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Literature summary for 3.4.23.16 extracted from

  • Tojo, Y.; Koh, Y.; Amano, M.; Aoki, M.; Das, D.; Ghosh, A.K.; Mitsuya, H.
    Novel Protease Inhibitors (PIs) Containing Macrocyclic Components and 3(R),3a(S),6a(R)-bis-Tetrahydrofuranylurethane (bis-THF) That Are Potent Against Multi-PI-Resistant HIV-1 Variants In Vitro (2010), Antimicrob. Agents Chemother., 54, 3460-3470.
    View publication on PubMedView publication on EuropePMC
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Cloned(Commentary)

Cloned (Comment) Organism
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 Human immunodeficiency virus 1

Protein Variants

Protein Variants Comment Organism
I84V occuring in HIV-1 variant, (3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-yl [(2S,3R)-3-hydroxy-4-[(7Z)-13-methoxy-1,1-dioxido-3,4,5,6,9,10-hexahydro-2H-11,1,2-benzoxathiazacyclotridecin-2-yl]-1-phenylbutan-2-yl]carbamate (GRL-216) prevented from blocking dimerization, HIV-1 resistence to (3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-yl [(2S,3R)-3-hydroxy-4-[(7Z)-13-methoxy-1,1-dioxido-3,4,5,6,9,10-hexahydro-2H-11,1,2-benzoxathiazacyclotridecin-2-yl]-1-phenylbutan-2-yl]carbamate (GRL-216) Human immunodeficiency virus 1
V82I occuring in HIV-1 variant, (3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-yl [(2S,3R)-3-hydroxy-4-[(7Z)-13-methoxy-1,1-dioxido-3,4,5,6,9,10-hexahydro-2H-11,1,2-benzoxathiazacyclotridecin-2-yl]-1-phenylbutan-2-yl]carbamate (GRL-216) prevented from blocking dimerization, HIV-1 resistence to (3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-yl [(2S,3R)-3-hydroxy-4-[(7Z)-13-methoxy-1,1-dioxido-3,4,5,6,9,10-hexahydro-2H-11,1,2-benzoxathiazacyclotridecin-2-yl]-1-phenylbutan-2-yl]carbamate (GRL-216) Human immunodeficiency virus 1

Inhibitors

Inhibitors Comment Organism Structure
(3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-yl [(2S,3R)-3-hydroxy-4-(13-methoxy-1,1-dioxido-3,4,5,6,7,8,9,10-octahydro-2H-11,1,2-benzoxathiazacyclotridecin-2-yl)-1-phenylbutan-2-yl]carbamate GRL-246 Human immunodeficiency virus 1
(3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-yl [(2S,3R)-3-hydroxy-4-[(7Z)-12-methoxy-1,1-dioxido-4,5,6,9-tetrahydro-10,1,2-benzoxathiazacyclododecin-2(3H)-yl]-1-phenylbutan-2-yl]carbamate GRL-396 Human immunodeficiency virus 1
(3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-yl [(2S,3R)-3-hydroxy-4-[(7Z)-13-methoxy-1,1-dioxido-3,4,5,6,9,10-hexahydro-2H-11,1,2-benzoxathiazacyclotridecin-2-yl]-1-phenylbutan-2-yl]carbamate GRL-216, blocks dimerization Human immunodeficiency virus 1
(3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-yl [(2S,3R)-3-hydroxy-4-[(7Z)-14-methoxy-1,1-dioxido-4,5,6,9,10,11-hexahydro-12,1,2-benzoxathiazacyclotetradecin-2(3H)-yl]-1-phenylbutan-2-yl]carbamate GRL-286, blocks dimerization Human immunodeficiency virus 1

Organism

Organism UniProt Comment Textmining
Human immunodeficiency virus 1
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Synonyms

Synonyms Comment Organism
HIV-1 protease
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 Human immunodeficiency virus 1