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Items: 1 to 50 of 90

1.

Correction: AMN107 (nilotinib): a novel and selective inhibitor of BCR-ABL.

Weisberg E, Manley P, Mestan J, Cowan-Jacob S, Ray A, Griffin JD.

Br J Cancer. 2019 Jul;121(3):282. doi: 10.1038/s41416-019-0505-7.

2.

5-(4,6-Dimorpholino-1,3,5-triazin-2-yl)-4-(trifluoromethyl)pyridin-2-amine (PQR309), a Potent, Brain-Penetrant, Orally Bioavailable, Pan-Class I PI3K/mTOR Inhibitor as Clinical Candidate in Oncology.

Beaufils F, Cmiljanovic N, Cmiljanovic V, Bohnacker T, Melone A, Marone R, Jackson E, Zhang X, Sele A, Borsari C, Mestan J, Hebeisen P, Hillmann P, Giese B, Zvelebil M, Fabbro D, Williams RL, Rageot D, Wymann MP.

J Med Chem. 2017 Sep 14;60(17):7524-7538. doi: 10.1021/acs.jmedchem.7b00930. Epub 2017 Sep 1.

3.

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
4.

Phosphorylation of Tyr245 in the open-inhibited state of Abelson kinase does not induce downstream signaling.

Skora L, Kempf D, Mestan J, D'Orazio D, Jahnke W.

Eur J Haematol. 2016 May;96(5):502-6. doi: 10.1111/ejh.12627. Epub 2015 Jul 22.

PMID:
26154982
5.

NMR reveals the allosteric opening and closing of Abelson tyrosine kinase by ATP-site and myristoyl pocket inhibitors.

Skora L, Mestan J, Fabbro D, Jahnke W, Grzesiek S.

Proc Natl Acad Sci U S A. 2013 Nov 19;110(47):E4437-45. doi: 10.1073/pnas.1314712110. Epub 2013 Nov 4.

6.

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
7.

IL-8-mediated angiogenic responses of endothelial cells to lipid antigen activation of iNKT cells depend on EGFR transactivation.

Kyriakakis E, Cavallari M, Pfaff D, Fabbro D, Mestan J, Philippova M, De Libero G, Erne P, Resink TJ.

J Leukoc Biol. 2011 Nov;90(5):929-39. doi: 10.1189/jlb.0211097. Epub 2011 Aug 1.

PMID:
21807744
8.

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
9.

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.

10.

Binding or bending: distinction of allosteric Abl kinase agonists from antagonists by an NMR-based conformational assay.

Jahnke W, Grotzfeld RM, Pellé X, Strauss A, Fendrich G, Cowan-Jacob SW, Cotesta S, Fabbro D, Furet P, Mestan J, Marzinzik AL.

J Am Chem Soc. 2010 May 26;132(20):7043-8. doi: 10.1021/ja101837n.

PMID:
20450175
11.

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
12.

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
13.

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
14.

Tracing pathway activities with kinase inhibitors and reverse phase protein arrays.

van Oostrum J, Calonder C, Rechsteiner D, Ehrat M, Mestan J, Fabbro D, Voshol H.

Proteomics Clin Appl. 2009 Apr;3(4):412-22. doi: 10.1002/prca.200800070. Epub 2008 Dec 9.

PMID:
21136968
15.

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.

PMID:
17303698
16.

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.

17.

AMN107 (nilotinib): a novel and selective inhibitor of BCR-ABL.

Weisberg E, Manley P, Mestan J, Cowan-Jacob S, Ray A, Griffin JD.

Br J Cancer. 2006 Jun 19;94(12):1765-9. Epub 2006 May 23. Review. Erratum in: Br J Cancer. 2019 Jul;121(3):282.

18.

Bcr-Abl resistance screening predicts a limited spectrum of point mutations to be associated with clinical resistance to the Abl kinase inhibitor nilotinib (AMN107).

von Bubnoff N, Manley PW, Mestan J, Sanger J, Peschel C, Duyster J.

Blood. 2006 Aug 15;108(4):1328-33. Epub 2006 Apr 13.

PMID:
16614241
19.

Allosteric inhibitors of Bcr-abl-dependent cell proliferation.

Adrián FJ, Ding Q, Sim T, Velentza A, Sloan C, Liu Y, Zhang G, Hur W, Ding S, Manley P, Mestan J, Fabbro D, Gray NS.

Nat Chem Biol. 2006 Feb;2(2):95-102. Epub 2006 Jan 15.

PMID:
16415863
20.

Advances in the structural biology, design and clinical development of Bcr-Abl kinase inhibitors for the treatment of chronic myeloid leukaemia.

Manley PW, Cowan-Jacob SW, Mestan J.

Biochim Biophys Acta. 2005 Dec 30;1754(1-2):3-13. Epub 2005 Sep 8. Review.

PMID:
16172030
21.

AMN107, a novel aminopyrimidine inhibitor of Bcr-Abl, has in vitro activity against imatinib-resistant chronic myeloid leukemia.

Golemovic M, Verstovsek S, Giles F, Cortes J, Manshouri T, Manley PW, Mestan J, Dugan M, Alland L, Griffin JD, Arlinghaus RB, Sun T, Kantarjian H, Beran M.

Clin Cancer Res. 2005 Jul 1;11(13):4941-7.

22.

In vitro activity of Bcr-Abl inhibitors AMN107 and BMS-354825 against clinically relevant imatinib-resistant Abl kinase domain mutants.

O'Hare T, Walters DK, Stoffregen EP, Jia T, Manley PW, Mestan J, Cowan-Jacob SW, Lee FY, Heinrich MC, Deininger MW, Druker BJ.

Cancer Res. 2005 Jun 1;65(11):4500-5.

23.

Characterization of AMN107, a selective inhibitor of native and mutant Bcr-Abl.

Weisberg E, Manley PW, Breitenstein W, Brüggen J, Cowan-Jacob SW, Ray A, Huntly B, Fabbro D, Fendrich G, Hall-Meyers E, Kung AL, Mestan J, Daley GQ, Callahan L, Catley L, Cavazza C, Azam M, Neuberg D, Wright RD, Gilliland DG, Griffin JD.

Cancer Cell. 2005 Feb;7(2):129-41. Erratum in: Cancer Cell. 2005 Apr;7(4):399. Mohammed, Azam [corrected to Azam, Mohammad].

24.

The human ubiquitin-conjugating enzyme Cdc34 controls cellular proliferation through regulation of p27Kip1 protein levels.

Butz N, Ruetz S, Natt F, Hall J, Weiler J, Mestan J, Ducarre M, Grossenbacher R, Hauser P, Kempf D, Hofmann F.

Exp Cell Res. 2005 Feb 15;303(2):482-93.

PMID:
15652359
25.

Urea derivatives of STI571 as inhibitors of Bcr-Abl and PDGFR kinases.

Manley PW, Breitenstein W, Brüggen J, Cowan-Jacob SW, Furet P, Mestan J, Meyer T.

Bioorg Med Chem Lett. 2004 Dec 6;14(23):5793-7.

PMID:
15501042
26.

AEE788: a dual family epidermal growth factor receptor/ErbB2 and vascular endothelial growth factor receptor tyrosine kinase inhibitor with antitumor and antiangiogenic activity.

Traxler P, Allegrini PR, Brandt R, Brueggen J, Cozens R, Fabbro D, Grosios K, Lane HA, McSheehy P, Mestan J, Meyer T, Tang C, Wartmann M, Wood J, Caravatti G.

Cancer Res. 2004 Jul 15;64(14):4931-41.

27.

Overexpression, genomic amplification and therapeutic potential of inhibiting the UbcH10 ubiquitin conjugase in human carcinomas of diverse anatomic origin.

Wagner KW, Sapinoso LM, El-Rifai W, Frierson HF, Butz N, Mestan J, Hofmann F, Deveraux QL, Hampton GM.

Oncogene. 2004 Aug 26;23(39):6621-9.

PMID:
15208666
28.

S6K1(-/-)/S6K2(-/-) mice exhibit perinatal lethality and rapamycin-sensitive 5'-terminal oligopyrimidine mRNA translation and reveal a mitogen-activated protein kinase-dependent S6 kinase pathway.

Pende M, Um SH, Mieulet V, Sticker M, Goss VL, Mestan J, Mueller M, Fumagalli S, Kozma SC, Thomas G.

Mol Cell Biol. 2004 Apr;24(8):3112-24.

29.

In vivo antitumor activity of NVP-AEW541-A novel, potent, and selective inhibitor of the IGF-IR kinase.

García-Echeverría C, Pearson MA, Marti A, Meyer T, Mestan J, Zimmermann J, Gao J, Brueggen J, Capraro HG, Cozens R, Evans DB, Fabbro D, Furet P, Porta DG, Liebetanz J, Martiny-Baron G, Ruetz S, Hofmann F.

Cancer Cell. 2004 Mar;5(3):231-9.

30.

Imatinib (STI571) resistance in chronic myelogenous leukemia: molecular basis of the underlying mechanisms and potential strategies for treatment.

Cowan-Jacob SW, Guez V, Fendrich G, Griffin JD, Fabbro D, Furet P, Liebetanz J, Mestan J, Manley PW.

Mini Rev Med Chem. 2004 Mar;4(3):285-99. Review.

PMID:
15032675
31.

Advances in the structural biology, design and clinical development of VEGF-R kinase inhibitors for the treatment of angiogenesis.

Manley PW, Bold G, Brüggen J, Fendrich G, Furet P, Mestan J, Schnell C, Stolz B, Meyer T, Meyhack B, Stark W, Strauss A, Wood J.

Biochim Biophys Acta. 2004 Mar 11;1697(1-2):17-27. Review.

PMID:
15023347
32.

Anthranilic acid amides: a novel class of antiangiogenic VEGF receptor kinase inhibitors.

Manley PW, Furet P, Bold G, Brüggen J, Mestan J, Meyer T, Schnell CR, Wood J, Haberey M, Huth A, Krüger M, Menrad A, Ottow E, Seidelmann D, Siemeister G, Thierauch KH.

J Med Chem. 2002 Dec 19;45(26):5687-93.

PMID:
12477352
33.

Protein kinases as targets for anticancer agents: from inhibitors to useful drugs.

Fabbro D, Ruetz S, Buchdunger E, Cowan-Jacob SW, Fendrich G, Liebetanz J, Mestan J, O'Reilly T, Traxler P, Chaudhuri B, Fretz H, Zimmermann J, Meyer T, Caravatti G, Furet P, Manley PW.

Pharmacol Ther. 2002 Feb-Mar;93(2-3):79-98. Review.

PMID:
12191602
34.

Vascular endothelial growth factor (VEGF) receptor-2 antagonists inhibit VEGF- and basic fibroblast growth factor-induced angiogenesis in vivo and in vitro.

Tille JC, Wood J, Mandriota SJ, Schnell C, Ferrari S, Mestan J, Zhu Z, Witte L, Pepper MS.

J Pharmacol Exp Ther. 2001 Dec;299(3):1073-85.

PMID:
11714897
35.

Skp2 is oncogenic and overexpressed in human cancers.

Gstaiger M, Jordan R, Lim M, Catzavelos C, Mestan J, Slingerland J, Krek W.

Proc Natl Acad Sci U S A. 2001 Apr 24;98(9):5043-8. Epub 2001 Apr 17.

36.

SH3GLB, a new endophilin-related protein family featuring an SH3 domain.

Pierrat B, Simonen M, Cueto M, Mestan J, Ferrigno P, Heim J.

Genomics. 2001 Jan 15;71(2):222-34.

PMID:
11161816
37.

New anilinophthalazines as potent and orally well absorbed inhibitors of the VEGF receptor tyrosine kinases useful as antagonists of tumor-driven angiogenesis

Bold G, Altmann KH, Frei J, Lang M, Manley PW, Traxler P, Wietfeld B, Bruggen J, Buchdunger E, Cozens R, Ferrari S, Furet P, Hofmann F, Martiny-Baron G, Mestan J, Rosel J, Sills M, Stover D, Acemoglu F, Boss E, Emmenegger R, Lasser L, Masso E, Roth R, Schlachter C, Vetterli W.

J Med Chem. 2000 Aug 10;43(16):3200. No abstract available.

PMID:
10956229
38.

New anilinophthalazines as potent and orally well absorbed inhibitors of the VEGF receptor tyrosine kinases useful as antagonists of tumor-driven angiogenesis.

Bold G, Altmann KH, Frei J, Lang M, Manley PW, Traxler P, Wietfeld B, Brüggen J, Buchdunger E, Cozens R, Ferrari S, Furet P, Hofmann F, Martiny-Baron G, Mestan J, Rösel J, Sills M, Stover D, Acemoglu F, Boss E, Emmenegger R, Lässer L, Masso E, Roth R, Schlachter C, Vetterli W.

J Med Chem. 2000 Jun 15;43(12):2310-23. Erratum in: J Med Chem 2000 Aug 10;43(16):3200.

PMID:
10882357
39.

PTK787/ZK 222584, a novel and potent inhibitor of vascular endothelial growth factor receptor tyrosine kinases, impairs vascular endothelial growth factor-induced responses and tumor growth after oral administration.

Wood JM, Bold G, Buchdunger E, Cozens R, Ferrari S, Frei J, Hofmann F, Mestan J, Mett H, O'Reilly T, Persohn E, Rösel J, Schnell C, Stover D, Theuer A, Towbin H, Wenger F, Woods-Cook K, Menrad A, Siemeister G, Schirner M, Thierauch KH, Schneider MR, Drevs J, Martiny-Baron G, Totzke F.

Cancer Res. 2000 Apr 15;60(8):2178-89.

40.

Inhibitors of protein kinases: CGP 41251, a protein kinase inhibitor with potential as an anticancer agent.

Fabbro D, Buchdunger E, Wood J, Mestan J, Hofmann F, Ferrari S, Mett H, O'Reilly T, Meyer T.

Pharmacol Ther. 1999 May-Jun;82(2-3):293-301. Review.

PMID:
10454207
41.

New aza-dipeptide analogues as potent and orally absorbed HIV-1 protease inhibitors: candidates for clinical development.

Bold G, Fässler A, Capraro HG, Cozens R, Klimkait T, Lazdins J, Mestan J, Poncioni B, Rösel J, Stover D, Tintelnot-Blomley M, Acemoglu F, Beck W, Boss E, Eschbach M, Hürlimann T, Masso E, Roussel S, Ucci-Stoll K, Wyss D, Lang M.

J Med Chem. 1998 Aug 27;41(18):3387-401.

PMID:
9719591
42.

Heat-treated myosin does not bind ATPase--inhibiting antibodies.

Gröschel-Stewart U, Christian AL, Mestan J.

Biochem Mol Biol Int. 1997 Jul;42(3):611-9.

PMID:
9247719
43.
44.

Profile of CGP 61755: a novel and potent HIV-1 protease inhibitor that shows enhanced anti-HIV activity when combined with other antiretroviral agents in vitro.

Lazdins JK, Bold G, Capraro HG, Cozens R, Fässler A, Flesch G, Klimkait T, Lang M, Mestan J, Poncioni B, Rösel J, Stover D, Tintelnot-Blomley M, Walker MR, Woods-Cook K.

Schweiz Med Wochenschr. 1996 Oct 26;126(43):1849-51.

PMID:
8916294
45.

Aza-peptide analogs as potent human immunodeficiency virus type-1 protease inhibitors with oral bioavailability.

Fässler A, Bold G, Capraro HG, Cozens R, Mestan J, Poncioni B, Rösel J, Tintelnot-Blomley M, Lang M.

J Med Chem. 1996 Aug 2;39(16):3203-16.

PMID:
8759643
46.

Synthesis of potent and orally active HIV-protease inhibitors.

Capraro HG, Bold G, Fässler A, Cozens R, Klimkait T, Lazdins J, Mestan J, Poncioni B, Rösel JL, Stover D, Lang M.

Arch Pharm (Weinheim). 1996 Jun;329(6):273-8.

PMID:
8767110
47.

Induction of intracellular and plasma 2',5'-oligoadenylate synthetase by pentostatin.

Ho AD, Klotzbücher A, Gross A, Dietz G, Mestan J, Jakobsen H, Hunstein W.

Leukemia. 1992 Mar;6(3):209-14.

PMID:
1564958
48.

Beta interferon subtype 1 induction by tumor necrosis factor.

Jacobsen H, Mestan J, Mittnacht S, Dieffenbach CW.

Mol Cell Biol. 1989 Jul;9(7):3037-42.

49.

Antiviral activity of tumour necrosis factor. Synergism with interferons and induction of oligo-2',5'-adenylate synthetase.

Mestan J, Brockhaus M, Kirchner H, Jacobsen H.

J Gen Virol. 1988 Dec;69 ( Pt 12):3113-20.

PMID:
2462015
50.

Preactivation of macrophages in mice acutely infected with Schistosoma mansoni.

Esparza I, Ruppel A, Mestan J, Krammer PH.

Immunobiology. 1988 May;177(2):105-19.

PMID:
3136079

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