Synthesis of potent water-soluble tissue transglutaminase inhibitors

Martin Griffin; Alexandre Mongeot; Russell Collighan; Robert E. Saint; Richard A. Jones; Ian G.C. Coutts; Daniel L. Rathbone

doi:10.1016/j.bmcl.2008.09.006

Synthesis of potent water-soluble tissue transglutaminase inhibitors

Martin Griffin
, Alexandre Mongeot
, Russell Collighan
, Robert E. Saint
, Richard A. Jones
, Ian G.C. Coutts
, Daniel L. Rathbone

Biocity
Nottingham Trent University

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

67 Citations (Scopus)

Abstract

Dipeptide-based sulfonium peptidylmethylketones derived from 6-diazo-5-oxo-L-norleucine (DON) have been investigated as potential water-soluble inhibitors of extracellular transglutaminase. The lead compounds were prepared in four steps and exhibited potent activity against tissue transglutaminase.

Original language	English
Pages (from-to)	5559-5562
Number of pages	4
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	18
Issue number	20
DOIs	https://doi.org/10.1016/j.bmcl.2008.09.006
Publication status	Published - 15 Oct 2008

Keywords

transglutaminase
inhibitors
dipeptide

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10.1016/j.bmcl.2008.09.006

Cite this

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title = "Synthesis of potent water-soluble tissue transglutaminase inhibitors",

abstract = "Dipeptide-based sulfonium peptidylmethylketones derived from 6-diazo-5-oxo-L-norleucine (DON) have been investigated as potential water-soluble inhibitors of extracellular transglutaminase. The lead compounds were prepared in four steps and exhibited potent activity against tissue transglutaminase.",

keywords = "transglutaminase, inhibitors, dipeptide",

author = "Martin Griffin and Alexandre Mongeot and Russell Collighan and Saint, \{Robert E.\} and Jones, \{Richard A.\} and Coutts, \{Ian G.C.\} and Rathbone, \{Daniel L.\}",

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AU - Griffin, Martin

AU - Mongeot, Alexandre

AU - Collighan, Russell

AU - Saint, Robert E.

AU - Jones, Richard A.

AU - Coutts, Ian G.C.

AU - Rathbone, Daniel L.

PY - 2008/10/15

Y1 - 2008/10/15

N2 - Dipeptide-based sulfonium peptidylmethylketones derived from 6-diazo-5-oxo-L-norleucine (DON) have been investigated as potential water-soluble inhibitors of extracellular transglutaminase. The lead compounds were prepared in four steps and exhibited potent activity against tissue transglutaminase.

AB - Dipeptide-based sulfonium peptidylmethylketones derived from 6-diazo-5-oxo-L-norleucine (DON) have been investigated as potential water-soluble inhibitors of extracellular transglutaminase. The lead compounds were prepared in four steps and exhibited potent activity against tissue transglutaminase.

KW - transglutaminase

KW - inhibitors

KW - dipeptide

UR - https://www.scopus.com/pages/publications/53349166956

U2 - 10.1016/j.bmcl.2008.09.006

DO - 10.1016/j.bmcl.2008.09.006

M3 - Article

SN - 0960-894X

VL - 18

SP - 5559

EP - 5562

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 20

ER -

Synthesis of potent water-soluble tissue transglutaminase inhibitors

Abstract

Keywords

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