Results 31 to 40 of about 989 (99)

Author response: HIV-1 integrase tetramers are the antiviral target of pyridine-based allosteric integrase inhibitors

, 2019
Pratibha C Koneru, Ashwanth C Francis, Nanjie Deng, Stephanie V Rebensburg, Ashley C Hoyte, Jared Lindenberger, Daniel Adu-Ampratwum, Ross C Larue, Michael F Wempe, Alan N Engelman, Dmitry Lyumkis, James R Fuchs, Ronald M Levy, Gregory B Melikyan, Mamuka Kvaratskhelia   +14 more
  +4 more sources

Decision letter: HIV-1 integrase tetramers are the antiviral target of pyridine-based allosteric integrase inhibitors

, 2019
Julie Overbaugh, Eric Freed
  +4 more sources

The Drug-Induced Interface That Drives HIV-1 Integrase Hypermultimerization and Loss of Function

mBio, 2023
Allosteric HIV-1 integrase (IN) inhibitors (ALLINIs) are an emerging class of small molecules that disrupt viral maturation by inducing the aberrant multimerization of IN. Here, we present cocrystal structures of HIV-1 IN with two potent ALLINIs, namely,
Matthew R. Singer, Tung Dinh, Lev Levintov, Arun S. Annamalai, Juan S. Rey, Lorenzo Briganti, Nicola J. Cook, Valerie E. Pye, Ian A. Taylor, Kyungjin Kim, Alan N. Engelman, Baek Kim, Juan R. Perilla, Mamuka Kvaratskhelia, Peter Cherepanov   +14 more
doaj   +1 more source

Structural Basis for Inhibitor-Induced Aggregation of HIV Integrase. [PDF]

PLoS Biology, 2016
The allosteric inhibitors of integrase (termed ALLINIs) interfere with HIV replication by binding to the viral-encoded integrase (IN) protein. Surprisingly, ALLINIs interfere not with DNA integration but with viral particle assembly late during HIV ...
Kushol Gupta, Vesa Turkki, Scott Sherrill-Mix, Young Hwang, Grant Eilers, Louis Taylor, Charlene McDanal, Ping Wang, David Temelkoff, Robert T Nolte, Emile Velthuisen, Jerry Jeffrey, Gregory D Van Duyne, Frederic D Bushman   +13 more
doaj   +1 more source

Structure of a HIV-1 IN-Allosteric inhibitor complex at 2.93 Å resolution: Routes to inhibitor optimization.

PLoS Pathogens, 2023
HIV integrase (IN) inserts viral DNA into the host genome and is the target of the strand transfer inhibitors (STIs), a class of small molecules currently in clinical use.
Grant Eilers, Kushol Gupta, Audrey Allen, Saira Montermoso, Hemma Murali, Robert Sharp, Young Hwang, Frederic D Bushman, Gregory Van Duyne   +8 more
doaj   +1 more source

Cis-Allosteric Regulation of HIV-1 Reverse Transcriptase by Integrase

Viruses, 2022
Reverse transcriptase (RT) and integrase (IN) are encoded tandemly in the pol genes of retroviruses. We reported recently that HIV-1 RT and IN need to be supplied as the pol precursor intermediates, in which RT and IN are in fusion form (RTIN) to exert ...
Takao Masuda, Osamu Kotani, Masaru Yokoyama, Yuya Abe, Gota Kawai, Hironori Sato   +5 more
doaj   +1 more source

Strategies in the Design and Development of Non-Nucleoside Reverse Transcriptase Inhibitors (NNRTIs)

Viruses, 2023
AIDS (acquired immunodeficiency syndrome) is a potentially life-threatening infectious disease caused by human immunodeficiency virus (HIV). To date, thousands of people have lost their lives annually due to HIV infection, and it continues to be a big ...
Murugesan Vanangamudi, Senthilkumar Palaniappan, Muthu Kumaradoss Kathiravan, Vigneshwaran Namasivayam   +3 more
doaj   +1 more source

HIV-1 integrase binding to genomic RNA 5′-UTR induces local structural changes in vitro and in virio

Retrovirology, 2021
Background During HIV-1 maturation, Gag and Gag-Pol polyproteins are proteolytically cleaved and the capsid protein polymerizes to form the honeycomb capsid lattice.
Shuohui Liu, Pratibha C. Koneru, Wen Li, Chathuri Pathirage, Alan N. Engelman, Mamuka Kvaratskhelia, Karin Musier-Forsyth   +6 more
doaj   +1 more source

Influence of the amino-terminal sequence on the structure and function of HIV integrase

Retrovirology, 2020
Background Antiretroviral therapy (ART) can mitigate the morbidity and mortality caused by the human immunodeficiency virus (HIV). Successful development of ART can be accelerated by accurate structural and biochemical data on targets and their responses
Grant Eilers, Kushol Gupta, Audrey Allen, Jeffrey Zhou, Young Hwang, Michael B. Cory, Frederic D. Bushman, Gregory Van Duyne   +7 more
doaj   +1 more source

A new class of multimerization selective inhibitors of HIV-1 integrase. [PDF]

PLoS Pathogens, 2014
The quinoline-based allosteric HIV-1 integrase (IN) inhibitors (ALLINIs) are promising candidates for clinically useful antiviral agents. Studies using these compounds have highlighted the role of IN in both early and late stages of virus replication ...
Amit Sharma, Alison Slaughter, Nivedita Jena, Lei Feng, Jacques J Kessl, Hind J Fadel, Nirav Malani, Frances Male, Li Wu, Eric Poeschla, Frederic D Bushman, James R Fuchs, Mamuka Kvaratskhelia   +12 more
doaj   +1 more source