Discovery of a structurally novel, drug-like and potent inhibitor of peptidylarginine deiminase

Patrizia Ferretti; U. Kin Pong; Barbora Vagaska; Rohan Merchant; Christopher J. Matthews; Charles M. Marson

doi:10.1039/c3md00091e

Discovery of a structurally novel, drug-like and potent inhibitor of peptidylarginine deiminase

Patrizia Ferretti
, U. Kin Pong
, Barbora Vagaska
, Rohan Merchant
, Christopher J. Matthews
, Charles M. Marson

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

11 Citations (Scopus)

Abstract

The synthesis and biological properties of a structurally novel, potent and non-peptidic inhibitor of peptidylarginine deiminase are described. The novel drug-like PAD inhibitor contains a 3,5-dihydroimidazol-4-one ring that replaces the acyclic guanidine-binding unit present in arginine residues. This new drug-like PAD inhibitor was effective at 100 nM or below and could have relevance to diseases in which PAD expression is up-regulated, including rheumatoid arthritis, cancer, multiple sclerosis, and neural injury.

Original language	English
Pages (from-to)	1109-1113
Number of pages	5
Journal	MedChemComm
Volume	4
Issue number	7
DOIs	https://doi.org/10.1039/c3md00091e
Publication status	Published - Jul 2013
Externally published	Yes

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This output contributes to the following UN Sustainable Development Goals (SDGs)

SDG 3 Good Health and Well-being

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10.1039/c3md00091e

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title = "Discovery of a structurally novel, drug-like and potent inhibitor of peptidylarginine deiminase",

abstract = "The synthesis and biological properties of a structurally novel, potent and non-peptidic inhibitor of peptidylarginine deiminase are described. The novel drug-like PAD inhibitor contains a 3,5-dihydroimidazol-4-one ring that replaces the acyclic guanidine-binding unit present in arginine residues. This new drug-like PAD inhibitor was effective at 100 nM or below and could have relevance to diseases in which PAD expression is up-regulated, including rheumatoid arthritis, cancer, multiple sclerosis, and neural injury.",

author = "Patrizia Ferretti and \{Kin Pong\}, U. and Barbora Vagaska and Rohan Merchant and Matthews, \{Christopher J.\} and Marson, \{Charles M.\}",

year = "2013",

month = jul,

doi = "10.1039/c3md00091e",

language = "English",

volume = "4",

pages = "1109--1113",

number = "7",

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T1 - Discovery of a structurally novel, drug-like and potent inhibitor of peptidylarginine deiminase

AU - Ferretti, Patrizia

AU - Kin Pong, U.

AU - Vagaska, Barbora

AU - Merchant, Rohan

AU - Matthews, Christopher J.

AU - Marson, Charles M.

PY - 2013/7

Y1 - 2013/7

N2 - The synthesis and biological properties of a structurally novel, potent and non-peptidic inhibitor of peptidylarginine deiminase are described. The novel drug-like PAD inhibitor contains a 3,5-dihydroimidazol-4-one ring that replaces the acyclic guanidine-binding unit present in arginine residues. This new drug-like PAD inhibitor was effective at 100 nM or below and could have relevance to diseases in which PAD expression is up-regulated, including rheumatoid arthritis, cancer, multiple sclerosis, and neural injury.

AB - The synthesis and biological properties of a structurally novel, potent and non-peptidic inhibitor of peptidylarginine deiminase are described. The novel drug-like PAD inhibitor contains a 3,5-dihydroimidazol-4-one ring that replaces the acyclic guanidine-binding unit present in arginine residues. This new drug-like PAD inhibitor was effective at 100 nM or below and could have relevance to diseases in which PAD expression is up-regulated, including rheumatoid arthritis, cancer, multiple sclerosis, and neural injury.

UR - https://www.scopus.com/pages/publications/84879877182

U2 - 10.1039/c3md00091e

DO - 10.1039/c3md00091e

M3 - Article

AN - SCOPUS:84879877182

SN - 2040-2503

VL - 4

SP - 1109

EP - 1113

JO - MedChemComm

JF - MedChemComm

IS - 7

ER -

Discovery of a structurally novel, drug-like and potent inhibitor of peptidylarginine deiminase

Abstract

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