Literature DB >> 31938459

Discovery of VU6015929: A Selective Discoidin Domain Receptor 1/2 (DDR1/2) Inhibitor to Explore the Role of DDR1 in Antifibrotic Therapy.

Daniel E Jeffries1, Corina M Borza2, Anna L Blobaum3,4, Ambra Pozzi2,5, Craig W Lindsley1,3,4.   

Abstract

Herein, we report the discovery of a potent and selective dual DDR1/2 inhibitor, 7e (VU6015929), displaying low cytotoxicity, good kinome selectivity, and possessing an acceptable in vitro DMPK profile with good rodent in vivo pharmacokinetics. VU6015929 potently blocks collagen-induced DDR1 activation and collagen-IV production, suggesting DDR1 inhibition as an exciting target for antifibrotic therapy.
Copyright © 2019 American Chemical Society.

Entities:  

Year:  2019        PMID： 31938459      PMCID： PMC6956352          DOI： 10.1021/acsmedchemlett.9b00382

Source DB:  PubMed          Journal:  ACS Med Chem Lett        ISSN： 1948-5875            Impact factor:   4.345


  12 in total

1.  Identification of type II and III DDR2 inhibitors.

Authors:  André Richters; Hoang D Nguyen; Trang Phan; Jeffrey R Simard; Christian Grütter; Julian Engel; Daniel Rauh
Journal:  J Med Chem       Date:  2014-05-05       Impact factor: 7.446

Review 2.  The Role of Discoidin Domain Receptor 1 in Inflammation, Fibrosis and Renal Disease.

Authors:  Aude Dorison; Jean-Claude Dussaule; Christos Chatziantoniou
Journal:  Nephron       Date:  2017-07-26       Impact factor: 2.847

Review 3.  Cell signaling by receptor tyrosine kinases.

Authors:  Mark A Lemmon; Joseph Schlessinger
Journal:  Cell       Date:  2010-06-25       Impact factor: 41.582

4.  Discoidin domain receptor 1 kinase activity is required for regulating collagen IV synthesis.

Authors:  Corina M Borza; Yan Su; Truc-Linh Tran; Ling Yu; Nick Steyns; Kayla J Temple; Marcin J Skwark; Jens Meiler; Craig W Lindsley; Brennan R Hicks; Birgit Leitinger; Roy Zent; Ambra Pozzi
Journal:  Matrix Biol       Date:  2016-12-01       Impact factor: 11.583

5.  Genetic inhibition of discoidin domain receptor 1 protects mice against crescentic glomerulonephritis.

Authors:  Monique Kerroch; Dominique Guerrot; Sophie Vandermeersch; Sandrine Placier; Laurent Mesnard; Chantal Jouanneau; Eric Rondeau; Pierre Ronco; Jean-Jacques Boffa; Christos Chatziantoniou; Jean-Claude Dussaule
Journal:  FASEB J       Date:  2012-07-02       Impact factor: 5.191

6.  Structural mechanisms determining inhibition of the collagen receptor DDR1 by selective and multi-targeted type II kinase inhibitors.

Authors:  Peter Canning; Li Tan; Kiki Chu; Sam W Lee; Nathanael S Gray; Alex N Bullock
Journal:  J Mol Biol       Date:  2014-04-23       Impact factor: 5.469

7.  Characterization of DDR2 Inhibitors for the Treatment of DDR2 Mutated Nonsmall Cell Lung Cancer.

Authors:  Hideki Terai; Li Tan; Ellen M Beauchamp; John M Hatcher; Qingsong Liu; Matthew Meyerson; Nathanael S Gray; Peter S Hammerman
Journal:  ACS Chem Biol       Date:  2015-09-25       Impact factor: 5.100

8.  Selective pharmacological inhibition of DDR1 prevents experimentally-induced glomerulonephritis in prevention and therapeutic regime.

Authors:  Solange Moll; Yukari Yasui; Ahmed Abed; Takeshi Murata; Hideaki Shimada; Akira Maeda; Naoshi Fukushima; Masakazu Kanamori; Sabine Uhles; Laura Badi; Thomas Cagarelli; Ivan Formentini; Faye Drawnel; Guy Georges; Tobias Bergauer; Rodolfo Gasser; R Daniel Bonfil; Rafael Fridman; Hans Richter; Juergen Funk; Marcus J Moeller; Christos Chatziantoniou; Marco Prunotto
Journal:  J Transl Med       Date:  2018-06-01       Impact factor: 5.531

9.  Structure-Based Design of Tetrahydroisoquinoline-7-carboxamides as Selective Discoidin Domain Receptor 1 (DDR1) Inhibitors.

Authors:  Zhen Wang; Huan Bian; Sergio G Bartual; Wenting Du; Jinfeng Luo; Hu Zhao; Shasha Zhang; Cheng Mo; Yang Zhou; Yong Xu; Zhengchao Tu; Xiaomei Ren; Xiaoyun Lu; Rolf A Brekken; Libo Yao; Alex N Bullock; Jin Su; Ke Ding
Journal:  J Med Chem       Date:  2016-06-03       Impact factor: 7.446

10.  DNA-Encoded Library-Derived DDR1 Inhibitor Prevents Fibrosis and Renal Function Loss in a Genetic Mouse Model of Alport Syndrome.

Authors:  Hans Richter; Alexander L Satz; Marc Bedoucha; Bernd Buettelmann; Ann C Petersen; Anja Harmeier; Ricardo Hermosilla; Remo Hochstrasser; Dominique Burger; Bernard Gsell; Rodolfo Gasser; Sylwia Huber; Melanie N Hug; Buelent Kocer; Bernd Kuhn; Martin Ritter; Markus G Rudolph; Franziska Weibel; Judith Molina-David; Jin-Ju Kim; Javier Varona Santos; Martine Stihle; Guy J Georges; R Daniel Bonfil; Rafael Fridman; Sabine Uhles; Solange Moll; Christian Faul; Alessia Fornoni; Marco Prunotto
Journal:  ACS Chem Biol       Date:  2018-12-16       Impact factor: 5.100
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  6 in total

1.  Discovery of 4-cyclopropyl-3-(2-((1-cyclopropyl-1H-pyrazol-4-yl) amino) quinazolin-6-yl)-N-(3-(trifluoromethyl) phenyl) benzamides as potent discoidin domain receptor inhibitors for the treatment of idiopathic pulmonary fibrosis.

Authors:  Qi Wang; Bixi Tang; Dandan Sun; Ying Dong; Yinchun Ji; Huanyu Shi; Liwei Zhou; Yueyue Yang; Menglan Luo; Qian Tan; Lin Chen; Yue Dong; Cong Li; Rongrong Xie; Yi Zang; Jingkang Shen; Bing Xiong; Jia Li; Danqi Chen
Journal:  Acta Pharm Sin B       Date:  2021-11-17       Impact factor: 14.903

2.  Discovery of a novel DDRs kinase inhibitor XBLJ-13 for the treatment of idiopathic pulmonary fibrosis.

Authors:  Ying Dong; Bi-Xi Tang; Qi Wang; Li-Wei Zhou; Cong Li; Xuan Zhang; Dan-Dan Sun; Xin Sun; Xue-Mei Zhang; Bing Xiong; Jia Li; Hong Shi; Dan-Qi Chen; Yi Zang
Journal:  Acta Pharmacol Sin       Date:  2021-11-24       Impact factor: 7.169

3.  Inhibitors of Discoidin Domain Receptor (DDR) Kinases for Cancer and Inflammation.

Authors:  William A Denny; Jack U Flanagan
Journal:  Biomolecules       Date:  2021-11-10

4.  The Collagen Receptor Discoidin Domain Receptor 1b Enhances Integrin β1-Mediated Cell Migration by Interacting With Talin and Promoting Rac1 Activation.

Authors:  Corina M Borza; Gema Bolas; Xiuqi Zhang; Mary Beth Browning Monroe; Ming-Zhi Zhang; Jens Meiler; Marcin J Skwark; Raymond C Harris; Lynne A Lapierre; James R Goldenring; Magnus Hook; Jose Rivera; Kyle L Brown; Birgit Leitinger; Matthew J Tyska; Markus Moser; Ralph T Böttcher; Roy Zent; Ambra Pozzi
Journal:  Front Cell Dev Biol       Date:  2022-03-03

Review 5.  Genetic and pharmacological tools to study the role of discoidin domain receptors in kidney disease.

Authors:  Corina M Borza; Gema Bolas; Ambra Pozzi
Journal:  Front Pharmacol       Date:  2022-09-28       Impact factor: 5.988

6.  DDR1 contributes to kidney inflammation and fibrosis by promoting the phosphorylation of BCR and STAT3.

Authors:  Corina M Borza; Gema Bolas; Fabian Bock; Xiuqi Zhang; Favour C Akabogu; Ming-Zhi Zhang; Mark de Caestecker; Min Yang; Haichun Yang; Ethan Lee; Leslie Gewin; Agnes B Fogo; W Hayes McDonald; Roy Zent; Ambra Pozzi
Journal:  JCI Insight       Date:  2022-02-08
  6 in total

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