Matches in SemOpenAlex for { <https://semopenalex.org/work/W2016226797> ?p ?o ?g. }
Showing items 1 to 86 of
86
with 100 items per page.
- W2016226797 endingPage "A45" @default.
- W2016226797 startingPage "A45" @default.
- W2016226797 abstract "HIV-1 integrase (IN) is one of three essential enzymes (along with reverse transcriptase and protease) encoded by the viral pol gene. IN mediates two critical reactions during viral replication; firstly 3′-end processing (3′EP) of the double-stranded viral DNA ends and then strand transfer (STF) which joins the viral DNA to the host chromosomal DNA forming a functional integrated proviral DNA. IN is a 288 amino acid protein containing three functional domains, the N-terminal domain (NTD), catalytic core domain (CCD) and the C-terminal domain (CTD). The CCD contains three conserved catalytic residues, Asp64, Asp116 and Glu152, which coordinate divalent metal ions essential for the STF reaction. Intensive research over the last two decades has led to the discovery and development of small molecule inhibitors of the IN STF reaction (INSTIs). INSTIs are catalytic inhibitors of IN, and act to chelate the divalent metal ions in the CCD. One INSTI, raltegravir (RAL, Merck Inc.) was approved in late 2007 for the treatment of HIV-1 infection in patients with prior antiretroviral (ARV) treatment experience and was recently approved also for first line therapy. A second INSTI, elvitegravir (EVG, Gilead Sciences, Inc.) is currently undergoing phase 3 studies in ARV treatment-experienced patients and phase 2 studies in ARV naïve patients as part of a novel fixed dose combination. Several additional INSTIs are in early stage clinical development. This review will discuss the discovery and development of this novel class of antiretrovirals. This article forms part of a special issue of Antiviral Research marking the 25th anniversary of antiretroviral drug discovery and development, Vol 85, issue 1, 2010." @default.
- W2016226797 created "2016-06-24" @default.
- W2016226797 creator A5001893764 @default.
- W2016226797 creator A5016741562 @default.
- W2016226797 creator A5017300854 @default.
- W2016226797 creator A5017745729 @default.
- W2016226797 creator A5017914492 @default.
- W2016226797 creator A5023796496 @default.
- W2016226797 creator A5040662398 @default.
- W2016226797 creator A5080351994 @default.
- W2016226797 date "2009-05-01" @default.
- W2016226797 modified "2023-09-28" @default.
- W2016226797 title "CXCR4 Chemokine Receptor Antagonists from Ultra-rigid Metal Complexes Profoundly Inhibit HIV-1 Replication, and also AMD3100-resistant Strains" @default.
- W2016226797 doi "https://doi.org/10.1016/j.antiviral.2009.02.100" @default.
- W2016226797 hasPublicationYear "2009" @default.
- W2016226797 type Work @default.
- W2016226797 sameAs 2016226797 @default.
- W2016226797 citedByCount "4" @default.
- W2016226797 countsByYear W20162267972014 @default.
- W2016226797 countsByYear W20162267972016 @default.
- W2016226797 countsByYear W20162267972019 @default.
- W2016226797 countsByYear W20162267972023 @default.
- W2016226797 crossrefType "journal-article" @default.
- W2016226797 hasAuthorship W2016226797A5001893764 @default.
- W2016226797 hasAuthorship W2016226797A5016741562 @default.
- W2016226797 hasAuthorship W2016226797A5017300854 @default.
- W2016226797 hasAuthorship W2016226797A5017745729 @default.
- W2016226797 hasAuthorship W2016226797A5017914492 @default.
- W2016226797 hasAuthorship W2016226797A5023796496 @default.
- W2016226797 hasAuthorship W2016226797A5040662398 @default.
- W2016226797 hasAuthorship W2016226797A5080351994 @default.
- W2016226797 hasConcept C104317684 @default.
- W2016226797 hasConcept C140704245 @default.
- W2016226797 hasConcept C142462285 @default.
- W2016226797 hasConcept C14430832 @default.
- W2016226797 hasConcept C156719811 @default.
- W2016226797 hasConcept C159047783 @default.
- W2016226797 hasConcept C185592680 @default.
- W2016226797 hasConcept C2522874641 @default.
- W2016226797 hasConcept C2777068322 @default.
- W2016226797 hasConcept C2780404665 @default.
- W2016226797 hasConcept C2993143319 @default.
- W2016226797 hasConcept C3013748606 @default.
- W2016226797 hasConcept C54355233 @default.
- W2016226797 hasConcept C552990157 @default.
- W2016226797 hasConcept C67705224 @default.
- W2016226797 hasConcept C73573662 @default.
- W2016226797 hasConcept C86803240 @default.
- W2016226797 hasConceptScore W2016226797C104317684 @default.
- W2016226797 hasConceptScore W2016226797C140704245 @default.
- W2016226797 hasConceptScore W2016226797C142462285 @default.
- W2016226797 hasConceptScore W2016226797C14430832 @default.
- W2016226797 hasConceptScore W2016226797C156719811 @default.
- W2016226797 hasConceptScore W2016226797C159047783 @default.
- W2016226797 hasConceptScore W2016226797C185592680 @default.
- W2016226797 hasConceptScore W2016226797C2522874641 @default.
- W2016226797 hasConceptScore W2016226797C2777068322 @default.
- W2016226797 hasConceptScore W2016226797C2780404665 @default.
- W2016226797 hasConceptScore W2016226797C2993143319 @default.
- W2016226797 hasConceptScore W2016226797C3013748606 @default.
- W2016226797 hasConceptScore W2016226797C54355233 @default.
- W2016226797 hasConceptScore W2016226797C552990157 @default.
- W2016226797 hasConceptScore W2016226797C67705224 @default.
- W2016226797 hasConceptScore W2016226797C73573662 @default.
- W2016226797 hasConceptScore W2016226797C86803240 @default.
- W2016226797 hasIssue "2" @default.
- W2016226797 hasLocation W20162267971 @default.
- W2016226797 hasOpenAccess W2016226797 @default.
- W2016226797 hasPrimaryLocation W20162267971 @default.
- W2016226797 hasRelatedWork W1997015701 @default.
- W2016226797 hasRelatedWork W2030572778 @default.
- W2016226797 hasRelatedWork W2068761442 @default.
- W2016226797 hasRelatedWork W2073327383 @default.
- W2016226797 hasRelatedWork W2092340666 @default.
- W2016226797 hasRelatedWork W2124631799 @default.
- W2016226797 hasRelatedWork W2390966738 @default.
- W2016226797 hasRelatedWork W2468218924 @default.
- W2016226797 hasRelatedWork W2634157224 @default.
- W2016226797 hasRelatedWork W3032152409 @default.
- W2016226797 hasVolume "82" @default.
- W2016226797 isParatext "false" @default.
- W2016226797 isRetracted "false" @default.
- W2016226797 magId "2016226797" @default.
- W2016226797 workType "article" @default.