Potent and selective inhibitors of the proteasome: dipeptidyl boronic acids.

Bioorganic & medicinal chemistry letters ·Vol. 8 ·No. 4 ·1998-02-17 ·Pages 333-8

Adams J, Behnke M, Chen S, Cruickshank AA, Dick LR, Grenier L, Klunder JM, Ma YT, Plamondon L, Stein RL

Abstract

Potent and selective dipeptidyl boronic acid proteasome inhibitors are described. As compared to peptidyl aldehyde compounds, boronic acids in this series display dramatically enhanced potency. Compounds such as 15 are promising new therapeutics for treatment of cancer and inflammatory diseases.

MeSH Terms

Boronic Acids/chemistry,pharmacology Cysteine Endopeptidases/drug effects Molecular Structure Multienzyme Complexes/drug effects Protease Inhibitors/chemistry,pharmacology Proteasome Endopeptidase Complex

Chemicals

Boronic Acids Multienzyme Complexes Protease Inhibitors Cysteine Endopeptidases Proteasome Endopeptidase Complex

Authors & Affiliations

10 authors, click to expand affiliations / ORCID

Adams J

ProScript, Inc., Cambridge, MA 02139, USA.

Behnke M

Chen S

Cruickshank A A

Dick L R

Grenier L

Klunder J M

Ma Y T

Plamondon L

Stein R L

Article Info

Journal

Bioorganic & medicinal chemistry letters

Abbr.

Bioorg Med Chem Lett

ISSN

0960-894X

DOI

10.1016/s0960-894x(98)00029-8

Published

1998-02-17

Pages

333-8

Language

English

Region

England

NLM ID

9107377

Subset

External Links

PubMed source DOI: 10.1016/s0960-894x(98)00029-8 View journal details

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Potent and selective inhibitors of the proteasome: dipeptidyl boronic acids.

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