Inhibitors | Comment | Organism | Structure |
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4'-ethynyl-2-fluoro-2'-deoxyadenosine | a translocation defective RT inhibitor, able to inhibit both WT and multi-drug resistant strains of HIV several orders of magnitude, modeling of the ternary complex of HIV-1 RT/DNA/inhibitor, overview. The 4'-ethynyl group is stabilized in a hydrophobic pocket formed by enzyme residues Ala114, Tyr115, Phe160, Met184, and the aliphatic segment of Asp185 | Human immunodeficiency virus 1 | |
additional information | nucleoside reverse transcriptase inhibitors mimic the natural dNTP substrate of the enzyme and bind to the 3'-primer terminus in the polymerase active site acting as chain terminators. A lack of a 3'-OH group promotes effective chain termination, but it also imparts a negative effect on the potency of the NRTI, including a diminished binding affinity for the RT target and decreased ability to be activated by cellular kinases. nucleoside reverse transcriptase inhibitors with 4'-substitutions and a 3'-OH are very effective at inhibiting both wild-type and multi-drug resistant strains of HIV, structure-function analysis, overview | Human immunodeficiency virus 1 |
Organism | UniProt | Comment | Textmining |
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Human immunodeficiency virus 1 | - |
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Synonyms | Comment | Organism |
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HIV reverse transcriptase | - |
Human immunodeficiency virus 1 |