Literature DB >> 26745766

Development of Autotaxin Inhibitors: An Overview of the Patent and Primary Literature.

Diana Castagna1, David C Budd2, Simon J F Macdonald2, Craig Jamieson1, Allan J B Watson1.   

Abstract

The autotaxin-lysophophatidic acid (ATX-LPA) signaling pathway is implicated in a variety of human disease states including angiogenesis, autoimmune diseases, cancer, fibrotic diseases, inflammation, neurodegeneration, and neuropathic pain, among others. As a result, ATX-LPA has become of significant interest within both the industrial and the academic communities. This review aims to provide a concise overview of the development of novel ATX inhibitors, including the disclosure of the first ATX clinical trial data.

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Year:  2016        PMID： 26745766     DOI： 10.1021/acs.jmedchem.5b01599

Source DB:  PubMed          Journal:  J Med Chem        ISSN： 0022-2623            Impact factor:   7.446


  17 in total

1.  Activity-Based DNA-Encoded Library Screening.

Authors:  Wesley G Cochrane; Marie L Malone; Vuong Q Dang; Valerie Cavett; Alexander L Satz; Brian M Paegel
Journal:  ACS Comb Sci       Date:  2019-03-29       Impact factor: 3.784

2.  Role of the autotaxin-lysophosphatidic acid axis in glaucoma, aqueous humor drainage and fibrogenic activity.

Authors:  Leona T Y Ho; Anja Osterwald; Iris Ruf; Daniel Hunziker; Patrizio Mattei; Pratap Challa; Robin Vann; Christoph Ullmer; Ponugoti Vasanth Rao
Journal:  Biochim Biophys Acta Mol Basis Dis       Date:  2019-10-21       Impact factor: 5.187

3.  Discovery of BI-2545: A Novel Autotaxin Inhibitor That Significantly Reduces LPA Levels in Vivo.

Authors:  Christian A Kuttruff; Marco Ferrara; Tom Bretschneider; Stefan Hoerer; Sandra Handschuh; Bernd Nosse; Helmut Romig; Paul Nicklin; Gerald J Roth
Journal:  ACS Med Chem Lett       Date:  2017-11-08       Impact factor: 4.345

4.  Autocrine lysophosphatidic acid signaling activates β-catenin and promotes lung allograft fibrosis.

Authors:  Pengxiu Cao; Yoshiro Aoki; Linda Badri; Natalie M Walker; Casey M Manning; Amir Lagstein; Eric R Fearon; Vibha N Lama
Journal:  J Clin Invest       Date:  2017-02-27       Impact factor: 14.808

5.  Discovery and Optimization of Selective and in Vivo Active Inhibitors of the Lysophosphatidylserine Lipase α/β-Hydrolase Domain-Containing 12 (ABHD12).

Authors:  Daisuke Ogasawara; Taka-Aki Ichu; Hui Jing; Jonathan J Hulce; Alex Reed; Olesya A Ulanovskaya; Benjamin F Cravatt
Journal:  J Med Chem       Date:  2019-02-05       Impact factor: 7.446

6.  Characterization of the properties of a selective, orally bioavailable autotaxin inhibitor in preclinical models of advanced stages of liver fibrosis.

Authors:  Manuel Baader; Tom Bretschneider; Andre Broermann; Joerg F Rippmann; Birgit Stierstorfer; Christian A Kuttruff; Michael Mark
Journal:  Br J Pharmacol       Date:  2018-01-17       Impact factor: 8.739

7.  Molecular modelling guided design, synthesis and QSAR analysis of new small molecule non-lipid autotaxin inhibitors.

Authors:  Souvik Banerjee; Derek D Norman; Shanshan Deng; Sayo O Fakayode; Sue Chin Lee; Abby L Parrill; Wei Li; Duane D Miller; Gabor J Tigyi
Journal:  Bioorg Chem       Date:  2020-08-26       Impact factor: 5.275

Review 8.  Autotaxin-Lysophosphatidic Acid: From Inflammation to Cancer Development.

Authors:  Silvia Anahi Valdés-Rives; Aliesha González-Arenas
Journal:  Mediators Inflamm       Date:  2017-12-21       Impact factor: 4.711

9.  Discovery of Potent Selective Nonzinc Binding Autotaxin Inhibitor BIO-32546.

Authors:  Bin Ma; Lei Zhang; Lihong Sun; Zhili Xin; Gnanasambandam Kumaravel; Douglas Marcotte; Jayanth V Chodaparambil; Qin Wang; Angela Wehr; Jing Jing; Victor Sukbong Hong; Ti Wang; Carol Huang; Zhaohui Shao; Sha Mi
Journal:  ACS Med Chem Lett       Date:  2021-06-14       Impact factor: 4.632

10.  Autotaxin determines colitis severity in mice and is secreted by B cells in the colon.

Authors:  Songbai Lin; Abedul Haque; Reben Raeman; Leilei Guo; Peijian He; Timothy L Denning; Bassel El-Rayes; Wouter H Moolenaar; C Chris Yun
Journal:  FASEB J       Date:  2018-11-27       Impact factor: 5.834
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