FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W2787783539> ?p ?o ?g. }

• W2787783539 abstract "Hepatitis B virus (HBV) reverse transcriptase (RT) is essential for viral replication and is an important drug target. Nonetheless, the notorious insolubility of HBV RT has hindered experimental structural studies and structure-based drug design. Here, we demonstrate that a Q151M substitution alone at the nucleotide-binding site (N-site) of human immunodeficiency virus type-1 (HIV-1) RT renders HIV-1 highly sensitive to entecavir (ETV), a potent nucleoside analogue RT inhibitor (NRTI) against HBV. The results suggest that Met151 forms a transient hydrophobic interaction with the cyclopentyl methylene of ETV, a characteristic hydrophobic moiety of ETV. We thus solved the crystal structures of HIV-1 RTQ151M:DNA complex with bound dGTP or ETV-triphosphate (ETV-TP). The structures revealed that ETV-TP is accommodated at the N-site slightly apart from the ribose ring of the 3'-end nucleotide, compared to the position of bound dGTP and previously reported NRTI/dNTP. In addition, the protruding methylene group of bound ETV-TP directly pushes the side-chain of Met184 backward. Met184 is a key residue that confers ETV resistance upon substitution with smaller Ile/Val. These results provide novel insights into NRTI binding to the N-site and further provide important clues for the development of novel anti-HBV/HIV-1 RT inhibitors to overcome critical drug resistance." @default.
• W2787783539 created "2018-02-23" @default.
• W2787783539 creator A5024405418 @default.
• W2787783539 creator A5034448543 @default.
• W2787783539 creator A5036478128 @default.
• W2787783539 creator A5037650438 @default.
• W2787783539 creator A5047899621 @default.
• W2787783539 creator A5055989025 @default.
• W2787783539 creator A5064404772 @default.
• W2787783539 creator A5084560457 @default.
• W2787783539 date "2018-01-26" @default.
• W2787783539 modified "2023-10-11" @default.
• W2787783539 title "HIV-1 with HBV-associated Q151M substitution in RT becomes highly susceptible to entecavir: structural insights into HBV-RT inhibition by entecavir" @default.
• W2787783539 cites W1585930597 @default.
• W2787783539 cites W1603287226 @default.
• W2787783539 cites W1771400641 @default.
• W2787783539 cites W1966200141 @default.
• W2787783539 cites W1973938190 @default.
• W2787783539 cites W1981526509 @default.
• W2787783539 cites W1989189545 @default.
• W2787783539 cites W1994961350 @default.
• W2787783539 cites W2005228785 @default.
• W2787783539 cites W2008428638 @default.
• W2787783539 cites W2024024034 @default.
• W2787783539 cites W2043497020 @default.
• W2787783539 cites W2069618817 @default.
• W2787783539 cites W2074658918 @default.
• W2787783539 cites W2078246204 @default.
• W2787783539 cites W2085965763 @default.
• W2787783539 cites W2087564721 @default.
• W2787783539 cites W2088618014 @default.
• W2787783539 cites W2095855829 @default.
• W2787783539 cites W2102059779 @default.
• W2787783539 cites W2107057287 @default.
• W2787783539 cites W2108921801 @default.
• W2787783539 cites W2110383908 @default.
• W2787783539 cites W2110847666 @default.
• W2787783539 cites W2114002124 @default.
• W2787783539 cites W2123144952 @default.
• W2787783539 cites W2124026197 @default.
• W2787783539 cites W2129923672 @default.
• W2787783539 cites W2130575875 @default.
• W2787783539 cites W2138764171 @default.
• W2787783539 cites W2146080841 @default.
• W2787783539 cites W2147234591 @default.
• W2787783539 cites W2147264814 @default.
• W2787783539 cites W2150085512 @default.
• W2787783539 cites W2152866400 @default.
• W2787783539 cites W2154714625 @default.
• W2787783539 cites W2159211495 @default.
• W2787783539 cites W2162520409 @default.
• W2787783539 cites W2165151174 @default.
• W2787783539 cites W2165989710 @default.
• W2787783539 cites W2166201309 @default.
• W2787783539 cites W2172120683 @default.
• W2787783539 cites W2180229411 @default.
• W2787783539 cites W2486192779 @default.
• W2787783539 cites W2606783704 @default.
• W2787783539 cites W4248872320 @default.
• W2787783539 doi "https://doi.org/10.1038/s41598-018-19602-9" @default.
• W2787783539 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/5785976" @default.
• W2787783539 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/29374261" @default.
• W2787783539 hasPublicationYear "2018" @default.
• W2787783539 type Work @default.
• W2787783539 sameAs 2787783539 @default.
• W2787783539 citedByCount "14" @default.
• W2787783539 countsByYear W27877835392018 @default.
• W2787783539 countsByYear W27877835392019 @default.
• W2787783539 countsByYear W27877835392020 @default.
• W2787783539 countsByYear W27877835392021 @default.
• W2787783539 countsByYear W27877835392022 @default.
• W2787783539 countsByYear W27877835392023 @default.
• W2787783539 crossrefType "journal-article" @default.
• W2787783539 hasAuthorship W2787783539A5024405418 @default.
• W2787783539 hasAuthorship W2787783539A5034448543 @default.
• W2787783539 hasAuthorship W2787783539A5036478128 @default.
• W2787783539 hasAuthorship W2787783539A5037650438 @default.
• W2787783539 hasAuthorship W2787783539A5047899621 @default.
• W2787783539 hasAuthorship W2787783539A5055989025 @default.
• W2787783539 hasAuthorship W2787783539A5064404772 @default.
• W2787783539 hasAuthorship W2787783539A5084560457 @default.
• W2787783539 hasBestOaLocation W27877835391 @default.
• W2787783539 hasConcept C104317684 @default.
• W2787783539 hasConcept C156719811 @default.
• W2787783539 hasConcept C159047783 @default.
• W2787783539 hasConcept C185592680 @default.
• W2787783539 hasConcept C2522874641 @default.
• W2787783539 hasConcept C2776175608 @default.
• W2787783539 hasConcept C2776543447 @default.
• W2787783539 hasConcept C2777333352 @default.
• W2787783539 hasConcept C2777869810 @default.
• W2787783539 hasConcept C2780593183 @default.
• W2787783539 hasConcept C512185932 @default.
• W2787783539 hasConcept C55493867 @default.
• W2787783539 hasConcept C67705224 @default.
• W2787783539 hasConcept C71240020 @default.
• W2787783539 hasConcept C86803240 @default.
• W2787783539 hasConceptScore W2787783539C104317684 @default.
• W2787783539 hasConceptScore W2787783539C156719811 @default.
• W2787783539 hasConceptScore W2787783539C159047783 @default.

• next