Bioorganic and Medicinal Chemistry Letters, volume 15, issue 11, pages 2829-2833

Design, synthesis, and biological evaluation of novel human 5′-deoxy-5′-methylthioadenosine phosphorylase (MTAP) substrates

Pei-Pei Kung ¹

Luke R Zehnder ¹

Jerry J. Meng ¹

Stanley W Kupchinsky ¹

Donald J. Skalitzky ¹

M Catherine Johnson ¹

Karen A. Maegley ¹

Anne Ekker ¹

Leslie A. Kuhn ¹

Peter G. Peter E. Rose1 ¹

Laura A Bloom ¹

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Pfizer Global Research & Development-La Jolla, 10770 Science Center Drive, San Diego, CA 92121, USA. |

Publication type: Journal Article

Publication date: 2005-06-01

Elsevier

Journal: Bioorganic and Medicinal Chemistry Letters

scimago Q2

SJR: 0.508

CiteScore: 5.7

Impact factor: 2.5

ISSN: 0960894X, 14643405

DOI: 10.1016/j.bmcl.2005.03.107

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PubMed ID: 15911263

Organic Chemistry

Drug Discovery

Biochemistry

Molecular Biology

Pharmaceutical Science

Clinical Biochemistry

Molecular Medicine

Abstract

The structure-based design, chemical synthesis, and biological evaluation of novel MTAP substrates are described. These compounds incorporate various C5'-moieties and are shown to have different k(cat)/K(m) values compared with the natural MTAP substrate (MTA).

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Publisher

Elsevier

Journal

Bioorganic and Medicinal Chemistry Letters

scimago Q2

SJR

0.508

CiteScore

5.7

Impact factor

2.5

ISSN

0960894X (Print)

14643405 (Electronic)

Design, synthesis, and biological evaluation of novel human 5′-deoxy-5′-methylthioadenosine phosphorylase (MTAP) substrates

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