3krr › Citations

Potent and selective inhibition of polycythemia by the quinoxaline JAK2 inhibitor NVP-BSK805.

Baffert F, Régnier CH, De Pover A, Pissot-Soldermann C, Tavares GA, Blasco F, Brueggen J, Chène P, Drueckes P, Erdmann D, Furet P, Gerspacher M, Lang M, Ledieu D, Nolan L, Ruetz S, Trappe J, Vangrevelinghe E, Wartmann M, Wyder L, Hofmann F, Radimerski T
Mol Cancer Ther 9 1945-55 (2010)
Cited: 78 times
EuropePMC logo PMID: 20587663

Abstract

The recent discovery of an acquired activating point mutation in JAK2, substituting valine at amino acid position 617 for phenylalanine, has greatly improved our understanding of the molecular mechanism underlying chronic myeloproliferative neoplasms. Strikingly, the JAK2(V617F) mutation is found in nearly all patients suffering from polycythemia vera and in roughly every second patient suffering from essential thrombocythemia and primary myelofibrosis. Thus, JAK2 represents a promising target for the treatment of myeloproliferative neoplasms and considerable efforts are ongoing to discover and develop inhibitors of the kinase. Here, we report potent inhibition of JAK2(V617F) and JAK2 wild-type enzymes by a novel substituted quinoxaline, NVP-BSK805, which acts in an ATP-competitive manner. Within the JAK family, NVP-BSK805 displays more than 20-fold selectivity towards JAK2 in vitro, as well as excellent selectivity in broader kinase profiling. The compound blunts constitutive STAT5 phosphorylation in JAK2(V617F)-bearing cells, with concomitant suppression of cell proliferation and induction of apoptosis. In vivo, NVP-BSK805 exhibited good oral bioavailability and a long half-life. The inhibitor was efficacious in suppressing leukemic cell spreading and splenomegaly in a Ba/F3 JAK2(V617F) cell-driven mouse mechanistic model. Furthermore, NVP-BSK805 potently suppressed recombinant human erythropoietin-induced polycythemia and extramedullary erythropoiesis in mice and rats.

Reviews - 3krr mentioned but not cited (2)

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Articles - 3krr mentioned but not cited (18)

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Reviews citing this publication (12)

  1. Janus kinase inhibitors for the treatment of myeloproliferative neoplasias and beyond. Quintás-Cardama A, Kantarjian H, Cortes J, Verstovsek S. Nat Rev Drug Discov 10 127-140 (2011)
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  8. "Do We Know Jack" About JAK? A Closer Look at JAK/STAT Signaling Pathway. Bousoik E, Montazeri Aliabadi H. Front Oncol 8 287 (2018)
  9. Pharmacological Inhibition of Oncogenic STAT3 and STAT5 Signaling in Hematopoietic Cancers. Brachet-Botineau M, Polomski M, Neubauer HA, Juen L, Hédou D, Viaud-Massuard MC, Prié G, Gouilleux F. Cancers (Basel) 12 (2020)
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  11. Second-Generation Jak2 Inhibitors for Advanced Prostate Cancer: Are We Ready for Clinical Development? Beinhoff P, Sabharwal L, Udhane V, Maranto C, LaViolette PS, Jacobsohn KM, Tsai S, Iczkowski KA, Wang L, Hall WA, Dehm SM, Kilari D, Nevalainen MT. Cancers (Basel) 13 5204 (2021)
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Articles citing this publication (46)

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  8. Comprehensive review of JAK inhibitors in myeloproliferative neoplasms. Sonbol MB, Firwana B, Zarzour A, Morad M, Rana V, Tiu RV. Ther Adv Hematol 4 15-35 (2013)
  9. Co-targeting the PI3K/mTOR and JAK2 signalling pathways produces synergistic activity against myeloproliferative neoplasms. Bartalucci N, Tozzi L, Bogani C, Martinelli S, Rotunno G, Villeval JL, Vannucchi AM. J. Cell. Mol. Med. 17 1385-1396 (2013)
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  11. The oral HDAC inhibitor pracinostat (SB939) is efficacious and synergistic with the JAK2 inhibitor pacritinib (SB1518) in preclinical models of AML. Novotny-Diermayr V, Hart S, Goh KC, Cheong A, Ong LC, Hentze H, Pasha MK, Jayaraman R, Ethirajulu K, Wood JM. Blood Cancer J 2 e69 (2012)
  12. Differential effects of hydroxyurea and INC424 on mutant allele burden and myeloproliferative phenotype in a JAK2-V617F polycythemia vera mouse model. Kubovcakova L, Lundberg P, Grisouard J, Hao-Shen H, Romanet V, Andraos R, Murakami M, Dirnhofer S, Wagner KU, Radimerski T, Skoda RC. Blood 121 1188-1199 (2013)
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  14. Triple-negative breast cancers with amplification of JAK2 at the 9p24 locus demonstrate JAK2-specific dependence. Balko JM, Schwarz LJ, Luo N, Estrada MV, Giltnane JM, Dávila-González D, Wang K, Sánchez V, Dean PT, Combs SE, Hicks D, Pinto JA, Landis MD, Doimi FD, Yelensky R, Miller VA, Stephens PJ, Rimm DL, Gómez H, Chang JC, Sanders ME, Cook RS, Arteaga CL. Sci Transl Med 8 334ra53 (2016)
  15. Decreased NK-cell tumour immunosurveillance consequent to JAK inhibition enhances metastasis in breast cancer models. Bottos A, Gotthardt D, Gill JW, Gattelli A, Frei A, Tzankov A, Sexl V, Wodnar-Filipowicz A, Hynes NE. Nat Commun 7 12258 (2016)
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  23. Oncogenic role and therapeutic targeting of ABL-class and JAK-STAT activating kinase alterations in Ph-like ALL. Roberts KG, Yang YL, Payne-Turner D, Lin W, Files JK, Dickerson K, Gu Z, Taunton J, Janke LJ, Chen T, Loh ML, Hunger SP, Mullighan CG. Blood Adv 1 1657-1671 (2017)
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  25. Alternatively spliced, truncated GCSF receptor promotes leukemogenic properties and sensitivity to JAK inhibition. Mehta HM, Futami M, Glaubach T, Lee DW, Andolina JR, Yang Q, Whichard Z, Quinn M, Lu HF, Kao WM, Przychodzen B, Sarkar CA, Minella A, Maciejewski JP, Corey SJ. Leukemia 28 1041-1051 (2014)
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