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Small molecule inhibitors of BRAF in clinical trials.
Zambon A, Niculescu-Duvaz I, Niculescu-Duvaz D, Marais R, Springer CJ. Zambon A, et al. Bioorg Med Chem Lett. 2012 Jan 15;22(2):789-92. doi: 10.1016/j.bmcl.2011.11.060. Epub 2011 Dec 3. Bioorg Med Chem Lett. 2012. PMID: 22222036 Review.
Development of novel, highly potent inhibitors of V-RAF murine sarcoma viral oncogene homologue B1 (BRAF): increasing cellular potency through optimization of a distal heteroaromatic group.
Suijkerbuijk BM, Niculescu-Duvaz I, Gaulon C, Dijkstra HP, Niculescu-Duvaz D, Ménard D, Zambon A, Nourry A, Davies L, Manne HA, Friedlos F, Ogilvie LM, Hedley D, Lopes F, Preece NP, Moreno-Farre J, Raynaud FI, Kirk R, Whittaker S, Marais R, Springer CJ. Suijkerbuijk BM, et al. Among authors: zambon a. J Med Chem. 2010 Apr 8;53(7):2741-56. doi: 10.1021/jm900607f. J Med Chem. 2010. PMID: 20199087
Gatekeeper mutations mediate resistance to BRAF-targeted therapies.
Whittaker S, Kirk R, Hayward R, Zambon A, Viros A, Cantarino N, Affolter A, Nourry A, Niculescu-Duvaz D, Springer C, Marais R. Whittaker S, et al. Among authors: zambon a. Sci Transl Med. 2010 Jun 9;2(35):35ra41. doi: 10.1126/scitranslmed.3000758. Sci Transl Med. 2010. PMID: 20538618
Novel tricyclic pyrazole BRAF inhibitors with imidazole or furan central scaffolds.
Niculescu-Duvaz D, Niculescu-Duvaz I, Suijkerbuijk BM, Ménard D, Zambon A, Nourry A, Davies L, Manne HA, Friedlos F, Ogilvie L, Hedley D, Takle AK, Wilson DM, Pons JF, Coulter T, Kirk R, Cantarino N, Whittaker S, Marais R, Springer CJ. Niculescu-Duvaz D, et al. Among authors: zambon a. Bioorg Med Chem. 2010 Sep 15;18(18):6934-52. doi: 10.1016/j.bmc.2010.06.031. Epub 2010 Jun 15. Bioorg Med Chem. 2010. PMID: 20667740 Free PMC article.
BRAF as a therapeutic target: a patent review (2006 - 2012).
Zambon A, Niculescu-Duvaz D, Niculescu-Duvaz I, Marais R, Springer CJ. Zambon A, et al. Expert Opin Ther Pat. 2013 Feb;23(2):155-64. doi: 10.1517/13543776.2013.741593. Epub 2013 Jan 7. Expert Opin Ther Pat. 2013. PMID: 23294221 Review.
Paradox-breaking RAF inhibitors that also target SRC are effective in drug-resistant BRAF mutant melanoma.
Girotti MR, Lopes F, Preece N, Niculescu-Duvaz D, Zambon A, Davies L, Whittaker S, Saturno G, Viros A, Pedersen M, Suijkerbuijk BM, Menard D, McLeary R, Johnson L, Fish L, Ejiama S, Sanchez-Laorden B, Hohloch J, Carragher N, Macleod K, Ashton G, Marusiak AA, Fusi A, Brognard J, Frame M, Lorigan P, Marais R, Springer C. Girotti MR, et al. Among authors: zambon a. Cancer Cell. 2015 Jan 12;27(1):85-96. doi: 10.1016/j.ccell.2014.11.006. Epub 2014 Dec 11. Cancer Cell. 2015. PMID: 25500121 Free PMC article.
Anti-metastatic Inhibitors of Lysyl Oxidase (LOX): Design and Structure-Activity Relationships.
Leung L, Niculescu-Duvaz D, Smithen D, Lopes F, Callens C, McLeary R, Saturno G, Davies L, Aljarah M, Brown M, Johnson L, Zambon A, Chambers T, Ménard D, Bayliss N, Knight R, Fish L, Lawrence R, Challinor M, Tang H, Marais R, Springer C. Leung L, et al. Among authors: zambon a. J Med Chem. 2019 Jun 27;62(12):5863-5884. doi: 10.1021/acs.jmedchem.9b00335. Epub 2019 May 23. J Med Chem. 2019. PMID: 31070916 Free PMC article.
537 results