 2.518

4.  Transmitted/founder and chronic HIV-1 envelope proteins are distinguished by differential utilization of CCR5.

Authors:  Zahra F Parker; Shilpa S Iyer; Craig B Wilen; Nicholas F Parrish; Kelechi C Chikere; Fang-Hua Lee; Chuka A Didigu; Reem Berro; Per Johan Klasse; Benhur Lee; John P Moore; George M Shaw; Beatrice H Hahn; Robert W Doms
Journal:  J Virol       Date:  2012-12-26       Impact factor: 5.103

Review 5.  Emerging concepts and approaches for chemokine-receptor drug discovery.

Authors:  Morgan O'Hayre; Catherina L Salanga; Tracy M Handel; Damon J Hamel
Journal:  Expert Opin Drug Discov       Date:  2010-11       Impact factor: 6.098

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

Authors:  John P Moore; Robert W Doms
Journal:  Proc Natl Acad Sci U S A       Date:  2003-09-05       Impact factor: 11.205

7.  Genetic and phenotypic analyses of human immunodeficiency virus type 1 escape from a small-molecule CCR5 inhibitor.

Authors:  Shawn E Kuhmann; Pavel Pugach; Kevin J Kunstman; Joann Taylor; Robyn L Stanfield; Amy Snyder; Julie M Strizki; Janice Riley; Bahige M Baroudy; Ian A Wilson; Bette T Korber; Steven M Wolinsky; John P Moore
Journal:  J Virol       Date:  2004-03       Impact factor: 5.103

8.  Effect of CCR5 receptor antagonists on endocytosis of the human CCR5 receptor in CHO-K1 cells.

Authors:  J Longden; E-L Cooke; S J Hill
Journal:  Br J Pharmacol       Date:  2008-01-28       Impact factor: 8.739

9.  Cell surface expression of CCR5 and other host factors influence the inhibition of HIV-1 infection of human lymphocytes by CCR5 ligands.

Authors:  Thomas J Ketas; Shawn E Kuhmann; Ashley Palmer; Juan Zurita; Weijing He; Sunil K Ahuja; Per Johan Klasse; John P Moore
Journal:  Virology       Date:  2007-04-10       Impact factor: 3.616

10.  Use of a small molecule CCR5 inhibitor in macaques to treat simian immunodeficiency virus infection or prevent simian-human immunodeficiency virus infection.

Authors:  Ronald S Veazey; Per Johan Klasse; Thomas J Ketas; Jacqueline D Reeves; Michael Piatak; Kevin Kunstman; Shawn E Kuhmann; Preston A Marx; Jeffrey D Lifson; Jason Dufour; Megan Mefford; Ivona Pandrea; Steven M Wolinsky; Robert W Doms; Julie A DeMartino; Salvatore J Siciliano; Kathy Lyons; Martin S Springer; John P Moore
Journal:  J Exp Med       Date:  2003-11-17       Impact factor: 14.307
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