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Peptide, Peptidomimetic and Small‐molecule Drug Discovery Targeting HIV‐1 Host‐cell Attachment and Entry through gp120, gp41, CCR5 and CXCR4 †
Author(s) -
Kazmierski Wieslaw M.,
Kenakin Terry P.,
Gudmundsson Kristjan S.
Publication year - 2006
Publication title -
chemical biology and drug design
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.59
H-Index - 77
eISSN - 1747-0285
pISSN - 1747-0277
DOI - 10.1111/j.1747-0285.2005.00319.x
Subject(s) - peptidomimetic , gp41 , chemistry , peptide , drug discovery , human immunodeficiency virus (hiv) , small molecule , drug , molecule , combinatorial chemistry , biophysics , stereochemistry , biochemistry , virology , biology , pharmacology , organic chemistry , immunology , antigen , epitope
This review highlights selected examples of peptide, peptidomimetic and small‐molecule drug discovery targeting HIV‐1 to advance novel anti‐HIV pharmaceuticals that inhibit initial stages of the viral cycle; namely, attachment and entry. Some of these approaches have culminated in the development of peptide‐based drugs, while other have exploited peptides as enabling tools toward the identification of small‐molecule lead compounds. Both of these conceptually different approaches have facilitated lead optimization of molecules with complementary and often surprising anti‐HIV pharmacological properties, supporting their role in pharmaceutical development. Furthermore, such molecules enabled mechanistic elucidation of viral attachment and entry and provided additional insights toward achieving the desired drug profile.