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A targeted covalent small molecule inhibitor of HIV-1 fusion.
Zhou, Guangyan; He, Li; Li, Kathy H; Pedroso, Cássio C S; Gochin, Miriam.
Afiliación
  • Zhou G; Department of Basic Sciences, Touro University California, 1310 Club Drive, Mare Island, Vallejo, CA 94592, USA. miriam.gochin@tu.edu.
  • He L; Department of Basic Sciences, Touro University California, 1310 Club Drive, Mare Island, Vallejo, CA 94592, USA. miriam.gochin@tu.edu.
  • Li KH; Department of Pharmaceutical Chemistry, UCSF School of Pharmacy, San Francisco, CA 94143, USA.
  • Pedroso CCS; Lawrence Berkeley National Laboratory, The Molecular Foundry, 1 Cyclotron Road, 67R5114, Berkeley, CA 94720, USA.
  • Gochin M; Department of Basic Sciences, Touro University California, 1310 Club Drive, Mare Island, Vallejo, CA 94592, USA. miriam.gochin@tu.edu and Department of Pharmaceutical Chemistry, UCSF School of Pharmacy, San Francisco, CA 94143, USA.
Chem Commun (Camb) ; 57(37): 4528-4531, 2021 May 06.
Article en En | MEDLINE | ID: mdl-33956029
ABSTRACT
We describe a low molecular weight covalent inhibitor targeting a conserved lysine residue within the hydrophobic pocket of HIV-1 glycoprotein-41. The inhibitor bound selectively to the hydrophobic pocket and exhibited an order of magnitude enhancement of anti-fusion activity against HIV-1 compared to its non-covalent counterpart. The findings represent a significant advance in the quest to obtain non-peptide fusion inhibitors.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Ésteres del Ácido Sulfúrico / Proteína gp41 de Envoltorio del VIH / VIH / Fármacos Anti-VIH / Inhibidores de Fusión de VIH / Bibliotecas de Moléculas Pequeñas Idioma: En Revista: Chem Commun (Camb) Asunto de la revista: QUIMICA Año: 2021 Tipo del documento: Article País de afiliación: Estados Unidos
Texto completo
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Ésteres del Ácido Sulfúrico / Proteína gp41 de Envoltorio del VIH / VIH / Fármacos Anti-VIH / Inhibidores de Fusión de VIH / Bibliotecas de Moléculas Pequeñas Idioma: En Revista: Chem Commun (Camb) Asunto de la revista: QUIMICA Año: 2021 Tipo del documento: Article País de afiliación: Estados Unidos