Results 31 to 40 of about 1,267 (159)

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 Rebensburg, Ashley C. Hoyte, Jared Lindenberger, Daniel Adu‐Ampratwum, Ross C. Larue, Michael F. Wempe, Alan Engelman, Dmitry Lyumkis, James R. Fuchs, Ronald M. Levy, Gregory B. Melikyan, Mamuka Kvaratskhelia   +14 more
  +4 more sources

Structural Studies of the HIV-1 Integrase Protein: Compound Screening and Characterization of a DNA-Binding Inhibitor. [PDF]

PLoS ONE, 2015
Understanding the HIV integrase protein and mechanisms of resistance to HIV integrase inhibitors is complicated by the lack of a full length HIV integrase crystal structure. Moreover, a lentiviral integrase structure with co-crystallised DNA has not been
Peter K Quashie, Ying-Shan Han, Said Hassounah, Thibault Mesplède, Mark A Wainberg   +4 more
doaj   +1 more source

Multimodal Functionalities of HIV-1 Integrase

Viruses, 2022
Integrase is the retroviral protein responsible for integrating reverse transcripts into cellular genomes. Co-packaged with viral RNA and reverse transcriptase into capsid-encased viral cores, human immunodeficiency virus 1 (HIV-1) integrase has long ...
Alan N. Engelman, Mamuka Kvaratskhelia
doaj   +1 more source

Core Modifications to the 4-(4,4-Dimethylpiperidinyl) 2,6-Dimethylpyridinyl Class of Hiv-1 Allosteric Integrase Inhibitors

SSRN Electronic Journal, 2022
Kyle Parcella, M. Patel, Yong Qiang Tu, Kyle J. Eastman, Kevin M. Peese, Eric P. Gillis, Ira B. Dicker, Brian McAuliffe, Bo Ding, Paul Falk, Jean Simmermacher, Dawn C. Parker, Prasanna Sivaprakasam, Javed Khan, Kevin Kish, H.A. Lewis, Umesh Hanumegowda, Susan Jenkins, John F. Kadow, Mark Krystal, Nicholas A. Meanwell, B. Narasimhulu Naidu   +21 more
openalex   +2 more sources

Allosteric Inhibitor Development Targeting HIV‐1 Integrase [PDF]

ChemMedChem, 2011
AbstractHIV‐1 integrase (IN) is one of three essential enzymes for viral replication, and is a focus of ardent antiretroviral drug discovery and development efforts. Diligent research has led to the development of the strand‐transfer‐specific chemical class of IN inhibitors, with two compounds from this group, raltegravir and elvitegravir, advancing ...
Laith Q, Al-Mawsawi, Nouri, Neamati
openaire   +2 more sources

Protein Oligomer Engineering: A New Frontier for Studying Protein Structure, Function, and Toxicity

Angewandte Chemie, Volume 135, Issue 23, June 5, 2023., 2023
This minireview classifies protein oligomers according to toxicity, biological function, and application as well as summarizes frontier methods for engineering protein oligomers. From the analysis of the advantages and deficits of each methodology, we highlight protein grafting as a promising and robust method for future oligomer engineering with the ...
Chang Liu, Jinghui Luo
wiley   +2 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

Multimodal mechanism of action of allosteric HIV-1 integrase inhibitors [PDF]

Expert Reviews in Molecular Medicine, 2013
Integrase (IN) is required for lentivirus replication and is a proven drug target for the prevention of AIDS in HIV-1-infected patients. While clinical strand transfer inhibitors disarm the IN active site, allosteric inhibition of enzyme activity through the disruption of IN–IN protein interfaces holds great therapeutic potential.
Kellie Ann, Jurado, Alan, Engelman
openaire   +2 more sources

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