Literature DB >> 24900635

Discovery of Small Molecule RIP1 Kinase Inhibitors for the Treatment of Pathologies Associated with Necroptosis.

Philip A Harris1, Deepak Bandyopadhyay1, Scott B Berger1, Nino Campobasso1, Carol A Capriotti1, Julie A Cox1, Lauren Dare1, Joshua N Finger1, Sandra J Hoffman1, Kirsten M Kahler2, Ruth Lehr1, John D Lich1, Rakesh Nagilla1, Robert T Nolte2, Michael T Ouellette1, Christina S Pao1, Michelle C Schaeffer1, Angela Smallwood1, Helen H Sun1, Barbara A Swift1, Rachel D Totoritis1, Paris Ward1, Robert W Marquis1, John Bertin1, Peter J Gough1.   

Abstract

Potent inhibitors of RIP1 kinase from three distinct series, 1-aminoisoquinolines, pyrrolo[2,3-b]pyridines, and furo[2,3-d]pyrimidines, all of the type II class recognizing a DLG-out inactive conformation, were identified from screening of our in-house kinase focused sets. An exemplar from the furo[2,3-d]pyrimidine series showed a dose proportional response in protection from hypothermia in a mouse model of TNFα induced lethal shock.

Entities:  

Keywords:  RIP1; necroptosis; type II kinase inhibitors

Year:  2013        PMID： 24900635      PMCID： PMC4027519          DOI： 10.1021/ml400382p

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


  21 in total

1.  Comprehensive analysis of kinase inhibitor selectivity.

Authors:  Mindy I Davis; Jeremy P Hunt; Sanna Herrgard; Pietro Ciceri; Lisa M Wodicka; Gabriel Pallares; Michael Hocker; Daniel K Treiber; Patrick P Zarrinkar
Journal:  Nat Biotechnol       Date:  2011-10-30       Impact factor: 54.908

2.  The adaptor protein FADD protects epidermal keratinocytes from necroptosis in vivo and prevents skin inflammation.

Authors:  Marion C Bonnet; Daniela Preukschat; Patrick-Simon Welz; Geert van Loo; Maria A Ermolaeva; Wilhelm Bloch; Ingo Haase; Manolis Pasparakis
Journal:  Immunity       Date:  2011-10-13       Impact factor: 31.745

3.  Type-II kinase inhibitor docking, screening, and profiling using modified structures of active kinase states.

Authors:  Irina Kufareva; Ruben Abagyan
Journal:  J Med Chem       Date:  2008-12-25       Impact factor: 7.446

4.  Orally active 4-amino-5-diarylurea-furo[2,3-d]pyrimidine derivatives as anti-angiogenic agent inhibiting VEGFR2 and Tie-2.

Authors:  Yasushi Miyazaki; Jun Tang; Yutaka Maeda; Masato Nakano; Liping Wang; Robert T Nolte; Hideyuki Sato; Masaki Sugai; Yuji Okamoto; Anne T Truesdale; Daniel F Hassler; Eldridge N Nartey; Denis R Patrick; Maureen L Ho; Kazunori Ozawa
Journal:  Bioorg Med Chem Lett       Date:  2006-12-24       Impact factor: 2.823

5.  Synergistic protective effects of humanin and necrostatin-1 on hypoxia and ischemia/reperfusion injury.

Authors:  Xingshun Xu; Kao-Wei Chua; Chu C Chua; Chun-Feng Liu; Ronald C Hamdy; Balvin H L Chua
Journal:  Brain Res       Date:  2010-08-01       Impact factor: 3.252

6.  FADD prevents RIP3-mediated epithelial cell necrosis and chronic intestinal inflammation.

Authors:  Patrick-Simon Welz; Andy Wullaert; Katerina Vlantis; Vangelis Kondylis; Vanesa Fernández-Majada; Maria Ermolaeva; Petra Kirsch; Anja Sterner-Kock; Geert van Loo; Manolis Pasparakis
Journal:  Nature       Date:  2011-07-31       Impact factor: 49.962

7.  Necroptosis turns TNF lethal.

Authors:  Lorenzo Galluzzi; Guido Kroemer
Journal:  Immunity       Date:  2011-12-23       Impact factor: 31.745

8.  Rip1 (receptor-interacting protein kinase 1) mediates necroptosis and contributes to renal ischemia/reperfusion injury.

Authors:  Andreas Linkermann; Jan H Bräsen; Nina Himmerkus; Shuya Liu; Tobias B Huber; Ulrich Kunzendorf; Stefan Krautwald
Journal:  Kidney Int       Date:  2012-01-11       Impact factor: 10.612

9.  Necrostatin: a potentially novel cardioprotective agent?

Authors:  Christopher C T Smith; Sean M Davidson; Shiang Y Lim; James C Simpkin; John S Hothersall; Derek M Yellon
Journal:  Cardiovasc Drugs Ther       Date:  2007-07-31       Impact factor: 3.727

10.  Caspase-8 regulates TNF-α-induced epithelial necroptosis and terminal ileitis.

Authors:  Claudia Günther; Eva Martini; Nadine Wittkopf; Kerstin Amann; Benno Weigmann; Helmut Neumann; Maximilian J Waldner; Stephen M Hedrick; Stefan Tenzer; Markus F Neurath; Christoph Becker
Journal:  Nature       Date:  2011-09-14       Impact factor: 49.962
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  39 in total

1.  Ensemble pharmacophore meets ensemble docking: a novel screening strategy for the identification of RIPK1 inhibitors.

Authors:  S M Fayaz; G K Rajanikant
Journal:  J Comput Aided Mol Des       Date:  2014-07-01       Impact factor: 3.686

2.  When PERK inhibitors turn out to be new potent RIPK1 inhibitors: critical issues on the specificity and use of GSK2606414 and GSK2656157.

Authors:  Diego Rojas-Rivera; Tinneke Delvaeye; Ria Roelandt; Wim Nerinckx; Koen Augustyns; Peter Vandenabeele; Mathieu J M Bertrand
Journal:  Cell Death Differ       Date:  2017-04-28       Impact factor: 15.828

Review 3.  Necroptosis and RIPK1-mediated neuroinflammation in CNS diseases.

Authors:  Junying Yuan; Palak Amin; Dimitry Ofengeim
Journal:  Nat Rev Neurosci       Date:  2019-01       Impact factor: 34.870

Review 4.  Small molecule probes for cellular death machines.

Authors:  Ying Li; Lihui Qian; Junying Yuan
Journal:  Curr Opin Chem Biol       Date:  2017-06-16       Impact factor: 8.822

5.  RIPK3 Activates Parallel Pathways of MLKL-Driven Necroptosis and FADD-Mediated Apoptosis to Protect against Influenza A Virus.

Authors:  Shoko Nogusa; Roshan J Thapa; Christopher P Dillon; Swantje Liedmann; Thomas H Oguin; Justin P Ingram; Diego A Rodriguez; Rachelle Kosoff; Shalini Sharma; Oliver Sturm; Katherine Verbist; Peter J Gough; John Bertin; Boris M Hartmann; Stuart C Sealfon; William J Kaiser; Edward S Mocarski; Carolina B López; Paul G Thomas; Andrew Oberst; Douglas R Green; Siddharth Balachandran
Journal:  Cell Host Microbe       Date:  2016-06-16       Impact factor: 21.023

6.  Receptor-interacting Ser/Thr kinase 1 (RIPK1) and myosin IIA-dependent ceramidosomes form membrane pores that mediate blebbing and necroptosis.

Authors:  Rose Nganga; Natalia Oleinik; Jisun Kim; Shanmugam Panneer Selvam; Ryan De Palma; Kristen A Johnson; Rasesh Y Parikh; Vamsi Gangaraju; Yuri Peterson; Mohammed Dany; Robert V Stahelin; Christina Voelkel-Johnson; Zdzislaw M Szulc; Erhard Bieberich; Besim Ogretmen
Journal:  J Biol Chem       Date:  2018-11-12       Impact factor: 5.157

Review 7.  Complex Pathologic Roles of RIPK1 and RIPK3: Moving Beyond Necroptosis.

Authors:  Kelby W Wegner; Danish Saleh; Alexei Degterev
Journal:  Trends Pharmacol Sci       Date:  2017-01-23       Impact factor: 14.819

Review 8.  Programmed necrosis in the cross talk of cell death and inflammation.

Authors:  Francis Ka-Ming Chan; Nivea Farias Luz; Kenta Moriwaki
Journal:  Annu Rev Immunol       Date:  2014-12-10       Impact factor: 28.527

Review 9.  Regulated necrosis: disease relevance and therapeutic opportunities.

Authors:  Marcus Conrad; José Pedro Friedmann Angeli; Peter Vandenabeele; Brent R Stockwell
Journal:  Nat Rev Drug Discov       Date:  2016-01-18       Impact factor: 84.694

10.  Computational design of new protein kinase 2 inhibitors for the treatment of inflammatory diseases using QSAR, pharmacophore-structure-based virtual screening, and molecular dynamics.

Authors:  Josiane V Cruz; Rodolfo B Serafim; Gabriel M da Silva; Silvana Giuliatti; Joaquín M C Rosa; Moysés F Araújo Neto; Franco H A Leite; Carlton A Taft; Carlos H T P da Silva; Cleydson B R Santos
Journal:  J Mol Model       Date:  2018-08-07       Impact factor: 1.810
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