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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: lopes f. 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.
The paradox-breaking panRAF plus SRC family kinase inhibitor, CCT3833, is effective in mutant KRAS-driven cancers.
Saturno G, Lopes F, Niculescu-Duvaz I, Niculescu-Duvaz D, Zambon A, Davies L, Johnson L, Preece N, Lee R, Viros A, Holovanchuk D, Pedersen M, McLeary R, Lorigan P, Dhomen N, Fisher C, Banerji U, Dean E, Krebs MG, Gore M, Larkin J, Marais R, Springer C. Saturno G, et al. Among authors: lopes f. Ann Oncol. 2021 Feb;32(2):269-278. doi: 10.1016/j.annonc.2020.10.483. Epub 2020 Oct 29. Ann Oncol. 2021. PMID: 33130216 Free PMC article.
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: lopes f. J Med Chem. 2010 Apr 8;53(7):2741-56. doi: 10.1021/jm900607f. J Med Chem. 2010. PMID: 20199087
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 BMJM, 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: lopes f. Cancer Cell. 2017 Mar 13;31(3):466. doi: 10.1016/j.ccell.2017.02.007. Cancer Cell. 2017. PMID: 28292443 Free PMC article. No abstract available.
Novel hinge binder improves activity and pharmacokinetic properties of BRAF inhibitors.
Zambon A, Ménard D, Suijkerbuijk BM, Niculescu-Duvaz I, Whittaker S, Niculescu-Duvaz D, Nourry A, Davies L, Manne HA, Lopes F, Preece N, Hedley D, Ogilvie LM, Kirk R, Marais R, Springer CJ. Zambon A, et al. Among authors: lopes f. J Med Chem. 2010 Aug 12;53(15):5639-55. doi: 10.1021/jm100383b. J Med Chem. 2010. PMID: 20597484
A novel, selective, and efficacious nanomolar pyridopyrazinone inhibitor of V600EBRAF.
Whittaker S, Ménard D, Kirk R, Ogilvie L, Hedley D, Zambon A, Lopes F, Preece N, Manne H, Rana S, Lambros M, Reis-Filho JS, Marais R, Springer CJ. Whittaker S, et al. Among authors: lopes f. Cancer Res. 2010 Oct 15;70(20):8036-44. doi: 10.1158/0008-5472.CAN-10-1366. Epub 2010 Aug 31. Cancer Res. 2010. PMID: 20807807 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: lopes f. 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.
2-Aminomethylene-5-sulfonylthiazole Inhibitors of Lysyl Oxidase (LOX) and LOXL2 Show Significant Efficacy in Delaying Tumor Growth.
Smithen DA, Leung LMH, Challinor M, Lawrence R, Tang H, Niculescu-Duvaz D, Pearce SP, Mcleary R, Lopes F, Aljarah M, Brown M, Johnson L, Thomson G, Marais R, Springer C. Smithen DA, et al. Among authors: lopes f. J Med Chem. 2020 Mar 12;63(5):2308-2324. doi: 10.1021/acs.jmedchem.9b01112. Epub 2019 Sep 4. J Med Chem. 2020. PMID: 31430136 Free PMC article.
1,142 results