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Lenacapavir: A Novel, Potent, and Selective First-in-Class Inhibitor of HIV-1 Capsid Function Exhibits Optimal Pharmacokinetic Properties for a Long-Acting Injectable Antiretroviral Agent.
Subramanian R, Tang J, Zheng J, Lu B, Wang K, Yant SR, Stepan GJ, Mulato A, Yu H, Schroeder S, Shaik N, Singh R, Wolckenhauer S, Chester A, Tse WC, Chiu A, Rhee M, Cihlar T, Rowe W, Smith BJ. Subramanian R, et al. Among authors: yu h. Mol Pharm. 2023 Dec 4;20(12):6213-6225. doi: 10.1021/acs.molpharmaceut.3c00626. Epub 2023 Nov 2. Mol Pharm. 2023. PMID: 37917742 Free PMC article.
Study of marine natural products including resorcyclic acid lactones from Humicola fuscoatra that reactivate latent HIV-1 expression in an in vitro model of central memory CD4+ T cells.
Mejia EJ, Loveridge ST, Stepan G, Tsai A, Jones GS, Barnes T, White KN, Drašković M, Tenney K, Tsiang M, Geleziunas R, Cihlar T, Pagratis N, Tian Y, Yu H, Crews P. Mejia EJ, et al. Among authors: yu h. J Nat Prod. 2014 Mar 28;77(3):618-24. doi: 10.1021/np400889x. Epub 2014 Feb 4. J Nat Prod. 2014. PMID: 24495105 Free PMC article.
Histone deacetylase inhibitor romidepsin induces HIV expression in CD4 T cells from patients on suppressive antiretroviral therapy at concentrations achieved by clinical dosing.
Wei DG, Chiang V, Fyne E, Balakrishnan M, Barnes T, Graupe M, Hesselgesser J, Irrinki A, Murry JP, Stepan G, Stray KM, Tsai A, Yu H, Spindler J, Kearney M, Spina CA, McMahon D, Lalezari J, Sloan D, Mellors J, Geleziunas R, Cihlar T. Wei DG, et al. Among authors: yu h. PLoS Pathog. 2014 Apr 10;10(4):e1004071. doi: 10.1371/journal.ppat.1004071. eCollection 2014 Apr. PLoS Pathog. 2014. PMID: 24722454 Free PMC article. Clinical Trial.
Abyssomicin 2 reactivates latent HIV-1 by a PKC- and HDAC-independent mechanism.
León B, Navarro G, Dickey BJ, Stepan G, Tsai A, Jones GS, Morales ME, Barnes T, Ahmadyar S, Tsiang M, Geleziunas R, Cihlar T, Pagratis N, Tian Y, Yu H, Linington RG. León B, et al. Among authors: yu h. Org Lett. 2015 Jan 16;17(2):262-5. doi: 10.1021/ol503349y. Epub 2015 Jan 5. Org Lett. 2015. PMID: 25560385 Free PMC article.
Antiviral Activity of Bictegravir (GS-9883), a Novel Potent HIV-1 Integrase Strand Transfer Inhibitor with an Improved Resistance Profile.
Tsiang M, Jones GS, Goldsmith J, Mulato A, Hansen D, Kan E, Tsai L, Bam RA, Stepan G, Stray KM, Niedziela-Majka A, Yant SR, Yu H, Kukolj G, Cihlar T, Lazerwith SE, White KL, Jin H. Tsiang M, et al. Among authors: yu h. Antimicrob Agents Chemother. 2016 Nov 21;60(12):7086-7097. doi: 10.1128/AAC.01474-16. Print 2016 Dec. Antimicrob Agents Chemother. 2016. PMID: 27645238 Free PMC article.
A highly potent long-acting small-molecule HIV-1 capsid inhibitor with efficacy in a humanized mouse model.
Yant SR, Mulato A, Hansen D, Tse WC, Niedziela-Majka A, Zhang JR, Stepan GJ, Jin D, Wong MH, Perreira JM, Singer E, Papalia GA, Hu EY, Zheng J, Lu B, Schroeder SD, Chou K, Ahmadyar S, Liclican A, Yu H, Novikov N, Paoli E, Gonik D, Ram RR, Hung M, McDougall WM, Brass AL, Sundquist WI, Cihlar T, Link JO. Yant SR, et al. Among authors: yu h. Nat Med. 2019 Sep;25(9):1377-1384. doi: 10.1038/s41591-019-0560-x. Epub 2019 Sep 9. Nat Med. 2019. PMID: 31501601 Free PMC article.
Clinical targeting of HIV capsid protein with a long-acting small molecule.
Link JO, Rhee MS, Tse WC, Zheng J, Somoza JR, Rowe W, Begley R, Chiu A, Mulato A, Hansen D, Singer E, Tsai LK, Bam RA, Chou CH, Canales E, Brizgys G, Zhang JR, Li J, Graupe M, Morganelli P, Liu Q, Wu Q, Halcomb RL, Saito RD, Schroeder SD, Lazerwith SE, Bondy S, Jin D, Hung M, Novikov N, Liu X, Villaseñor AG, Cannizzaro CE, Hu EY, Anderson RL, Appleby TC, Lu B, Mwangi J, Liclican A, Niedziela-Majka A, Papalia GA, Wong MH, Leavitt SA, Xu Y, Koditek D, Stepan GJ, Yu H, Pagratis N, Clancy S, Ahmadyar S, Cai TZ, Sellers S, Wolckenhauer SA, Ling J, Callebaut C, Margot N, Ram RR, Liu YP, Hyland R, Sinclair GI, Ruane PJ, Crofoot GE, McDonald CK, Brainard DM, Lad L, Swaminathan S, Sundquist WI, Sakowicz R, Chester AE, Lee WE, Daar ES, Yant SR, Cihlar T. Link JO, et al. Among authors: yu h. Nature. 2020 Aug;584(7822):614-618. doi: 10.1038/s41586-020-2443-1. Epub 2020 Jul 1. Nature. 2020. PMID: 32612233 Free PMC article. Clinical Trial.
Preclinical characterization of a non-peptidomimetic HIV protease inhibitor with improved metabolic stability.
Mulato A, Lansdon E, Aoyama R, Voigt J, Lee M, Liclican A, Lee G, Singer E, Stafford B, Gong R, Murray B, Chan J, Lee J, Xu Y, Ahmadyar S, Gonzalez A, Cho A, Stepan GJ, Schmitz U, Schultz B, Marchand B, Brumshtein B, Wang R, Yu H, Cihlar T, Xu L, Yant SR. Mulato A, et al. Among authors: yu h. Antimicrob Agents Chemother. 2024 Apr 3;68(4):e0137323. doi: 10.1128/aac.01373-23. Epub 2024 Feb 21. Antimicrob Agents Chemother. 2024. PMID: 38380945 Free PMC article.
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