Structure-based design, synthesis, and in vitro assay of novel nucleoside analog inhibitors against HIV-1 reverse transcriptase

Xianjun Liu; Wei Xie; Raven H. Huang

doi:10.1016/j.bmcl.2005.05.099

Structure-based design, synthesis, and in vitro assay of novel nucleoside analog inhibitors against HIV-1 reverse transcriptase

Xianjun Liu, Wei Xie, Raven H. Huang

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

Abstract

Crystal structure of HIV-RT in complex with a DNA template:primer and a dTTP leads us to design and synthesize a new class of nucleoside analog inhibitors containing a branched 3′-group against HIV-RT. An in vitro primer extension assay indicates that three out of five compounds are effective HIV-RT inhibitors.

Original language	English (US)
Pages (from-to)	3775-3777
Number of pages	3
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	15
Issue number	16
DOIs	https://doi.org/10.1016/j.bmcl.2005.05.099
State	Published - Aug 15 2005

Keywords

HIV-RT
Nucleoside analogs
Primer extension assay
RT inhibitors
Structure-based design

ASJC Scopus subject areas

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

Online availability

10.1016/j.bmcl.2005.05.099

Library availability

Discover UIUC Full Text

Cite this

@article{73223352e18a4df7a7100d1ea0981384,

title = "Structure-based design, synthesis, and in vitro assay of novel nucleoside analog inhibitors against HIV-1 reverse transcriptase",

abstract = "Crystal structure of HIV-RT in complex with a DNA template:primer and a dTTP leads us to design and synthesize a new class of nucleoside analog inhibitors containing a branched 3′-group against HIV-RT. An in vitro primer extension assay indicates that three out of five compounds are effective HIV-RT inhibitors.",

keywords = "HIV-RT, Nucleoside analogs, Primer extension assay, RT inhibitors, Structure-based design",

author = "Xianjun Liu and Wei Xie and Huang, {Raven H.}",

note = "Funding Information: This work was supported by the start-up fund from University of Illinois at Urbana-Champaign and a grant from American Cancer Society, Illinois Division. We thank R. Switzer and D. Kranz for a critical reading of the manuscript. ",

year = "2005",

month = aug,

day = "15",

doi = "10.1016/j.bmcl.2005.05.099",

language = "English (US)",

volume = "15",

pages = "3775--3777",

journal = "Bioorganic and Medicinal Chemistry Letters",

issn = "0960-894X",

publisher = "Elsevier Ltd",

number = "16",

}

TY - JOUR

T1 - Structure-based design, synthesis, and in vitro assay of novel nucleoside analog inhibitors against HIV-1 reverse transcriptase

AU - Liu, Xianjun

AU - Xie, Wei

AU - Huang, Raven H.

N1 - Funding Information: This work was supported by the start-up fund from University of Illinois at Urbana-Champaign and a grant from American Cancer Society, Illinois Division. We thank R. Switzer and D. Kranz for a critical reading of the manuscript.

PY - 2005/8/15

Y1 - 2005/8/15

N2 - Crystal structure of HIV-RT in complex with a DNA template:primer and a dTTP leads us to design and synthesize a new class of nucleoside analog inhibitors containing a branched 3′-group against HIV-RT. An in vitro primer extension assay indicates that three out of five compounds are effective HIV-RT inhibitors.

AB - Crystal structure of HIV-RT in complex with a DNA template:primer and a dTTP leads us to design and synthesize a new class of nucleoside analog inhibitors containing a branched 3′-group against HIV-RT. An in vitro primer extension assay indicates that three out of five compounds are effective HIV-RT inhibitors.

KW - HIV-RT

KW - Nucleoside analogs

KW - Primer extension assay

KW - RT inhibitors

KW - Structure-based design

UR - http://www.scopus.com/inward/record.url?scp=22844433211&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=22844433211&partnerID=8YFLogxK

U2 - 10.1016/j.bmcl.2005.05.099

DO - 10.1016/j.bmcl.2005.05.099

M3 - Article

C2 - 15993595

AN - SCOPUS:22844433211

SN - 0960-894X

VL - 15

SP - 3775

EP - 3777

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 16

ER -

Structure-based design, synthesis, and in vitro assay of novel nucleoside analog inhibitors against HIV-1 reverse transcriptase

Abstract

Keywords

ASJC Scopus subject areas

Online availability

Library availability

Related links

Fingerprint

Cite this