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

School of Chemistry

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

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	7
Journal	MedChemComm
Volume	2015
Issue number	6
DOIs	https://doi.org/10.1039/C5MD00081E
Publication status	Published - 1 Jun 2015

Keywords

autotaxin
drug discovery
lysophosphatidic acid
lead compound
inhibitor

Access to Document

10.1039/C5MD00081E

Handle.net

Persistent link

Cite this

@article{67cfeeb7727d4c0c808dccd7ca1c960d,

title = "Identification of a novel class of autotaxin inhibitors through cross-screening",

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.",

keywords = "autotaxin, drug discovery, lysophosphatidic acid, lead compound, inhibitor",

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.\}",

year = "2015",

month = jun,

day = "1",

doi = "10.1039/C5MD00081E",

language = "English",

volume = "2015",

pages = "1149--1155",

journal = "MedChemComm",

issn = "2040-2503",

publisher = "Royal Society of Chemistry",

number = "6",

}

TY - JOUR

T1 - Identification of a novel class of autotaxin inhibitors through cross-screening

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

Y1 - 2015/6/1

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 - https://www.scopus.com/pages/publications/84935836533

U2 - 10.1039/C5MD00081E

DO - 10.1039/C5MD00081E

M3 - Article

SN - 2040-2503

VL - 2015

SP - 1149

EP - 1155

JO - MedChemComm

JF - MedChemComm

IS - 6

ER -

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

Abstract

Keywords

Access to Document

Handle.net

Other files and links

Fingerprint

Cite this