Discoidin domain receptor 1 (DDR1) kinase as target for structure-based drug discovery
TLDR
Recent discoveries of novel inhibitors and their co-crystal structure with the DDR1 kinase domain have made structure-based drug discovery for DDR1 amenable, and several established inhibitors, such as imatinib, dasatinib and nilotinib, have been found to inhibit DDR kinase activity.About:
This article is published in Drug Discovery Today.The article was published on 2015-02-01 and is currently open access. It has received 63 citations till now. The article focuses on the topics: Discoidin domain-containing receptor 2 & DDR1.read more
Citations
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Liver fibrosis: Direct antifibrotic agents and targeted therapies.
TL;DR: Targeted antifibrotic therapies that address molecules and mechanisms that are central to fibrogenesis or fibrolysis, including strategies that allow targeting of activated hepatic stellate cells and myofibroblasts and other fibrogenic effector cells are discussed.
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Extracellular matrix component signaling in cancer.
TL;DR: Roles of the three major matrix receptor types are summarized, with emphasis on how they function in tumor progression.
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Discoidin Domain Receptors: Potential Actors and Targets in Cancer
Hassan Rammal,Charles Saby,Kevin Magnien,Laurence Van-Gulick,Roselyne Garnotel,Emilie Buache,Hassan El Btaouri,Pierre Jeannesson,Hamid Morjani +8 more
TL;DR: This research presents a novel probabilistic procedure called “spot-spot analysis” that allows for real-time analysis of the response of the immune system to natural catastrophes.
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Mechanical regulation of myofibroblast phenoconversion and collagen contraction.
TL;DR: This work focuses on mechanical and chemical regulation of collagen contraction by fibroblast and the involvement of these factors in their phenotypic conversion to myofibroblasts.
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New Promise and Opportunities for Allosteric Kinase Inhibitors
TL;DR: Recent developments in the rapidly advancing field of allosteric kinase inhibitors are reviewed including examples of proteolysis targeting chimeras (PROTACs), and unique binding modes for each type of inhibitors are highlighted to address future opportunities in this area.
References
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Comprehensive analysis of kinase inhibitor selectivity.
Mindy I. Davis,Jeremy P Hunt,Jeremy P Hunt,Sanna Herrgard,Pietro Ciceri,Pietro Ciceri,Lisa M Wodicka,Lisa M Wodicka,Gabriel Pallares,Gabriel Pallares,Michael D. Hocker,Daniel K Treiber,Daniel K Treiber,Patrick P Zarrinkar,Patrick P Zarrinkar +14 more
TL;DR: Analysis of the interaction patterns reveals a class of 'group-selective' inhibitors broadly active against a single subfamily of kinases, but selective outside that subfamily.
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Active and Inactive Protein Kinases: Structural Basis for Regulation
TL;DR: This review summarizes the current understand of the crystal structure Control mechanisms that have been recognized to determination of cAPK and showed the structural importance of Thr-197 or domains that may function in response to second phosphorylation and demonstrated possible roles of messengers.
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Quantitative chemical proteomics reveals mechanisms of action of clinical ABL kinase inhibitors
Marcus Bantscheff,Dirk Eberhard,Yann Abraham,Sonja Bastuck,Markus Boesche,Scott Hobson,Toby Mathieson,Jessica Perrin,Manfred Raida,Christina Rau,Valerie Reader,Gavain Sweetman,Andreas Bauer,Tewis Bouwmeester,Carsten Hopf,Ulrich Kruse,Gitte Neubauer,Nigel Ramsden,Jens Rick,Bernhard Kuster,Gerard Drewes +20 more
TL;DR: Quantitative profiling of the drugs Imatinib, dasatinib and bosutinib in K562 cells confirms known targets including ABL and SRC family kinases and identifies the receptor tyrosine kinase DDR1 and the oxidoreductase NQO2 as novel targets of imatinib.
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Rational design of inhibitors that bind to inactive kinase conformations
Yi Liu,Nathanael S. Gray +1 more
TL;DR: A structural analysis of binding modes of known human type II inhibitors are presented and it is demonstrated that they conform to a pharmacophore model that is currently being used to design a new generation of kinase inhibitors.
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The Discoidin Domain Receptor Tyrosine Kinases Are Activated by Collagen
TL;DR: The results suggest that the discoidin-related DDR tyrosine kinases are novel collagen receptors with the potential to control cellular responses to the extracellular matrix.