Literature DB >> 19445582

Prospect of JAK2 inhibitor therapy in myeloproliferative neoplasms.

Ehab Atallah1, Srdan Verstovsek.   

Abstract

The discovery of the Janus kinase (JAK)2 V617F mutation in patients with myeloproliferative neoplasms was a major milestone in understanding the biology of those disorders. Several groups simultaneously reported on the high incidence of this mutation in patients with myeloproliferative neoplasms: almost all patients with polycythemia vera harbor the mutation and about 50% of patients with essential thrombocythemia and primary myelofibrosis have the mutation, making the development of JAK2 tyrosine kinase inhibitors an attractive therapeutic goal. In addition, inhibition of JAK2 kinase may have a therapeutic role in other hematologic malignancies, such as chronic myeloid leukemia or lymphoma. A number of molecules that inhibit JAK2 kinase have been described in the literature, and several are being evaluated in a clinical setting. Here, we summarize current clinical experience with JAK2 inhibitors.

Entities:  

Mesh:

Substances:

Year:  2009        PMID: 19445582      PMCID: PMC5176249          DOI: 10.1586/era.09.14

Source DB:  PubMed          Journal:  Expert Rev Anticancer Ther        ISSN: 1473-7140            Impact factor:   4.512


  44 in total

1.  Comparison of effects of the tyrosine kinase inhibitors AG957, AG490, and STI571 on BCR-ABL--expressing cells, demonstrating synergy between AG490 and STI571.

Authors:  X Sun; J E Layton; A Elefanty; G J Lieschke
Journal:  Blood       Date:  2001-04-01       Impact factor: 22.113

2.  Photochemical preparation of a pyridone containing tetracycle: a Jak protein kinase inhibitor.

Authors:  James E Thompson; Rose M Cubbon; Richard T Cummings; Linda S Wicker; Robert Frankshun; Barry R Cunningham; Patricia M Cameron; Peter T Meinke; Nigel Liverton; Youmin Weng; Julie A DeMartino
Journal:  Bioorg Med Chem Lett       Date:  2002-04-22       Impact factor: 2.823

3.  JAK2 seems to be a typical cooperating mutation in therapy-related t(8;21)/ AML1-ETO-positive AML.

Authors:  S Schnittger; U Bacher; W Kern; C Haferlach; T Haferlach
Journal:  Leukemia       Date:  2006-11-09       Impact factor: 11.528

4.  Erlotinib effectively inhibits JAK2V617F activity and polycythemia vera cell growth.

Authors:  Zhe Li; Mingjiang Xu; Shu Xing; Wanting Tina Ho; Takefumi Ishii; Qingshan Li; Xueqi Fu; Zhizhuang Joe Zhao
Journal:  J Biol Chem       Date:  2006-12-18       Impact factor: 5.157

5.  The structural basis of Janus kinase 2 inhibition by a potent and specific pan-Janus kinase inhibitor.

Authors:  Isabelle S Lucet; Emmanuelle Fantino; Michelle Styles; Rebecca Bamert; Onisha Patel; Sophie E Broughton; Mark Walter; Christopher J Burns; Herbert Treutlein; Andrew F Wilks; Jamie Rossjohn
Journal:  Blood       Date:  2005-09-20       Impact factor: 22.113

6.  Activating mutation in the tyrosine kinase JAK2 in polycythemia vera, essential thrombocythemia, and myeloid metaplasia with myelofibrosis.

Authors:  Ross L Levine; Martha Wadleigh; Jan Cools; Benjamin L Ebert; Gerlinde Wernig; Brian J P Huntly; Titus J Boggon; Iwona Wlodarska; Jennifer J Clark; Sandra Moore; Jennifer Adelsperger; Sumin Koo; Jeffrey C Lee; Stacey Gabriel; Thomas Mercher; Alan D'Andrea; Stefan Fröhling; Konstanze Döhner; Peter Marynen; Peter Vandenberghe; Ruben A Mesa; Ayalew Tefferi; James D Griffin; Michael J Eck; William R Sellers; Matthew Meyerson; Todd R Golub; Stephanie J Lee; D Gary Gilliland
Journal:  Cancer Cell       Date:  2005-04       Impact factor: 31.743

7.  Multi-institutional randomized phase II trial of gefitinib for previously treated patients with advanced non-small-cell lung cancer (The IDEAL 1 Trial) [corrected].

Authors:  Masahiro Fukuoka; Seiji Yano; Giuseppe Giaccone; Tomohide Tamura; Kazuhiko Nakagawa; Jean-Yves Douillard; Yutaka Nishiwaki; Johan Vansteenkiste; Shinzoh Kudoh; Danny Rischin; Richard Eek; Takeshi Horai; Kazumasa Noda; Ichiro Takata; Egbert Smit; Steven Averbuch; Angela Macleod; Andrea Feyereislova; Rui-Ping Dong; José Baselga
Journal:  J Clin Oncol       Date:  2003-05-14       Impact factor: 44.544

8.  Emodin has a cytotoxic activity against human multiple myeloma as a Janus-activated kinase 2 inhibitor.

Authors:  Akihiro Muto; Mayumi Hori; Yosuke Sasaki; Akari Saitoh; Iho Yasuda; Tadahito Maekawa; Tomoe Uchida; Keiko Asakura; Tomonori Nakazato; Toshio Kaneda; Masahiro Kizaki; Yasuo Ikeda; Tadashi Yoshida
Journal:  Mol Cancer Ther       Date:  2007-03       Impact factor: 6.261

9.  Leukemic blasts in transformed JAK2-V617F-positive myeloproliferative disorders are frequently negative for the JAK2-V617F mutation.

Authors:  Alexandre Theocharides; Marjorie Boissinot; François Girodon; Richard Garand; Soon-Siong Teo; Eric Lippert; Pascaline Talmant; Andre Tichelli; Sylvie Hermouet; Radek C Skoda
Journal:  Blood       Date:  2007-03-15       Impact factor: 22.113

10.  Z3, a novel Jak2 tyrosine kinase small-molecule inhibitor that suppresses Jak2-mediated pathologic cell growth.

Authors:  Jacqueline Sayyah; Andrew Magis; David A Ostrov; Robert W Allan; Raul C Braylan; Peter P Sayeski
Journal:  Mol Cancer Ther       Date:  2008-08       Impact factor: 6.261

View more
  9 in total

1.  Benzoxathiol derivative BOT-4-one suppresses L540 lymphoma cell survival and proliferation via inhibition of JAK3/STAT3 signaling.

Authors:  Byung Hak Kim; Yun Sook Min; Jung Sook Choi; Gyeong Hun Baeg; Young Soo Kim; Jong Wook Shin; Tae Yoon Kim; Sang Kyu Ye
Journal:  Exp Mol Med       Date:  2011-05-31       Impact factor: 8.718

2.  Combination treatment in vitro with Nutlin, a small-molecule antagonist of MDM2, and pegylated interferon-α 2a specifically targets JAK2V617F-positive polycythemia vera cells.

Authors:  Min Lu; Xiaoli Wang; Yan Li; Joseph Tripodi; Goar Mosoyan; John Mascarenhas; Marina Kremyanskaya; Vesna Najfeld; Ronald Hoffman
Journal:  Blood       Date:  2012-08-07       Impact factor: 22.113

3.  Targeting transcription factor Stat5a/b as a therapeutic strategy for prostate cancer.

Authors:  Zhiyong Liao; Marja T Nevalainen
Journal:  Am J Transl Res       Date:  2010-11-21       Impact factor: 4.060

4.  Structure-based design of oxygen-linked macrocyclic kinase inhibitors: discovery of SB1518 and SB1578, potent inhibitors of Janus kinase 2 (JAK2) and Fms-like tyrosine kinase-3 (FLT3).

Authors:  Anders Poulsen; Anthony William; Stéphanie Blanchard; Angeline Lee; Harish Nagaraj; Haishan Wang; Eeling Teo; Evelyn Tan; Kee Chuan Goh; Brian Dymock
Journal:  J Comput Aided Mol Des       Date:  2012-04-22       Impact factor: 3.686

5.  Development and validation of a tetra-primer amplification refractory mutation system-polymerase chain reaction combined with melting analysis-assay for clinical JAK2 V617F mutation detection.

Authors:  Weiwei Liu; Tingting Hu; Yuming Chen; Xinju Zhang; Xiaoye Gu; Ming Guan
Journal:  Mol Diagn Ther       Date:  2014-10       Impact factor: 4.074

Review 6.  Beyond transcription factors: how oncogenic signalling reshapes the epigenetic landscape.

Authors:  Fan Liu; Lan Wang; Fabiana Perna; Stephen D Nimer
Journal:  Nat Rev Cancer       Date:  2016-06       Impact factor: 60.716

7.  Development and inter-laboratory validation of unlabeled probe melting curve analysis for detection of JAK2 V617F mutation in polycythemia vera.

Authors:  Zhiyuan Wu; Hong Yuan; Xinju Zhang; Weiwei Liu; Jinhua Xu; Wei Zhang; Ming Guan
Journal:  PLoS One       Date:  2011-10-20       Impact factor: 3.240

Review 8.  Second-Generation Jak2 Inhibitors for Advanced Prostate Cancer: Are We Ready for Clinical Development?

Authors:  Paul Beinhoff; Lavannya Sabharwal; Vindhya Udhane; Cristina Maranto; Peter S LaViolette; Kenneth M Jacobsohn; Susan Tsai; Kenneth A Iczkowski; Liang Wang; William A Hall; Scott M Dehm; Deepak Kilari; Marja T Nevalainen
Journal:  Cancers (Basel)       Date:  2021-10-17       Impact factor: 6.575

9.  Combined targeting of JAK2 and Bcl-2/Bcl-xL to cure mutant JAK2-driven malignancies and overcome acquired resistance to JAK2 inhibitors.

Authors:  Michaela Waibel; Vanessa S Solomon; Deborah A Knight; Rachael A Ralli; Sang-Kyu Kim; Kellie-Marie Banks; Eva Vidacs; Clemence Virely; Keith C S Sia; Lauryn S Bracken; Racquel Collins-Underwood; Christina Drenberg; Laura B Ramsey; Sara C Meyer; Megumi Takiguchi; Ross A Dickins; Ross Levine; Jacques Ghysdael; Mark A Dawson; Richard B Lock; Charles G Mullighan; Ricky W Johnstone
Journal:  Cell Rep       Date:  2013-11-21       Impact factor: 9.423

  9 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.