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Open AccessReview

Recent Advances in HIV-1 Gag Inhibitor Design and Development

Department of Biochemistry & Molecular Biology, Drexel University College of Medicine, Rooms 10307, 10309, and 10315, 245 North 15th Street, Philadelphia, PA 19102, USA
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Molecules 2020, 25(7), 1687; https://doi.org/10.3390/molecules25071687
Received: 3 March 2020 / Revised: 31 March 2020 / Accepted: 5 April 2020 / Published: 7 April 2020
(This article belongs to the Special Issue Antiviral Agents)
Acquired Immune Deficiency Syndrome (AIDS) treatment with combination antiretroviral therapy (cART) has improved the life quality of many patients since its implementation. However, resistance mutations and the accumulation of severe side effects associated with cART remain enormous challenges that need to be addressed with the continual design and redesign of anti-HIV drugs. In this review, we focus on the importance of the HIV-1 Gag polyprotein as the master coordinator of HIV-1 assembly and maturation and as an emerging drug target. Due to its multiple roles in the HIV-1 life cycle, the individual Gag domains are attractive but also challenging targets for inhibitor design. However, recent encouraging developments in targeting the Gag domains such as the capsid protein with highly potent and potentially long-acting inhibitors, as well as the exploration and successful targeting of challenging HIV-1 proteins such as the matrix protein, have demonstrated the therapeutic viability of this important protein. Such Gag-directed inhibitors have great potential for combating the AIDS pandemic and to be useful tools to dissect HIV-1 biology. View Full-Text
Keywords: HIV-1 Gag polyprotein; antiretrovirals; matrix protein; capsid protein; nucleocapsid protein; p6 protein HIV-1 Gag polyprotein; antiretrovirals; matrix protein; capsid protein; nucleocapsid protein; p6 protein
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Dick, A.; Cocklin, S. Recent Advances in HIV-1 Gag Inhibitor Design and Development. Molecules 2020, 25, 1687.

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