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Design of non-nucleoside inhibitors of HIV-1 reverse transcriptase with improved drug resistance properties. 1.

Hopkins AL, Ren J, Milton J, Hazen RJ, Chan JH, Stuart DI, Stammers DK. Hopkins AL, et al. J Med Chem. 2004 Nov 18;47(24):5912-22. doi: 10.1021/jm040071z. J Med Chem. 2004. PMID: 15537346

Design of non-nucleoside inhibitors of HIV-1 reverse transcriptase with improved drug resistance properties. 2.

Freeman GA, Andrews Iii CW 3rd, Hopkins AL, Lowell GS, Schaller LT, Cowan JR, Gonzales SS, Koszalka GW, Hazen RJ, Boone LR, Ferris RG, Creech KL, Roberts GB, Short SA, Weaver K, Reynolds DJ, Milton J, Ren J, Stuart DI, Stammers DK, Chan JH. Freeman GA, et al. J Med Chem. 2004 Nov 18;47(24):5923-36. doi: 10.1021/jm040072r. J Med Chem. 2004. PMID: 15537347

Novel benzophenones as non-nucleoside reverse transcriptase inhibitors of HIV-1.

Chan JH, Freeman GA, Tidwell JH, Romines KR, Schaller LT, Cowan JR, Gonzales SS, Lowell GS, Andrews CW 3rd, Reynolds DJ, St Clair M, Hazen RJ, Ferris RG, Creech KL, Roberts GB, Short SA, Weaver K, Koszalka GW, Boone LR. Chan JH, et al. J Med Chem. 2004 Feb 26;47(5):1175-82. doi: 10.1021/jm030255y. J Med Chem. 2004. PMID: 14971897

Design, synthesis, and SAR of a novel pyrazinone series with non-nucleoside HIV-1 reverse transcriptase inhibitory activity.

Heeres J, de Jonge MR, Koymans LM, Daeyaert FF, Vinkers M, Van Aken KJ, Arnold E, Das K, Kilonda A, Hoornaert GJ, Compernolle F, Cegla M, Azzam RA, Andries K, de Béthune MP, Azijn H, Pauwels R, Lewi PJ, Janssen PA. Heeres J, et al. J Med Chem. 2005 Mar 24;48(6):1910-8. doi: 10.1021/jm040829e. J Med Chem. 2005. PMID: 15771435

Design of annulated pyrazoles as inhibitors of HIV-1 reverse transcriptase.

Sweeney ZK, Harris SF, Arora SF, Javanbakht H, Li Y, Fretland J, Davidson JP, Billedeau JR, Gleason SK, Hirschfeld D, Kennedy-Smith JJ, Mirzadegan T, Roetz R, Smith M, Sperry S, Suh JM, Wu J, Tsing S, Villaseñor AG, Paul A, Su G, Heilek G, Hang JQ, Zhou AS, Jernelius JA, Zhang FJ, Klumpp K. Sweeney ZK, et al. J Med Chem. 2008 Dec 11;51(23):7449-58. doi: 10.1021/jm800527x. J Med Chem. 2008. PMID: 19007201

Structural mechanisms of drug resistance for mutations at codons 181 and 188 in HIV-1 reverse transcriptase and the improved resilience of second generation non-nucleoside inhibitors.

Ren J, Nichols C, Bird L, Chamberlain P, Weaver K, Short S, Stuart DI, Stammers DK. Ren J, et al. J Mol Biol. 2001 Sep 28;312(4):795-805. doi: 10.1006/jmbi.2001.4988. J Mol Biol. 2001. PMID: 11575933

Crystallography and the design of anti-AIDS drugs: conformational flexibility and positional adaptability are important in the design of non-nucleoside HIV-1 reverse transcriptase inhibitors.

Das K, Lewi PJ, Hughes SH, Arnold E. Das K, et al. Prog Biophys Mol Biol. 2005 Jun;88(2):209-31. doi: 10.1016/j.pbiomolbio.2004.07.001. Prog Biophys Mol Biol. 2005. PMID: 15572156 Free article. Review.

Structural insights into mechanisms of non-nucleoside drug resistance for HIV-1 reverse transcriptases mutated at codons 101 or 138.

Ren J, Nichols CE, Stamp A, Chamberlain PP, Ferris R, Weaver KL, Short SA, Stammers DK. Ren J, et al. FEBS J. 2006 Aug;273(16):3850-60. doi: 10.1111/j.1742-4658.2006.05392.x. FEBS J. 2006. PMID: 16911530 Free article.

Relationship of potency and resilience to drug resistant mutations for GW420867X revealed by crystal structures of inhibitor complexes for wild-type, Leu100Ile, Lys101Glu, and Tyr188Cys mutant HIV-1 reverse transcriptases.

Ren J, Nichols CE, Chamberlain PP, Weaver KL, Short SA, Chan JH, Kleim JP, Stammers DK. Ren J, et al. J Med Chem. 2007 May 17;50(10):2301-9. doi: 10.1021/jm061117m. Epub 2007 Apr 19. J Med Chem. 2007. PMID: 17441703

The design and synthesis of diaryl ether second generation HIV-1 non-nucleoside reverse transcriptase inhibitors (NNRTIs) with enhanced potency versus key clinical mutations.

Tucker TJ, Saggar S, Sisko JT, Tynebor RM, Williams TM, Felock PJ, Flynn JA, Lai MT, Liang Y, McGaughey G, Liu M, Miller M, Moyer G, Munshi V, Perlow-Poehnelt R, Prasad S, Sanchez R, Torrent M, Vacca JP, Wan BL, Yan Y. Tucker TJ, et al. Bioorg Med Chem Lett. 2008 May 1;18(9):2959-66. doi: 10.1016/j.bmcl.2008.03.064. Epub 2008 Mar 25. Bioorg Med Chem Lett. 2008. PMID: 18396399

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