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Roles of conformational and positional adaptability in structure-based design of TMC125-R165335 (etravirine) and related non-nucleoside reverse transcriptase inhibitors that are highly potent and effective against wild-type and drug-resistant HIV-1 variants.
Das K, Clark AD Jr, Lewi PJ, Heeres J, De Jonge MR, Koymans LM, Vinkers HM, Daeyaert F, Ludovici DW, Kukla MJ, De Corte B, Kavash RW, Ho CY, Ye H, Lichtenstein MA, Andries K, Pauwels R, De Béthune MP, Boyer PL, Clark P, Hughes SH, Janssen PA, Arnold E. Das K, et al. Among authors: lichtenstein ma. J Med Chem. 2004 May 6;47(10):2550-60. doi: 10.1021/jm030558s. J Med Chem. 2004. PMID: 15115397
Evolution of anti-HIV drug candidates. Part 3: Diarylpyrimidine (DAPY) analogues.
Ludovici DW, De Corte BL, Kukla MJ, Ye H, Ho CY, Lichtenstein MA, Kavash RW, Andries K, de Béthune MP, Azijn H, Pauwels R, Lewi PJ, Heeres J, Koymans LM, de Jonge MR, Van Aken KJ, Daeyaert FF, Das K, Arnold E, Janssen PA. Ludovici DW, et al. Among authors: lichtenstein ma. Bioorg Med Chem Lett. 2001 Sep 3;11(17):2235-9. doi: 10.1016/s0960-894x(01)00412-7. Bioorg Med Chem Lett. 2001. PMID: 11527705
Design of facilitated dissociation enables control over cytokine signaling duration.
Broerman AJ, Pollmann C, Lichtenstein MA, Jackson MD, Tessmer MH, Ryu WH, Abedi MH, Sahtoe DD, Allen A, Kang A, De La Cruz J, Brackenbrough E, Sankaran B, Bera AK, Zuckerman DM, Stoll S, Praetorius F, Piehler J, Baker D. Broerman AJ, et al. Among authors: lichtenstein ma. bioRxiv [Preprint]. 2024 Nov 16:2024.11.15.623900. doi: 10.1101/2024.11.15.623900. bioRxiv. 2024. PMID: 39605600 Free PMC article. Preprint.