Literature DB >> 12951093

Design and synthesis of dimeric HIV-1 integrase inhibitory peptides.

Krzysztof Krajewski1, Ya-Qiu Long, Christophe Marchand, Yves Pommier, Peter P Roller.   

Abstract

Dimers of known HIV-1 integrase inhibitory hexapeptide H-His-Cys-Lys-Phe-Trp-Trp-NH(2) containing different lengths of cross linkers in the place of cysteine residue, were designed, and synthesized. The inhibitory potency of these dimeric peptides is consistently higher than the lead hexapeptide. The dimeric peptide with djenkolic acid linker exhibited IC(50) values of 5.3 and 6.5 microM, for 3'-end processing and strand transfer, respectively.

Entities:  

Mesh:

Substances:

Year:  2003        PMID: 12951093     DOI: 10.1016/s0960-894x(03)00679-6

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  2 in total

Review 1.  HIV-1 IN inhibitors: 2010 update and perspectives.

Authors:  Christophe Marchand; Kasthuraiah Maddali; Mathieu Métifiot; Yves Pommier
Journal:  Curr Top Med Chem       Date:  2009       Impact factor: 3.295

2.  A symmetric region of the HIV-1 integrase dimerization interface is essential for viral replication.

Authors:  Erik Serrao; Wannes Thys; Jonas Demeulemeester; Laith Q Al-Mawsawi; Frauke Christ; Zeger Debyser; Nouri Neamati
Journal:  PLoS One       Date:  2012-09-18       Impact factor: 3.240

  2 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.