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Items: 1 to 50 of 89

1.

Investigations into the Potential Role of Metabolites on the Anti-Leukemic Activity of Imatinib, Nilotinib and Midostaurin.

Manley PW.

Chimia (Aarau). 2019 Aug 21;73(7):561-570. doi: 10.2533/chimia.2019.561.

PMID:
31431216
2.

Tyrosine kinase inhibitors relax pulmonary arteries in human and murine precision-cut lung slices.

Rieg AD, Bünting NA, Cranen C, Suleiman S, Spillner JW, Schnöring H, Schröder T, von Stillfried S, Braunschweig T, Manley PW, Schälte G, Rossaint R, Uhlig S, Martin C.

Respir Res. 2019 Jun 6;20(1):111. doi: 10.1186/s12931-019-1074-2.

3.

Comparison of the Kinase Profile of Midostaurin (Rydapt) with That of Its Predominant Metabolites and the Potential Relevance of Some Newly Identified Targets to Leukemia Therapy.

Manley PW, Caravatti G, Furet P, Roesel J, Tran P, Wagner T, Wartmann M.

Biochemistry. 2018 Sep 25;57(38):5576-5590. doi: 10.1021/acs.biochem.8b00727. Epub 2018 Sep 13.

PMID:
30148617
4.

Discovery of Asciminib (ABL001), an Allosteric Inhibitor of the Tyrosine Kinase Activity of BCR-ABL1.

Schoepfer J, Jahnke W, Berellini G, Buonamici S, Cotesta S, Cowan-Jacob SW, Dodd S, Drueckes P, Fabbro D, Gabriel T, Groell JM, Grotzfeld RM, Hassan AQ, Henry C, Iyer V, Jones D, Lombardo F, Loo A, Manley PW, Pellé X, Rummel G, Salem B, Warmuth M, Wylie AA, Zoller T, Marzinzik AL, Furet P.

J Med Chem. 2018 Sep 27;61(18):8120-8135. doi: 10.1021/acs.jmedchem.8b01040. Epub 2018 Sep 7.

PMID:
30137981
5.

Midostaurin: its odyssey from discovery to approval for treating acute myeloid leukemia and advanced systemic mastocytosis.

Stone RM, Manley PW, Larson RA, Capdeville R.

Blood Adv. 2018 Feb 27;2(4):444-453. doi: 10.1182/bloodadvances.2017011080. Review. Erratum in: Blood Adv. 2018 Apr 10;2(7):787.

6.

Spotlight on midostaurin in the treatment of FLT3-mutated acute myeloid leukemia and systemic mastocytosis: design, development, and potential place in therapy.

Weisberg E, Sattler M, Manley PW, Griffin JD.

Onco Targets Ther. 2017 Dec 29;11:175-182. doi: 10.2147/OTT.S127679. eCollection 2018. Review.

7.

Inhibition of SDF-1-induced migration of oncogene-driven myeloid leukemia by the L-RNA aptamer (Spiegelmer), NOX-A12, and potentiation of tyrosine kinase inhibition.

Weisberg EL, Sattler M, Azab AK, Eulberg D, Kruschinski A, Manley PW, Stone R, Griffin JD.

Oncotarget. 2017 Nov 6;8(66):109973-109984. doi: 10.18632/oncotarget.22409. eCollection 2017 Dec 15.

8.

Midostaurin, a Natural Product-Derived Kinase Inhibitor Recently Approved for the Treatment of Hematological MalignanciesPublished as part of the Biochemistry series "Biochemistry to Bedside".

Manley PW, Weisberg E, Sattler M, Griffin JD.

Biochemistry. 2018 Feb 6;57(5):477-478. doi: 10.1021/acs.biochem.7b01126. Epub 2017 Nov 30. No abstract available.

9.

Midostaurin: a magic bullet that blocks mast cell expansion and activation.

Valent P, Akin C, Hartmann K, George TI, Sotlar K, Peter B, Gleixner KV, Blatt K, Sperr WR, Manley PW, Hermine O, Kluin-Nelemans HC, Arock M, Horny HP, Reiter A, Gotlib J.

Ann Oncol. 2017 Oct 1;28(10):2367-2376. doi: 10.1093/annonc/mdx290. Review.

PMID:
28945834
10.

Characterization of midostaurin as a dual inhibitor of FLT3 and SYK and potentiation of FLT3 inhibition against FLT3-ITD-driven leukemia harboring activated SYK kinase.

Weisberg EL, Puissant A, Stone R, Sattler M, Buhrlage SJ, Yang J, Manley PW, Meng C, Buonopane M, Daley JF, Lazo S, Wright R, Weinstock DM, Christie AL, Stegmaier K, Griffin JD.

Oncotarget. 2017 Jul 6;8(32):52026-52044. doi: 10.18632/oncotarget.19036. eCollection 2017 Aug 8.

11.

Erratum to: Imatinib relaxes the pulmonary venous bed of guinea pigs.

Maihöfer NA, Suleiman S, Dreymüller D, Manley PW, Rossaint R, Uhlig S, Martin C, Rieg AD.

Respir Res. 2017 Jun 19;18(1):121. doi: 10.1186/s12931-017-0612-z. No abstract available.

12.

Imatinib relaxes the pulmonary venous bed of guinea pigs.

Maihöfer NA, Suleiman S, Dreymüller D, Manley PW, Rossaint R, Uhlig S, Martin C, Rieg AD.

Respir Res. 2017 Feb 8;18(1):32. doi: 10.1186/s12931-017-0514-0. Erratum in: Respir Res. 2017 Jun 19;18(1):121.

13.

Deregulated hedgehog pathway signaling is inhibited by the smoothened antagonist LDE225 (Sonidegib) in chronic phase chronic myeloid leukaemia.

Irvine DA, Zhang B, Kinstrie R, Tarafdar A, Morrison H, Campbell VL, Moka HA, Ho Y, Nixon C, Manley PW, Wheadon H, Goodlad JR, Holyoake TL, Bhatia R, Copland M.

Sci Rep. 2016 May 9;6:25476. doi: 10.1038/srep25476.

14.

A Novel Potent Oral Series of VEGFR2 Inhibitors Abrogate Tumor Growth by Inhibiting Angiogenesis.

Bold G, Schnell C, Furet P, McSheehy P, Brüggen J, Mestan J, Manley PW, Drückes P, Burglin M, Dürler U, Loretan J, Reuter R, Wartmann M, Theuer A, Bauer-Probst B, Martiny-Baron G, Allegrini P, Goepfert A, Wood J, Littlewood-Evans A.

J Med Chem. 2016 Jan 14;59(1):132-46. doi: 10.1021/acs.jmedchem.5b01582. Epub 2015 Dec 21.

PMID:
26629594
15.

Target interaction profiling of midostaurin and its metabolites in neoplastic mast cells predicts distinct effects on activation and growth.

Peter B, Winter GE, Blatt K, Bennett KL, Stefanzl G, Rix U, Eisenwort G, Hadzijusufovic E, Gridling M, Dutreix C, Hoermann G, Schwaab J, Radia D, Roesel J, Manley PW, Reiter A, Superti-Furga G, Valent P.

Leukemia. 2016 Feb;30(2):464-72. doi: 10.1038/leu.2015.242. Epub 2015 Sep 9.

16.

Nilotinib is more potent than imatinib for treating plexiform neurofibroma in vitro and in vivo.

Wei J, Freytag M, Schober Y, Nockher WA, Mautner VF, Friedrich RE, Manley PW, Kluwe L, Kurtz A.

PLoS One. 2014 Oct 23;9(10):e107760. doi: 10.1371/journal.pone.0107760. eCollection 2014.

17.

Phosphoinositide 3-kinase inhibitors combined with imatinib in patient-derived xenograft models of gastrointestinal stromal tumors: rationale and efficacy.

Van Looy T, Wozniak A, Floris G, Sciot R, Li H, Wellens J, Vanleeuw U, Fletcher JA, Manley PW, Debiec-Rychter M, Schöffski P.

Clin Cancer Res. 2014 Dec 1;20(23):6071-82. doi: 10.1158/1078-0432.CCR-14-1823. Epub 2014 Oct 14.

18.

Imaging the intracellular distribution of tyrosine kinase inhibitors in living cells with quantitative hyperspectral stimulated Raman scattering.

Fu D, Zhou J, Zhu WS, Manley PW, Wang YK, Hood T, Wylie A, Xie XS.

Nat Chem. 2014 Jul;6(7):614-22. doi: 10.1038/nchem.1961. Epub 2014 May 25.

19.

Effects of Jak2 type 1 inhibitors NVP-BSK805 and NVP-BVB808 on Jak2 mutation-positive and Bcr-Abl-positive cell lines.

Ringel F, Kaeda J, Schwarz M, Oberender C, Grille P, Dörken B, Marque F, Manley PW, Radimerski T, le Coutre P.

Acta Haematol. 2014;132(1):75-86. doi: 10.1159/000356784. Epub 2014 Jan 31.

PMID:
24504330
20.

Efficacy and selectivity of nilotinib on NF1-associated tumors in vitro.

Jiang W, Schnabel C, Spyra M, Mautner VF, Friedrich RE, Hagel C, Manley PW, Kluwe L.

J Neurooncol. 2014 Jan;116(2):231-6. doi: 10.1007/s11060-013-1295-z. Epub 2013 Oct 31.

PMID:
24173684
21.

KIT signaling governs differential sensitivity of mature and primitive CML progenitors to tyrosine kinase inhibitors.

Corbin AS, O'Hare T, Gu Z, Kraft IL, Eiring AM, Khorashad JS, Pomicter AD, Zhang TY, Eide CA, Manley PW, Cortes JE, Druker BJ, Deininger MW.

Cancer Res. 2013 Sep 15;73(18):5775-86. doi: 10.1158/0008-5472.CAN-13-1318. Epub 2013 Jul 25.

22.

The kinetic deuterium isotope effect as applied to metabolic deactivation of imatinib to the des-methyl metabolite, CGP74588.

Manley PW, Blasco F, Mestan J, Aichholz R.

Bioorg Med Chem. 2013 Jun 1;21(11):3231-9. doi: 10.1016/j.bmc.2013.03.038. Epub 2013 Apr 1.

PMID:
23611771
23.

Modulation of activation-loop phosphorylation by JAK inhibitors is binding mode dependent.

Andraos R, Qian Z, Bonenfant D, Rubert J, Vangrevelinghe E, Scheufler C, Marque F, Régnier CH, De Pover A, Ryckelynck H, Bhagwat N, Koppikar P, Goel A, Wyder L, Tavares G, Baffert F, Pissot-Soldermann C, Manley PW, Gaul C, Voshol H, Levine RL, Sellers WR, Hofmann F, Radimerski T.

Cancer Discov. 2012 Jun;2(6):512-523. doi: 10.1158/2159-8290.CD-11-0324. Epub 2012 May 3.

24.

Inhibition of CXCR4 in CML cells disrupts their interaction with the bone marrow microenvironment and sensitizes them to nilotinib.

Weisberg E, Azab AK, Manley PW, Kung AL, Christie AL, Bronson R, Ghobrial IM, Griffin JD.

Leukemia. 2012 May;26(5):985-90. doi: 10.1038/leu.2011.360. Epub 2011 Dec 20.

25.

Structural resemblances and comparisons of the relative pharmacological properties of imatinib and nilotinib.

Manley PW, Stiefl N, Cowan-Jacob SW, Kaufman S, Mestan J, Wartmann M, Wiesmann M, Woodman R, Gallagher N.

Bioorg Med Chem. 2010 Oct 1;18(19):6977-86. doi: 10.1016/j.bmc.2010.08.026. Epub 2010 Aug 14.

PMID:
20817538
26.

A type-II kinase inhibitor capable of inhibiting the T315I "gatekeeper" mutant of Bcr-Abl.

Choi HG, Ren P, Adrian F, Sun F, Lee HS, Wang X, Ding Q, Zhang G, Xie Y, Zhang J, Liu Y, Tuntland T, Warmuth M, Manley PW, Mestan J, Gray NS, Sim T.

J Med Chem. 2010 Aug 12;53(15):5439-48. doi: 10.1021/jm901808w.

27.

Preclinical evaluation of nilotinib efficacy in an imatinib-resistant KIT-driven tumor model.

Cullinane C, Natoli A, Hui Y, Conus N, Jackson S, Brüggen J, Manley PW, McArthur GA.

Mol Cancer Ther. 2010 May;9(5):1461-8. doi: 10.1158/1535-7163.MCT-09-1181. Epub 2010 May 4.

28.

Functional activity of the OCT-1 protein is predictive of long-term outcome in patients with chronic-phase chronic myeloid leukemia treated with imatinib.

White DL, Dang P, Engler J, Frede A, Zrim S, Osborn M, Saunders VA, Manley PW, Hughes TP.

J Clin Oncol. 2010 Jun 1;28(16):2761-7. doi: 10.1200/JCO.2009.26.5819. Epub 2010 Apr 26.

PMID:
20421539
29.

Discovery of a small-molecule type II inhibitor of wild-type and gatekeeper mutants of BCR-ABL, PDGFRalpha, Kit, and Src kinases: novel type II inhibitor of gatekeeper mutants.

Weisberg E, Choi HG, Ray A, Barrett R, Zhang J, Sim T, Zhou W, Seeliger M, Cameron M, Azam M, Fletcher JA, Debiec-Rychter M, Mayeda M, Moreno D, Kung AL, Janne PA, Khosravi-Far R, Melo JV, Manley PW, Adamia S, Wu C, Gray N, Griffin JD.

Blood. 2010 May 27;115(21):4206-16. doi: 10.1182/blood-2009-11-251751. Epub 2010 Mar 18.

30.

Comparative In vitro cellular data alone are insufficient to predict clinical responses and guide the choice of BCR-ABL inhibitor for treating imatinib-resistant chronic myeloid leukemia.

Laneuville P, Dilea C, Yin OQ, Woodman RC, Mestan J, Manley PW.

J Clin Oncol. 2010 Apr 10;28(11):e169-71; author reply e172. doi: 10.1200/JCO.2009.26.4945. Epub 2010 Mar 1. No abstract available.

PMID:
20194843
31.

Inhibitors of the Abl kinase directed at either the ATP- or myristate-binding site.

Fabbro D, Manley PW, Jahnke W, Liebetanz J, Szyttenholm A, Fendrich G, Strauss A, Zhang J, Gray NS, Adrian F, Warmuth M, Pelle X, Grotzfeld R, Berst F, Marzinzik A, Cowan-Jacob SW, Furet P, Mestan J.

Biochim Biophys Acta. 2010 Mar;1804(3):454-62. doi: 10.1016/j.bbapap.2009.12.009.

PMID:
20152788
32.

Targeting Bcr-Abl by combining allosteric with ATP-binding-site inhibitors.

Zhang J, Adrián FJ, Jahnke W, Cowan-Jacob SW, Li AG, Iacob RE, Sim T, Powers J, Dierks C, Sun F, Guo GR, Ding Q, Okram B, Choi Y, Wojciechowski A, Deng X, Liu G, Fendrich G, Strauss A, Vajpai N, Grzesiek S, Tuntland T, Liu Y, Bursulaya B, Azam M, Manley PW, Engen JR, Daley GQ, Warmuth M, Gray NS.

Nature. 2010 Jan 28;463(7280):501-6. doi: 10.1038/nature08675. Epub 2010 Jan 13.

33.

Extended kinase profile and properties of the protein kinase inhibitor nilotinib.

Manley PW, Drueckes P, Fendrich G, Furet P, Liebetanz J, Martiny-Baron G, Mestan J, Trappe J, Wartmann M, Fabbro D.

Biochim Biophys Acta. 2010 Mar;1804(3):445-53. doi: 10.1016/j.bbapap.2009.11.008. Epub 2009 Nov 14.

PMID:
19922818
34.

Backbone NMR resonance assignment of the Abelson kinase domain in complex with imatinib.

Vajpai N, Strauss A, Fendrich G, Cowan-Jacob SW, Manley PW, Jahnke W, Grzesiek S.

Biomol NMR Assign. 2008 Jun;2(1):41-2. doi: 10.1007/s12104-008-9079-7. Epub 2008 Mar 5.

PMID:
19636920
35.

The interplay of structural information and functional studies in kinase drug design: insights from BCR-Abl.

Eck MJ, Manley PW.

Curr Opin Cell Biol. 2009 Apr;21(2):288-95. doi: 10.1016/j.ceb.2009.01.014. Epub 2009 Feb 11. Review.

PMID:
19217274
36.

Evidence that resistance to nilotinib may be due to BCR-ABL, Pgp, or Src kinase overexpression.

Mahon FX, Hayette S, Lagarde V, Belloc F, Turcq B, Nicolini F, Belanger C, Manley PW, Leroy C, Etienne G, Roche S, Pasquet JM.

Cancer Res. 2008 Dec 1;68(23):9809-16. doi: 10.1158/0008-5472.CAN-08-1008.

37.

Inhibition of collagen-induced discoidin domain receptor 1 and 2 activation by imatinib, nilotinib and dasatinib.

Day E, Waters B, Spiegel K, Alnadaf T, Manley PW, Buchdunger E, Walker C, Jarai G.

Eur J Pharmacol. 2008 Dec 3;599(1-3):44-53. doi: 10.1016/j.ejphar.2008.10.014. Epub 2008 Oct 11.

PMID:
18938156
38.

Coupling of mutated Met variants to DNA repair via Abl and Rad51.

Ganapathipillai SS, Medová M, Aebersold DM, Manley PW, Berthou S, Streit B, Blank-Liss W, Greiner RH, Rothen-Rutishauser B, Zimmer Y.

Cancer Res. 2008 Jul 15;68(14):5769-77. doi: 10.1158/0008-5472.CAN-08-1269.

39.

Solution conformations and dynamics of ABL kinase-inhibitor complexes determined by NMR substantiate the different binding modes of imatinib/nilotinib and dasatinib.

Vajpai N, Strauss A, Fendrich G, Cowan-Jacob SW, Manley PW, Grzesiek S, Jahnke W.

J Biol Chem. 2008 Jun 27;283(26):18292-302. doi: 10.1074/jbc.M801337200. Epub 2008 Apr 22.

40.

Synergistic growth-inhibitory effects of two tyrosine kinase inhibitors, dasatinib and PKC412, on neoplastic mast cells expressing the D816V-mutated oncogenic variant of KIT.

Gleixner KV, Mayerhofer M, Sonneck K, Gruze A, Samorapoompichit P, Baumgartner C, Lee FY, Aichberger KJ, Manley PW, Fabbro D, Pickl WF, Sillaber C, Valent P.

Haematologica. 2007 Nov;92(11):1451-9.

41.

Inhibition of the human P2X7 receptor by a novel protein tyrosine kinase antagonist.

Shemon AN, Sluyter R, Stokes L, Manley PW, Wiley JS.

Biochem Biophys Res Commun. 2008 Jan 18;365(3):515-20. Epub 2007 Nov 20.

PMID:
17999916
42.

Comparison of nilotinib and imatinib inhibition of FMS receptor signaling, macrophage production and osteoclastogenesis.

Brownlow N, Russell AE, Saravanapavan H, Wiesmann M, Murray JM, Manley PW, Dibb NJ.

Leukemia. 2008 Mar;22(3):649-52. Epub 2007 Sep 13. No abstract available.

PMID:
17851554
43.

Most CML patients who have a suboptimal response to imatinib have low OCT-1 activity: higher doses of imatinib may overcome the negative impact of low OCT-1 activity.

White DL, Saunders VA, Dang P, Engler J, Venables A, Zrim S, Zannettino A, Lynch K, Manley PW, Hughes T.

Blood. 2007 Dec 1;110(12):4064-72. Epub 2007 Aug 30.

44.

Second generation inhibitors of BCR-ABL for the treatment of imatinib-resistant chronic myeloid leukaemia.

Weisberg E, Manley PW, Cowan-Jacob SW, Hochhaus A, Griffin JD.

Nat Rev Cancer. 2007 May;7(5):345-56. Review.

PMID:
17457302
45.

Imatinib increases the intracellular concentration of nilotinib, which may explain the observed synergy between these drugs.

White DL, Saunders VA, Quinn SR, Manley PW, Hughes TP.

Blood. 2007 Apr 15;109(8):3609-10. No abstract available.

46.

Identification of BCR-ABL point mutations conferring resistance to the Abl kinase inhibitor AMN107 (nilotinib) by a random mutagenesis study.

Ray A, Cowan-Jacob SW, Manley PW, Mestan J, Griffin JD.

Blood. 2007 Jun 1;109(11):5011-5. Epub 2007 Feb 15.

47.

Structural biology contributions to the discovery of drugs to treat chronic myelogenous leukaemia.

Cowan-Jacob SW, Fendrich G, Floersheimer A, Furet P, Liebetanz J, Rummel G, Rheinberger P, Centeleghe M, Fabbro D, Manley PW.

Acta Crystallogr D Biol Crystallogr. 2007 Jan;63(Pt 1):80-93. Epub 2006 Dec 13.

48.

Adaptive secretion of granulocyte-macrophage colony-stimulating factor (GM-CSF) mediates imatinib and nilotinib resistance in BCR/ABL+ progenitors via JAK-2/STAT-5 pathway activation.

Wang Y, Cai D, Brendel C, Barett C, Erben P, Manley PW, Hochhaus A, Neubauer A, Burchert A.

Blood. 2007 Mar 1;109(5):2147-55. Epub 2006 Nov 7.

49.

Effects of PKC412, nilotinib, and imatinib against GIST-associated PDGFRA mutants with differential imatinib sensitivity.

Weisberg E, Wright RD, Jiang J, Ray A, Moreno D, Manley PW, Fabbro D, Hall-Meyers E, Catley L, Podar K, Kung AL, Griffin JD.

Gastroenterology. 2006 Dec;131(6):1734-42. Epub 2006 Sep 20.

50.

Beneficial effects of combining nilotinib and imatinib in preclinical models of BCR-ABL+ leukemias.

Weisberg E, Catley L, Wright RD, Moreno D, Banerji L, Ray A, Manley PW, Mestan J, Fabbro D, Jiang J, Hall-Meyers E, Callahan L, DellaGatta JL, Kung AL, Griffin JD.

Blood. 2007 Mar 1;109(5):2112-20. Epub 2006 Oct 26.

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