Evaluation of triazolamers as active site inhibitors of HIV-1 protease

Andrea L. Jochim; Stephen E. Miller; Nicholas G. Angelo; Paramjit S. Arora

doi:10.1016/j.bmcl.2009.09.049

Evaluation of triazolamers as active site inhibitors of HIV-1 protease

Andrea L. Jochim, Stephen E. Miller, Nicholas G. Angelo, Paramjit S. Arora

Chemistry

Research output: Contribution to journal › Article › peer-review

Abstract

Proteases typically recognize their peptide substrates in extended conformations. General approaches for designing protease inhibitors often consist of peptidomimetics that feature this conformation. Herein we discuss a combination of computational and experimental studies to evaluate the potential of triazole-linked β-strand mimetics as inhibitors of HIV-1 protease activity.

Original language	English (US)
Pages (from-to)	6023-6026
Number of pages	4
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	19
Issue number	21
DOIs	https://doi.org/10.1016/j.bmcl.2009.09.049
State	Published - Nov 1 2009

Keywords

Peptidomimetics
Protease inhibitor
β-Strand mimetics

ASJC Scopus subject areas

Biochemistry
Molecular Medicine
Molecular Biology
Pharmaceutical Science
Drug Discovery
Clinical Biochemistry
Organic Chemistry

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10.1016/j.bmcl.2009.09.049

Cite this

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title = "Evaluation of triazolamers as active site inhibitors of HIV-1 protease",

abstract = "Proteases typically recognize their peptide substrates in extended conformations. General approaches for designing protease inhibitors often consist of peptidomimetics that feature this conformation. Herein we discuss a combination of computational and experimental studies to evaluate the potential of triazole-linked β-strand mimetics as inhibitors of HIV-1 protease activity.",

keywords = "Peptidomimetics, Protease inhibitor, β-Strand mimetics",

author = "Jochim, {Andrea L.} and Miller, {Stephen E.} and Angelo, {Nicholas G.} and Arora, {Paramjit S.}",

note = "Funding Information: We thank Professor Celia Schiffer, UMass Medical School Center for AIDS Research, for generous donation of the wild type HIV-1 protease. We are grateful to the NSF ( CHE 0848410 ) for financial support of this work, and also thank the NSF for equipment Grants MRI-0116222 and CHE-0234863, and the NCRR/NIH for Research Facilities Improvement Grant C06 RR-16572. ",

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AU - Jochim, Andrea L.

AU - Miller, Stephen E.

AU - Angelo, Nicholas G.

AU - Arora, Paramjit S.

N1 - Funding Information: We thank Professor Celia Schiffer, UMass Medical School Center for AIDS Research, for generous donation of the wild type HIV-1 protease. We are grateful to the NSF ( CHE 0848410 ) for financial support of this work, and also thank the NSF for equipment Grants MRI-0116222 and CHE-0234863, and the NCRR/NIH for Research Facilities Improvement Grant C06 RR-16572.

PY - 2009/11/1

Y1 - 2009/11/1

N2 - Proteases typically recognize their peptide substrates in extended conformations. General approaches for designing protease inhibitors often consist of peptidomimetics that feature this conformation. Herein we discuss a combination of computational and experimental studies to evaluate the potential of triazole-linked β-strand mimetics as inhibitors of HIV-1 protease activity.

AB - Proteases typically recognize their peptide substrates in extended conformations. General approaches for designing protease inhibitors often consist of peptidomimetics that feature this conformation. Herein we discuss a combination of computational and experimental studies to evaluate the potential of triazole-linked β-strand mimetics as inhibitors of HIV-1 protease activity.

KW - Peptidomimetics

KW - Protease inhibitor

KW - β-Strand mimetics

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Evaluation of triazolamers as active site inhibitors of HIV-1 protease

Abstract

Keywords

ASJC Scopus subject areas

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