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PF-06463922 is a potent and selective next-generation ROS1/ALK inhibitor capable of blocking crizotinib-resistant ROS1 mutations.
Zou HY, Li Q, Engstrom LD, West M, Appleman V, Wong KA, McTigue M, Deng YL, Liu W, Brooun A, Timofeevski S, McDonnell SR, Jiang P, Falk MD, Lappin PB, Affolter T, Nichols T, Hu W, Lam J, Johnson TW, Smeal T, Charest A, Fantin VR. Zou HY, et al. Among authors: falk md. Proc Natl Acad Sci U S A. 2015 Mar 17;112(11):3493-8. doi: 10.1073/pnas.1420785112. Epub 2015 Mar 2. Proc Natl Acad Sci U S A. 2015. PMID: 25733882 Free PMC article.
Acquired resistance to crizotinib from a mutation in CD74-ROS1.
Awad MM, Katayama R, McTigue M, Liu W, Deng YL, Brooun A, Friboulet L, Huang D, Falk MD, Timofeevski S, Wilner KD, Lockerman EL, Khan TM, Mahmood S, Gainor JF, Digumarthy SR, Stone JR, Mino-Kenudson M, Christensen JG, Iafrate AJ, Engelman JA, Shaw AT. Awad MM, et al. Among authors: falk md. N Engl J Med. 2013 Jun 20;368(25):2395-401. doi: 10.1056/NEJMoa1215530. Epub 2013 Jun 1. N Engl J Med. 2013. PMID: 23724914 Free PMC article.
Structure-Based Drug Design and Synthesis of PI3Kα-Selective Inhibitor (PF-06843195).
Cheng H, Orr STM, Bailey S, Brooun A, Chen P, Deal JG, Deng YL, Edwards MP, Gallego GM, Grodsky N, Huang B, Jalaie M, Kaiser S, Kania RS, Kephart SE, Lafontaine J, Ornelas MA, Pairish M, Planken S, Shen H, Sutton S, Zehnder L, Almaden CD, Bagrodia S, Falk MD, Gukasyan HJ, Ho C, Kang X, Kosa RE, Liu L, Spilker ME, Timofeevski S, Visswanathan R, Wang Z, Meng F, Ren S, Shao L, Xu F, Kath JC. Cheng H, et al. Among authors: falk md. J Med Chem. 2021 Jan 14;64(1):644-661. doi: 10.1021/acs.jmedchem.0c01652. Epub 2020 Dec 24. J Med Chem. 2021. PMID: 33356246
High-throughput screen using a single-cell tyrosine phosphatase assay reveals biologically active inhibitors of tyrosine phosphatase CD45.
Stanford SM, Panchal RG, Walker LM, Wu DJ, Falk MD, Mitra S, Damle SS, Ruble D, Kaltcheva T, Zhang S, Zhang ZY, Bavari S, Barrios AM, Bottini N. Stanford SM, et al. Among authors: falk md. Proc Natl Acad Sci U S A. 2012 Aug 28;109(35):13972-7. doi: 10.1073/pnas.1205028109. Epub 2012 Aug 13. Proc Natl Acad Sci U S A. 2012. PMID: 22891353 Free PMC article.
Prokinetic actions of luminally acting 5-HT4 receptor agonists.
Konen JR, Haag MM, Guseva D, Hurd M, Linton AA, Lavoie B, Kerrigan CB, Joyce E, Bischoff SC, Swann S, Griffin L, Matsukawa J, Falk MD, Gibson TS, Hennig GW, Wykosky J, Mawe GM. Konen JR, et al. Among authors: falk md. Neurogastroenterol Motil. 2021 Apr;33(4):e14026. doi: 10.1111/nmo.14026. Epub 2020 Nov 12. Neurogastroenterol Motil. 2021. PMID: 33185015 Free PMC article.