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The MCL1 inhibitor S63845 is tolerable and effective in diverse cancer models.
Kotschy A, Szlavik Z, Murray J, Davidson J, Maragno AL, Le Toumelin-Braizat G, Chanrion M, Kelly GL, Gong JN, Moujalled DM, Bruno A, Csekei M, Paczal A, Szabo ZB, Sipos S, Radics G, Proszenyak A, Balint B, Ondi L, Blasko G, Robertson A, Surgenor A, Dokurno P, Chen I, Matassova N, Smith J, Pedder C, Graham C, Studeny A, Lysiak-Auvity G, Girard AM, Gravé F, Segal D, Riffkin CD, Pomilio G, Galbraith LC, Aubrey BJ, Brennan MS, Herold MJ, Chang C, Guasconi G, Cauquil N, Melchiore F, Guigal-Stephan N, Lockhart B, Colland F, Hickman JA, Roberts AW, Huang DC, Wei AH, Strasser A, Lessene G, Geneste O. Kotschy A, et al. Among authors: lockhart b. Nature. 2016 Oct 27;538(7626):477-482. doi: 10.1038/nature19830. Epub 2016 Oct 19. Nature. 2016. PMID: 27760111
S49076 is a novel kinase inhibitor of MET, AXL, and FGFR with strong preclinical activity alone and in association with bevacizumab.
Burbridge MF, Bossard CJ, Saunier C, Fejes I, Bruno A, Léonce S, Ferry G, Da Violante G, Bouzom F, Cattan V, Jacquet-Bescond A, Comoglio PM, Lockhart BP, Boutin JA, Cordi A, Ortuno JC, Pierré A, Hickman JA, Cruzalegui FH, Depil S. Burbridge MF, et al. Mol Cancer Ther. 2013 Sep;12(9):1749-62. doi: 10.1158/1535-7163.MCT-13-0075. Epub 2013 Jun 26. Mol Cancer Ther. 2013. PMID: 23804704
Targeting Bcl-2/Bcl-XL induces antitumor activity in uveal melanoma patient-derived xenografts.
Némati F, de Montrion C, Lang G, Kraus-Berthier L, Carita G, Sastre-Garau X, Berniard A, Vallerand D, Geneste O, de Plater L, Pierré A, Lockhart B, Desjardins L, Piperno-Neumann S, Depil S, Decaudin D. Némati F, et al. Among authors: lockhart b. PLoS One. 2014 Jan 13;9(1):e80836. doi: 10.1371/journal.pone.0080836. eCollection 2014. PLoS One. 2014. PMID: 24454684 Free PMC article.
Specific oncogenic activity of the Src-family tyrosine kinase c-Yes in colon carcinoma cells.
Sancier F, Dumont A, Sirvent A, Paquay de Plater L, Edmonds T, David G, Jan M, de Montrion C, Cogé F, Léonce S, Burbridge M, Bruno A, Boutin JA, Lockhart B, Roche S, Cruzalegui F. Sancier F, et al. Among authors: lockhart b. PLoS One. 2011 Feb 24;6(2):e17237. doi: 10.1371/journal.pone.0017237. PLoS One. 2011. PMID: 21390316 Free PMC article.
Only a subset of Met-activated pathways are required to sustain oncogene addiction.
Bertotti A, Burbridge MF, Gastaldi S, Galimi F, Torti D, Medico E, Giordano S, Corso S, Rolland-Valognes G, Lockhart BP, Hickman JA, Comoglio PM, Trusolino L. Bertotti A, et al. Sci Signal. 2009 Dec 8;2(100):ra80. doi: 10.1126/scisignal.2000643. Sci Signal. 2009. PMID: 19996456 Free article. Corrected and republished.
Genetic deletion of trace amine 1 receptors reveals their role in auto-inhibiting the actions of ecstasy (MDMA).
Di Cara B, Maggio R, Aloisi G, Rivet JM, Lundius EG, Yoshitake T, Svenningsson P, Brocco M, Gobert A, De Groote L, Cistarelli L, Veiga S, De Montrion C, Rodriguez M, Galizzi JP, Lockhart BP, Cogé F, Boutin JA, Vayer P, Verdouw PM, Groenink L, Millan MJ. Di Cara B, et al. Among authors: lockhart bp. J Neurosci. 2011 Nov 23;31(47):16928-40. doi: 10.1523/JNEUROSCI.2502-11.2011. J Neurosci. 2011. PMID: 22114263 Free PMC article.
163 results