Synonyms: example 51 [WO2013090664A1] | GSK-2838232 | GSK-8232 | GSK232
Compound class:
Synthetic organic
Comment: GSK2838232 is an investigational HIV maturation inhibitor [2-3]. This class of compounds bind to the HIV-1 gag protein and disrupt its cleavage by the viral protease that is crucial for forming new mature and infectious virus particles [4,6]. This mechanism is proposed to maintain antiviral efficacy against drug-resistant strains of HIV-1.
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References |
1. DeJesus E, Harward S, Jewell RC, Johnson M, Dumont E, Wilches V, Halliday F, Talarico CL, Jeffrey J, Gan J et al.. (2020)
A Phase IIa Study Evaluating Safety, Pharmacokinetics, and Antiviral Activity of GSK2838232, a Novel, Second-generation Maturation Inhibitor, in Participants With Human Immunodeficiency Virus Type 1 Infection. Clin Infect Dis, 71 (5): 1255-1262. [PMID:31769793] |
2. Hatcher MA, Johns BA, Martin MT, Tabet EA, Tang J. (2013)
Derivatives of betulin. Patent number: WO2013090664A1. Assignee: Glaxosmithkline Llc. Priority date: 14/12/2012. Publication date: 20/06/2013. |
3. Johnson M, Jewell RC, Peppercorn A, Gould E, Xu J, Lou Y, Davies M, Baldwin S, Tenorio AR, Burke M et al.. (2018)
The safety, tolerability, and pharmacokinetic profile of GSK2838232, a novel 2nd generation HIV maturation inhibitor, as assessed in healthy subjects. Pharmacol Res Perspect, 6 (4): e00408. [PMID:29930812] |
4. Salzwedel K, Martin DE, Sakalian M. (2007)
Maturation inhibitors: a new therapeutic class targets the virus structure. AIDS Rev, 9 (3): 162-72. [PMID:17982941] |
5. Stoddart CA, Joshi P, Sloan B, Bare JC, Smith PC, Allaway GP, Wild CT, Martin DE. (2007)
Potent activity of the HIV-1 maturation inhibitor bevirimat in SCID-hu Thy/Liv mice. PLoS One, 2 (11): e1251. [PMID:18043758] |
6. Waheed AA, Freed EO. (2012)
HIV type 1 Gag as a target for antiviral therapy. AIDS Res Hum Retroviruses, 28 (1): 54-75. [PMID:21848364] |