Literature DB >> 23823659

Specificity and mechanism-of-action of the JAK2 tyrosine kinase inhibitors ruxolitinib and SAR302503 (TG101348).

T Zhou1, S Georgeon2, R Moser3, D J Moore3, A Caflisch1, O Hantschel2.   

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Year:  2013        PMID： 23823659     DOI： 10.1038/leu.2013.205

Source DB:  PubMed          Journal:  Leukemia        ISSN： 0887-6924            Impact factor:   11.528


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  17 in total

1.  Optimization of inhibitors of the tyrosine kinase EphB4. 2. Cellular potency improvement and binding mode validation by X-ray crystallography.

Authors:  Karine Lafleur; Jing Dong; Danzhi Huang; Amedeo Caflisch; Cristina Nevado
Journal:  J Med Chem       Date:  2012-12-19       Impact factor: 7.446

2.  JAK inhibition with ruxolitinib versus best available therapy for myelofibrosis.

Authors:  Claire Harrison; Jean-Jacques Kiladjian; Haifa Kathrin Al-Ali; Heinz Gisslinger; Roger Waltzman; Viktoriya Stalbovskaya; Mari McQuitty; Deborah S Hunter; Richard Levy; Laurent Knoops; Francisco Cervantes; Alessandro M Vannucchi; Tiziano Barbui; Giovanni Barosi
Journal:  N Engl J Med       Date:  2012-03-01       Impact factor: 91.245

3.  LIGPLOT: a program to generate schematic diagrams of protein-ligand interactions.

Authors:  A C Wallace; R A Laskowski; J M Thornton
Journal:  Protein Eng       Date:  1995-02

4.  Rational design of inhibitors that bind to inactive kinase conformations.

Authors:  Yi Liu; Nathanael S Gray
Journal:  Nat Chem Biol       Date:  2006-07       Impact factor: 15.040

5.  Preclinical characterization of the selective JAK1/2 inhibitor INCB018424: therapeutic implications for the treatment of myeloproliferative neoplasms.

Authors:  Alfonso Quintás-Cardama; Kris Vaddi; Phillip Liu; Taghi Manshouri; Jun Li; Peggy A Scherle; Eian Caulder; Xiaoming Wen; Yanlong Li; Paul Waeltz; Mark Rupar; Timothy Burn; Yvonne Lo; Jennifer Kelley; Maryanne Covington; Stacey Shepard; James D Rodgers; Patrick Haley; Hagop Kantarjian; Jordan S Fridman; Srdan Verstovsek
Journal:  Blood       Date:  2010-02-03       Impact factor: 22.113

6.  Efficacy of TG101348, a selective JAK2 inhibitor, in treatment of a murine model of JAK2V617F-induced polycythemia vera.

Authors:  Gerlinde Wernig; Michael G Kharas; Rachel Okabe; Sandra A Moore; Dena S Leeman; Dana E Cullen; Maricel Gozo; Elizabeth P McDowell; Ross L Levine; John Doukas; Chi Ching Mak; Glenn Noronha; Michael Martin; Yon D Ko; Benjamin H Lee; Richard M Soll; Ayalew Tefferi; John D Hood; D Gary Gilliland
Journal:  Cancer Cell       Date:  2008-04       Impact factor: 31.743

7.  Safety and efficacy of TG101348, a selective JAK2 inhibitor, in myelofibrosis.

Authors:  Animesh Pardanani; Jason R Gotlib; Catriona Jamieson; Jorge E Cortes; Moshe Talpaz; Richard M Stone; Michael H Silverman; D Gary Gilliland; Jolene Shorr; Ayalew Tefferi
Journal:  J Clin Oncol       Date:  2011-01-10       Impact factor: 44.544

Review 8.  JAK inhibitor therapy for myelofibrosis: critical assessment of value and limitations.

Authors:  A Pardanani; A M Vannucchi; F Passamonti; F Cervantes; T Barbui; A Tefferi
Journal:  Leukemia       Date:  2010-11-16       Impact factor: 11.528

Review 9.  Is inhibition of kinase activity the only therapeutic strategy for LRRK2-associated Parkinson's disease?

Authors:  Iakov N Rudenko; Ruth Chia; Mark R Cookson
Journal:  BMC Med       Date:  2012-02-23       Impact factor: 8.775

10.  The Btk tyrosine kinase is a major target of the Bcr-Abl inhibitor dasatinib.

Authors:  Oliver Hantschel; Uwe Rix; Uwe Schmidt; Tilmann Bürckstümmer; Michael Kneidinger; Gregor Schütze; Jacques Colinge; Keiryn L Bennett; Wilfried Ellmeier; Peter Valent; Giulio Superti-Furga
Journal:  Proc Natl Acad Sci U S A       Date:  2007-08-07       Impact factor: 11.205
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  38 in total

1.  The JAK inhibitor ruxolitinib impairs dendritic cell migration via off-target inhibition of ROCK.

Authors:  J Rudolph; A Heine; T Quast; W Kolanus; J Trebicka; P Brossart; D Wolf
Journal:  Leukemia       Date:  2016-05-25       Impact factor: 11.528

2.  microRNA-23a, -27a and -24 synergistically regulate JAK1/Stat3 cascade and serve as novel therapeutic targets in human acute erythroid leukemia.

Authors:  R Su; L Dong; D Zou; H Zhao; Y Ren; F Li; P Yi; L Li; Y Zhu; Y Ma; J Wang; F Wang; J Yu
Journal:  Oncogene       Date:  2016-04-18       Impact factor: 9.867

3.  Pacritinib versus best available therapy for the treatment of myelofibrosis irrespective of baseline cytopenias (PERSIST-1): an international, randomised, phase 3 trial.

Authors:  Ruben A Mesa; Alessandro M Vannucchi; Adam Mead; Miklos Egyed; Anita Szoke; Aleksandr Suvorov; Janos Jakucs; Andrew Perkins; Ritam Prasad; Jiri Mayer; Judit Demeter; Peter Ganly; Jack W Singer; Huafeng Zhou; James P Dean; Peter A Te Boekhorst; Jyoti Nangalia; Jean-Jacques Kiladjian; Claire N Harrison
Journal:  Lancet Haematol       Date:  2017-03-20       Impact factor: 18.959

4.  Beyond JAK-STAT: novel therapeutic targets in Ph-negative MPN.

Authors:  Aaron T Gerds
Journal:  Hematology Am Soc Hematol Educ Program       Date:  2019-12-06

5.  Activation of the STING-Dependent Type I Interferon Response Reduces Microglial Reactivity and Neuroinflammation.

Authors:  Vidhu Mathur; Ritwik Burai; Ryan T Vest; Liana N Bonanno; Benoit Lehallier; Macy E Zardeneta; Karishma N Mistry; Danny Do; Samuel E Marsh; Edsel M Abud; Mathew Blurton-Jones; Lingyin Li; Hilal A Lashuel; Tony Wyss-Coray
Journal:  Neuron       Date:  2017-12-20       Impact factor: 17.173

6.  The Calreticulin control of human stress erythropoiesis is impaired by JAK2V617F in polycythemia vera.

Authors:  Mario Falchi; Lilian Varricchio; Fabrizio Martelli; Manuela Marra; Orietta Picconi; Agostino Tafuri; Gabriella Girelli; Vladimir N Uversky; Anna Rita Migliaccio
Journal:  Exp Hematol       Date:  2017-02-21       Impact factor: 3.084

7.  Synthetic Lethal Screen Demonstrates That a JAK2 Inhibitor Suppresses a BCL6-dependent IL10RA/JAK2/STAT3 Pathway in High Grade B-cell Lymphoma.

Authors:  Daniel Beck; Jenny Zobel; Ruth Barber; Sian Evans; Larissa Lezina; Rebecca L Allchin; Matthew Blades; Richard Elliott; Christopher J Lord; Alan Ashworth; Andrew C G Porter; Simon D Wagner
Journal:  J Biol Chem       Date:  2016-06-06       Impact factor: 5.157

8.  Colony-Stimulating Factor-1 Receptor Is Required for Nurse-like Cell Survival in Chronic Lymphocytic Leukemia.

Authors:  Avery Polk; Ye Lu; Tianjiao Wang; Erlene Seymour; Nathanael G Bailey; Jack W Singer; Philip S Boonstra; Megan S Lim; Sami Malek; Ryan A Wilcox
Journal:  Clin Cancer Res       Date:  2016-06-22       Impact factor: 12.531

9.  Preclinical characterization of signal transducer and activator of transcription 3 small molecule inhibitors for primary and metastatic brain cancer therapy.

Authors:  Hikmat H Assi; Chris Paran; Nathan VanderVeen; Jonathan Savakus; Robert Doherty; Emanuele Petruzzella; James D Hoeschele; Henry Appelman; Leda Raptis; Tom Mikkelsen; Pedro R Lowenstein; Maria G Castro
Journal:  J Pharmacol Exp Ther       Date:  2014-04-02       Impact factor: 4.030

Review 10.  Fedratinib: First Approval.

Authors:  Hannah A Blair
Journal:  Drugs       Date:  2019-10       Impact factor: 9.546
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