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Items: 18

1.

Characterization and phase I study of CLR457, an orally bioavailable pan-class I PI3-kinase inhibitor.

Harding JJ, Bauer TM, Tan DSW, Bedard PL, Rodon J, Doi T, Schnell C, Iyer V, Baffert F, Radhakrishnan R, Fabre C, Juric D.

Invest New Drugs. 2019 Apr;37(2):271-281. doi: 10.1007/s10637-018-0627-4. Epub 2018 Aug 3.

2.

Activity of the Type II JAK2 Inhibitor CHZ868 in B Cell Acute Lymphoblastic Leukemia.

Wu SC, Li LS, Kopp N, Montero J, Chapuy B, Yoda A, Christie AL, Liu H, Christodoulou A, van Bodegom D, van der Zwet J, Layer JV, Tivey T, Lane AA, Ryan JA, Ng SY, DeAngelo DJ, Stone RM, Steensma D, Wadleigh M, Harris M, Mandon E, Ebel N, Andraos R, Romanet V, Dölemeyer A, Sterker D, Zender M, Rodig SJ, Murakami M, Hofmann F, Kuo F, Eck MJ, Silverman LB, Sallan SE, Letai A, Baffert F, Vangrevelinghe E, Radimerski T, Gaul C, Weinstock DM.

Cancer Cell. 2015 Jul 13;28(1):29-41. doi: 10.1016/j.ccell.2015.06.005.

3.

CHZ868, a Type II JAK2 Inhibitor, Reverses Type I JAK Inhibitor Persistence and Demonstrates Efficacy in Myeloproliferative Neoplasms.

Meyer SC, Keller MD, Chiu S, Koppikar P, Guryanova OA, Rapaport F, Xu K, Manova K, Pankov D, O'Reilly RJ, Kleppe M, McKenney AS, Shih AH, Shank K, Ahn J, Papalexi E, Spitzer B, Socci N, Viale A, Mandon E, Ebel N, Andraos R, Rubert J, Dammassa E, Romanet V, Dölemeyer A, Zender M, Heinlein M, Rampal R, Weinberg RS, Hoffman R, Sellers WR, Hofmann F, Murakami M, Baffert F, Gaul C, Radimerski T, Levine RL.

Cancer Cell. 2015 Jul 13;28(1):15-28. doi: 10.1016/j.ccell.2015.06.006.

4.

JAK1/2 and Pan-deacetylase inhibitor combination therapy yields improved efficacy in preclinical mouse models of JAK2V617F-driven disease.

Evrot E, Ebel N, Romanet V, Roelli C, Andraos R, Qian Z, Dölemeyer A, Dammassa E, Sterker D, Cozens R, Hofmann F, Murakami M, Baffert F, Radimerski T.

Clin Cancer Res. 2013 Nov 15;19(22):6230-41. doi: 10.1158/1078-0432.CCR-13-0905. Epub 2013 Sep 30.

5.

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.

6.

Genetic resistance to JAK2 enzymatic inhibitors is overcome by HSP90 inhibition.

Weigert O, Lane AA, Bird L, Kopp N, Chapuy B, van Bodegom D, Toms AV, Marubayashi S, Christie AL, McKeown M, Paranal RM, Bradner JE, Yoda A, Gaul C, Vangrevelinghe E, Romanet V, Murakami M, Tiedt R, Ebel N, Evrot E, De Pover A, Régnier CH, Erdmann D, Hofmann F, Eck MJ, Sallan SE, Levine RL, Kung AL, Baffert F, Radimerski T, Weinstock DM.

J Exp Med. 2012 Feb 13;209(2):259-73. doi: 10.1084/jem.20111694. Epub 2012 Jan 23.

7.

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. 2010 Jul;9(7):1945-55. doi: 10.1158/1535-7163.MCT-10-0053. Epub 2010 Jun 29.

8.

Discovery and SAR of potent, orally available 2,8-diaryl-quinoxalines as a new class of JAK2 inhibitors.

Pissot-Soldermann C, Gerspacher M, Furet P, Gaul C, Holzer P, McCarthy C, Radimerski T, Regnier CH, Baffert F, Drueckes P, Tavares GA, Vangrevelinghe E, Blasco F, Ottaviani G, Ossola F, Scesa J, Reetz J.

Bioorg Med Chem Lett. 2010 Apr 15;20(8):2609-13. doi: 10.1016/j.bmcl.2010.02.056. Epub 2010 Feb 19.

PMID:
20231096
9.

2-Amino-aryl-7-aryl-benzoxazoles as potent, selective and orally available JAK2 inhibitors.

Gerspacher M, Furet P, Pissot-Soldermann C, Gaul C, Holzer P, Vangrevelinghe E, Lang M, Erdmann D, Radimerski T, Regnier CH, Chene P, De Pover A, Hofmann F, Baffert F, Buhl T, Aichholz R, Blasco F, Endres R, Trappe J, Drueckes P.

Bioorg Med Chem Lett. 2010 Mar 1;20(5):1724-7. doi: 10.1016/j.bmcl.2010.01.069. Epub 2010 Jan 21.

PMID:
20138510
10.

Inhibition of multiple vascular endothelial growth factor receptors (VEGFR) blocks lymph node metastases but inhibition of VEGFR-2 is sufficient to sensitize tumor cells to platinum-based chemotherapeutics.

Sini P, Samarzija I, Baffert F, Littlewood-Evans A, Schnell C, Theuer A, Christian S, Boos A, Hess-Stumpp H, Foekens JA, Setyono-Han B, Wood J, Hynes NE.

Cancer Res. 2008 Mar 1;68(5):1581-92. doi: 10.1158/0008-5472.CAN-06-4685.

11.

Cellular changes in normal blood capillaries undergoing regression after inhibition of VEGF signaling.

Baffert F, Le T, Sennino B, Thurston G, Kuo CJ, Hu-Lowe D, McDonald DM.

Am J Physiol Heart Circ Physiol. 2006 Feb;290(2):H547-59. Epub 2005 Sep 19.

12.

Angiopoietin-1 decreases plasma leakage by reducing number and size of endothelial gaps in venules.

Baffert F, Le T, Thurston G, McDonald DM.

Am J Physiol Heart Circ Physiol. 2006 Jan;290(1):H107-18. Epub 2005 Aug 26.

13.

Long-term and sustained COMP-Ang1 induces long-lasting vascular enlargement and enhanced blood flow.

Cho CH, Kim KE, Byun J, Jang HS, Kim DK, Baluk P, Baffert F, Lee GM, Mochizuki N, Kim J, Jeon BH, McDonald DM, Koh GY.

Circ Res. 2005 Jul 8;97(1):86-94. Epub 2005 Jun 16. Erratum in: Circ Res. 2006 May 12;98(9):e69.

PMID:
15961719
14.

Angiopoietin 1 causes vessel enlargement, without angiogenic sprouting, during a critical developmental period.

Thurston G, Wang Q, Baffert F, Rudge J, Papadopoulos N, Jean-Guillaume D, Wiegand S, Yancopoulos GD, McDonald DM.

Development. 2005 Jul;132(14):3317-26. Epub 2005 Jun 15.

15.

Inhibition of vascular endothelial growth factor (VEGF) signaling in cancer causes loss of endothelial fenestrations, regression of tumor vessels, and appearance of basement membrane ghosts.

Inai T, Mancuso M, Hashizume H, Baffert F, Haskell A, Baluk P, Hu-Lowe DD, Shalinsky DR, Thurston G, Yancopoulos GD, McDonald DM.

Am J Pathol. 2004 Jul;165(1):35-52.

16.

Age-related changes in vascular endothelial growth factor dependency and angiopoietin-1-induced plasticity of adult blood vessels.

Baffert F, Thurston G, Rochon-Duck M, Le T, Brekken R, McDonald DM.

Circ Res. 2004 Apr 16;94(7):984-92. Epub 2004 Mar 4.

PMID:
15001532
17.

The antiangiogenic agent neovastat (AE-941) inhibits vascular endothelial growth factor-mediated biological effects.

Béliveau R, Gingras D, Kruger EA, Lamy S, Sirois P, Simard B, Sirois MG, Tranqui L, Baffert F, Beaulieu E, Dimitriadou V, Pépin MC, Courjal F, Ricard I, Poyet P, Falardeau P, Figg WD, Dupont E.

Clin Cancer Res. 2002 Apr;8(4):1242-50.

18.

Effects of prolonged exposure to hypoxia on morphological changes of endothelial cells plated on fibrin gel.

Baffert F, Usson Y, Tranqui L.

Eur J Cell Biol. 2001 Jan;80(1):78-86.

PMID:
11211938

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