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Angewandte Chemie, Volume 134, Issue 51, December 19, 2022., 2022 Benzoxazolinate is a rare bis‐heterocyclic moiety that interacts with proteins and DNA. It was found that a putative acyl AMP‐ligase mediates the last cyclization step to afford benzoxazolinate. The enzyme was then used as a probe for genome mining, which led to the discovery of a new class of benzoxazolinate‐containing compounds in diverse bacteria ...
Yi‐Ming Shi +12 more
wiley +2 more sources
Integrase Strand Transfer Inhibitors Are Effective Anti-HIV Drugs
Viruses, 2021 Integrase strand transfer inhibitors (INSTIs) are currently recommended for the first line treatment of human immunodeficiency virus type one (HIV-1) infection. The first-generation INSTIs are effective but can select for resistant viruses.
Steven J. Smith +5 more
semanticscholar +1 more source
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 +4 more
doaj +1 more source
Antimicrobial Agents and Chemotherapy, 2021 P1093 is a multicenter, open-label, phase I/II study of pharmacokinetics, safety, and tolerability of dolutegravir plus an optimized background regimen in pediatric participants aged 4 weeks to
C. Vavro +8 more
semanticscholar +1 more source
Retroviral integrases and their cousins [PDF]
Current Opinion in Structural Biology, 1996 The recently determined structures of the catalytic domains of HIV integrase, avian sarcoma virus integrase and the Mu transposase are strikingly similar to each other and also exhibit significant similarity to several nucleases. All these enzymes of cut polynucleotides, leaving 3'OH and 5'PO4 groups. The integrase and transposase also possess a strand-
Rice, Phoebe +2 more
openaire +3 more sources
Integrase and integration: biochemical activities of HIV-1 integrase [PDF]
Retrovirology, 2008 Integration of retroviral DNA is an obligatory step of retrovirus replication because proviral DNA is the template for productive infection. Integrase, a retroviral enzyme, catalyses integration. The process of integration can be divided into two sequential reactions.
Ali Saïb +4 more
openaire +4 more sources
Cancer Communications, Volume 42, Issue 12, Page 1257-1287, December 2022., 2022 Abstract Clustered regularly interspaced short palindromic repeats‐associated protein (CRISPR/Cas9), an adaptive microbial immune system, has been exploited as a robust, accurate, efficient and programmable method for genome targeting and editing. This innovative and revolutionary technique can play a significant role in animal modeling, in vivo genome
Khaled S. Allemailem +6 more
wiley +1 more source
Resistance to Integrase Inhibitors [PDF]
Viruses, 2010 Integrase (IN) is a clinically validated target for the treatment of human immunodeficiency virus infections and raltegravir exhibits remarkable clinical activity. The next most advanced IN inhibitor is elvitegravir. However, mutant viruses lead to treatment failure and mutations within the IN coding sequence appear to confer cross-resistance.
Yves Pommier +3 more
openaire +4 more sources
Small molecule inhibitors of the LEDGF site of human immunodeficiency virus integrase identified by fragment screening and structure based design. [PDF]
PLoS ONE, 2012 A fragment-based screen against human immunodeficiency virus type 1 (HIV) integrase led to a number of compounds that bound to the lens epithelium derived growth factor (LEDGF) binding site of the integrase catalytic core domain.
Thomas S Peat +15 more
doaj +1 more source
Synthesis of programmable integrases [PDF]
Proceedings of the National Academy of Sciences, 2009 Accurate modification of the 3 billion-base-pair human genome requires tools with exceptional sequence specificity. Here, we describe a general strategy for the design of enzymes that target a single site within the genome. We generated chimeric zinc finger recombinases with cooperative DNA-binding and catalytic specificities that integrate transgenes ...
Charles A. Gersbach +2 more
openaire +3 more sources