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

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

44 Scopus citations

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
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 - 1 Nov 2009
Externally published	Yes

Keywords

Peptidomimetics
Protease inhibitor
β-Strand mimetics

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10.1016/j.bmcl.2009.09.049

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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. ",

year = "2009",

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doi = "10.1016/j.bmcl.2009.09.049",

language = "English",

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journal = "Bioorganic and Medicinal Chemistry Letters",

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TY - JOUR

T1 - Evaluation of triazolamers as active site inhibitors of HIV-1 protease

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

UR - https://www.scopus.com/pages/publications/71749114881

U2 - 10.1016/j.bmcl.2009.09.049

DO - 10.1016/j.bmcl.2009.09.049

M3 - Article

C2 - 19800230

AN - SCOPUS:71749114881

SN - 0960-894X

VL - 19

SP - 6023

EP - 6026

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 21

ER -

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

Abstract

Keywords

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