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Optimization of a series of dipeptides with a P3 threonine residue as non-covalent inhibitors of the chymotrypsin-like activity of the human 20S proteasome

descriptionPublicationkeyboard_double_arrow_right Article 01 Nov 2010 English Publisher:Elsevier BVJournal:Bioorganic & Medicinal Chemistry Letters, volume 20, pages 6,581-6,586 (issn: 0960-894X,

Authors: Michael D. Sintchak; Khristofer Garcia; Jonathan L. Blank; Kenneth M. Gigstad; Frank J. Bruzzese; Matthew Jones; Zhigen Hu; +9 Authors

doi: 10.1016/j.bmcl.2010.09.032

pmid: 20875739

Optimization of a series of dipeptides with a P3 threonine residue as non-covalent inhibitors of the chymotrypsin-like activity of the human 20S proteasome

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Abstract

Starting from a tripeptide screening hit, a series of dipeptide inhibitors of the proteasome with Thr as the P3 residue has been optimized with the aid of crystal structures in complex with the β-5/6 active site of y20S. Derivative 25, (β5 IC(50)=7.4 nM) inhibits only the chymotryptic activity of the proteasome, shows cellular activity against targets in the UPS, and inhibits proliferation.

Related Organizations

Millennium Pharmaceuticals
United States

Keywords

Models, Molecular, Threonine, Proteasome Endopeptidase Complex, Chymotrypsin, Humans, Dipeptides

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22 Research products, page 1 of 3

Proteasome subunit beta type-3
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Proteasome subunit beta type-5
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3SDK
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Proteasome subunit alpha type-6
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Proteasome subunit alpha type-2
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Structure of yeast 20S open-gate proteasome with Compound 25
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Structure of yeast 20S open-gate proteasome with Compound 25
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Fields of Science (3) View all

medical and health sciences

basic medicine

Fields of Science

medical and health sciences

basic medicine

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