Matches in SemOpenAlex for { <https://semopenalex.org/work/W2766696270> ?p ?o ?g. }
- W2766696270 abstract "Antiretroviral therapy for HIV-1 infection/AIDS has significantly extended the life expectancy of HIV-1-infected individuals and reduced HIV-1 transmission at very high rates. However, certain individuals who initially achieve viral suppression to undetectable levels may eventually suffer treatment failure mainly due to adverse effects and the emergence of drug-resistant HIV-1 variants. Here, we report GRL-142, a novel HIV-1 protease inhibitor containing an unprecedented 6-5-5-ring-fused crown-like tetrahydropyranofuran, which has extremely potent activity against all HIV-1 strains examined with IC50 values of attomolar-to-picomolar concentrations, virtually no effects on cellular growth, extremely high genetic barrier against the emergence of drug-resistant variants, and favorable intracellular and central nervous system penetration. GRL-142 forms optimum polar, van der Waals, and halogen bond interactions with HIV-1 protease and strongly blocks protease dimerization, demonstrating that combined multiple optimizing elements significantly enhance molecular and atomic interactions with a target protein and generate unprecedentedly potent and practically favorable agents." @default.
- W2766696270 created "2017-11-10" @default.
- W2766696270 creator A5002861815 @default.
- W2766696270 creator A5007062297 @default.
- W2766696270 creator A5012018663 @default.
- W2766696270 creator A5025763229 @default.
- W2766696270 creator A5030756908 @default.
- W2766696270 creator A5032049756 @default.
- W2766696270 creator A5034303915 @default.
- W2766696270 creator A5034448543 @default.
- W2766696270 creator A5039137137 @default.
- W2766696270 creator A5041169651 @default.
- W2766696270 creator A5041773055 @default.
- W2766696270 creator A5047899621 @default.
- W2766696270 creator A5058961574 @default.
- W2766696270 creator A5060980612 @default.
- W2766696270 creator A5061450565 @default.
- W2766696270 creator A5063881144 @default.
- W2766696270 creator A5065179493 @default.
- W2766696270 creator A5066581924 @default.
- W2766696270 creator A5069696119 @default.
- W2766696270 creator A5073657901 @default.
- W2766696270 creator A5075530794 @default.
- W2766696270 creator A5082484825 @default.
- W2766696270 date "2017-10-17" @default.
- W2766696270 modified "2023-09-26" @default.
- W2766696270 title "A novel central nervous system-penetrating protease inhibitor overcomes human immunodeficiency virus 1 resistance with unprecedented aM to pM potency" @default.
- W2766696270 cites W1507665550 @default.
- W2766696270 cites W1539796472 @default.
- W2766696270 cites W1569669680 @default.
- W2766696270 cites W1963775782 @default.
- W2766696270 cites W1974224443 @default.
- W2766696270 cites W1984032639 @default.
- W2766696270 cites W1994773651 @default.
- W2766696270 cites W2004270866 @default.
- W2766696270 cites W2028344920 @default.
- W2766696270 cites W2038840577 @default.
- W2766696270 cites W2044581646 @default.
- W2766696270 cites W2060980641 @default.
- W2766696270 cites W2061481922 @default.
- W2766696270 cites W2063915017 @default.
- W2766696270 cites W2068866500 @default.
- W2766696270 cites W2074411007 @default.
- W2766696270 cites W2078246204 @default.
- W2766696270 cites W2084575458 @default.
- W2766696270 cites W2085088518 @default.
- W2766696270 cites W2086182182 @default.
- W2766696270 cites W2092297151 @default.
- W2766696270 cites W2097493124 @default.
- W2766696270 cites W2098167941 @default.
- W2766696270 cites W2103513664 @default.
- W2766696270 cites W2106246537 @default.
- W2766696270 cites W2108676219 @default.
- W2766696270 cites W2108921801 @default.
- W2766696270 cites W2115719856 @default.
- W2766696270 cites W2118245054 @default.
- W2766696270 cites W2119751130 @default.
- W2766696270 cites W2137321682 @default.
- W2766696270 cites W2139772076 @default.
- W2766696270 cites W2144450046 @default.
- W2766696270 cites W2152293013 @default.
- W2766696270 cites W2152505869 @default.
- W2766696270 cites W2153868685 @default.
- W2766696270 cites W2165732545 @default.
- W2766696270 cites W2170573838 @default.
- W2766696270 cites W2177415592 @default.
- W2766696270 cites W2180229411 @default.
- W2766696270 cites W2295774726 @default.
- W2766696270 cites W2322243210 @default.
- W2766696270 cites W2466398959 @default.
- W2766696270 cites W2475857717 @default.
- W2766696270 cites W2528084523 @default.
- W2766696270 cites W2598934409 @default.
- W2766696270 cites W2606056265 @default.
- W2766696270 doi "https://doi.org/10.7554/elife.28020" @default.
- W2766696270 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/5644950" @default.
- W2766696270 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/29039736" @default.
- W2766696270 hasPublicationYear "2017" @default.
- W2766696270 type Work @default.
- W2766696270 sameAs 2766696270 @default.
- W2766696270 citedByCount "39" @default.
- W2766696270 countsByYear W27666962702018 @default.
- W2766696270 countsByYear W27666962702019 @default.
- W2766696270 countsByYear W27666962702020 @default.
- W2766696270 countsByYear W27666962702021 @default.
- W2766696270 countsByYear W27666962702022 @default.
- W2766696270 countsByYear W27666962702023 @default.
- W2766696270 crossrefType "journal-article" @default.
- W2766696270 hasAuthorship W2766696270A5002861815 @default.
- W2766696270 hasAuthorship W2766696270A5007062297 @default.
- W2766696270 hasAuthorship W2766696270A5012018663 @default.
- W2766696270 hasAuthorship W2766696270A5025763229 @default.
- W2766696270 hasAuthorship W2766696270A5030756908 @default.
- W2766696270 hasAuthorship W2766696270A5032049756 @default.
- W2766696270 hasAuthorship W2766696270A5034303915 @default.
- W2766696270 hasAuthorship W2766696270A5034448543 @default.
- W2766696270 hasAuthorship W2766696270A5039137137 @default.
- W2766696270 hasAuthorship W2766696270A5041169651 @default.
- W2766696270 hasAuthorship W2766696270A5041773055 @default.
- W2766696270 hasAuthorship W2766696270A5047899621 @default.