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HIV-1 escape from a small molecule, CCR5-specific entry inhibitor does not involve CXCR4 use.
Trkola A, Kuhmann SE, Strizki JM, Maxwell E, Ketas T, Morgan T, Pugach P, Xu S, Wojcik L, Tagat J, Palani A, Shapiro S, Clader JW, McCombie S, Reyes GR, Baroudy BM, Moore JP. Trkola A, et al. Among authors: strizki jm. Proc Natl Acad Sci U S A. 2002 Jan 8;99(1):395-400. doi: 10.1073/pnas.012519099. Proc Natl Acad Sci U S A. 2002. PMID: 11782552 Free PMC article.
SCH-C (SCH 351125), an orally bioavailable, small molecule antagonist of the chemokine receptor CCR5, is a potent inhibitor of HIV-1 infection in vitro and in vivo.
Strizki JM, Xu S, Wagner NE, Wojcik L, Liu J, Hou Y, Endres M, Palani A, Shapiro S, Clader JW, Greenlee WJ, Tagat JR, McCombie S, Cox K, Fawzi AB, Chou CC, Pugliese-Sivo C, Davies L, Moreno ME, Ho DD, Trkola A, Stoddart CA, Moore JP, Reyes GR, Baroudy BM. Strizki JM, et al. Proc Natl Acad Sci U S A. 2001 Oct 23;98(22):12718-23. doi: 10.1073/pnas.221375398. Epub 2001 Oct 16. Proc Natl Acad Sci U S A. 2001. PMID: 11606733 Free PMC article.
Discovery and characterization of vicriviroc (SCH 417690), a CCR5 antagonist with potent activity against human immunodeficiency virus type 1.
Strizki JM, Tremblay C, Xu S, Wojcik L, Wagner N, Gonsiorek W, Hipkin RW, Chou CC, Pugliese-Sivo C, Xiao Y, Tagat JR, Cox K, Priestley T, Sorota S, Huang W, Hirsch M, Reyes GR, Baroudy BM. Strizki JM, et al. Antimicrob Agents Chemother. 2005 Dec;49(12):4911-9. doi: 10.1128/AAC.49.12.4911-4919.2005. Antimicrob Agents Chemother. 2005. PMID: 16304152 Free PMC article.
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 bioavailable, potent CCR5 antagonist.
Tagat JR, Steensma RW, McCombie SW, Nazareno DV, Lin SI, Neustadt BR, Cox K, Xu S, Wojcik L, Murray MG, Vantuno N, Baroudy BM, Strizki JM. Tagat JR, et al. Among authors: strizki jm. J Med Chem. 2001 Oct 11;44(21):3343-6. doi: 10.1021/jm0155401. J Med Chem. 2001. PMID: 11585438
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