Identification of a novel class of autotaxin inhibitors through cross-screening

Diana Castagna; Emma L. Duffy; Dima  Semaan; Louise C. Young; John M. Pritchard; Simon J. F. Macdonald; David C. Budd; Craig Jamieson; Allan J. B. Watson

doi:10.1039/C5MD00081E

Identification of a novel class of autotaxin inhibitors through cross-screening

Diana Castagna, Emma L. Duffy, Dima Semaan, Louise C. Young, John M. Pritchard, Simon J. F. Macdonald, David C. Budd, Craig Jamieson, Allan J. B. Watson

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Abstract

Three novel series were generated in order to mimic the pharmacophoric features displayed by lead compound AM095, a Lysophosphatidic acid (LPA1) receptor antagonist. Biological evaluation of this array of putative LPA1 antagonists led us to the discovery of three novel series of inhibitors of the ecto-enzyme Autotaxin (ATX), responsible for LPA production in blood, with potencies in the range 1 – 4 μM accompanied with good (> 100 μg/mL) solubility.

Original language	English
Pages (from-to)	1149-1155
Number of pages	6
Journal	MedChemComm
Volume	2015
Issue number	6
Early online date	8 May 2015
DOIs	https://doi.org/10.1039/C5MD00081E
Publication status	Published - 1 Jun 2015

Keywords

autotaxin
drug discovery
lysophosphatidic acid
lead compound
inhibitor

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Castagna-etal-MCC-2015-Identification-of-a-novel-class-of-autotaxin-inhibitors-throughAccepted author manuscript, 1.09 MB

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abstract = "Three novel series were generated in order to mimic the pharmacophoric features displayed by lead compound AM095, a Lysophosphatidic acid (LPA1) receptor antagonist. Biological evaluation of this array of putative LPA1 antagonists led us to the discovery of three novel series of inhibitors of the ecto-enzyme Autotaxin (ATX), responsible for LPA production in blood, with potencies in the range 1 – 4 μM accompanied with good (> 100 μg/mL) solubility. ",

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author = "Diana Castagna and Duffy, {Emma L.} and Dima Semaan and Young, {Louise C.} and Pritchard, {John M.} and Macdonald, {Simon J. F.} and Budd, {David C.} and Craig Jamieson and Watson, {Allan J. B.}",

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AU - Castagna, Diana

AU - Duffy, Emma L.

AU - Semaan, Dima

AU - Young, Louise C.

AU - Pritchard, John M.

AU - Macdonald, Simon J. F.

AU - Budd, David C.

AU - Jamieson, Craig

AU - Watson, Allan J. B.

PY - 2015/6/1

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N2 - Three novel series were generated in order to mimic the pharmacophoric features displayed by lead compound AM095, a Lysophosphatidic acid (LPA1) receptor antagonist. Biological evaluation of this array of putative LPA1 antagonists led us to the discovery of three novel series of inhibitors of the ecto-enzyme Autotaxin (ATX), responsible for LPA production in blood, with potencies in the range 1 – 4 μM accompanied with good (> 100 μg/mL) solubility.

AB - Three novel series were generated in order to mimic the pharmacophoric features displayed by lead compound AM095, a Lysophosphatidic acid (LPA1) receptor antagonist. Biological evaluation of this array of putative LPA1 antagonists led us to the discovery of three novel series of inhibitors of the ecto-enzyme Autotaxin (ATX), responsible for LPA production in blood, with potencies in the range 1 – 4 μM accompanied with good (> 100 μg/mL) solubility.

KW - autotaxin

KW - drug discovery

KW - lysophosphatidic acid

KW - lead compound

KW - inhibitor

UR - http://pubs.rsc.org/en/Content/ArticleLanding/2015/MD/C5MD00081E#!divAbstract

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JO - MedChemComm

JF - MedChemComm

IS - 6

ER -

Identification of a novel class of autotaxin inhibitors through cross-screening

Abstract

Keywords

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