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Page 1
KRASG12C Inhibition with Sotorasib in Advanced Solid Tumors.
Hong DS, Fakih MG, Strickler JH, Desai J, Durm GA, Shapiro GI, Falchook GS, Price TJ, Sacher A, Denlinger CS, Bang YJ, Dy GK, Krauss JC, Kuboki Y, Kuo JC, Coveler AL, Park K, Kim TW, Barlesi F, Munster PN, Ramalingam SS, Burns TF, Meric-Bernstam F, Henary H, Ngang J, Ngarmchamnanrith G, Kim J, Houk BE, Canon J, Lipford JR, Friberg G, Lito P, Govindan R, Li BT. Hong DS, et al. Among authors: lipford jr. N Engl J Med. 2020 Sep 24;383(13):1207-1217. doi: 10.1056/NEJMoa1917239. Epub 2020 Sep 20. N Engl J Med. 2020. PMID: 32955176 Free PMC article. Clinical Trial.
The clinical KRAS(G12C) inhibitor AMG 510 drives anti-tumour immunity.
Canon J, Rex K, Saiki AY, Mohr C, Cooke K, Bagal D, Gaida K, Holt T, Knutson CG, Koppada N, Lanman BA, Werner J, Rapaport AS, San Miguel T, Ortiz R, Osgood T, Sun JR, Zhu X, McCarter JD, Volak LP, Houk BE, Fakih MG, O'Neil BH, Price TJ, Falchook GS, Desai J, Kuo J, Govindan R, Hong DS, Ouyang W, Henary H, Arvedson T, Cee VJ, Lipford JR. Canon J, et al. Among authors: lipford jr. Nature. 2019 Nov;575(7781):217-223. doi: 10.1038/s41586-019-1694-1. Epub 2019 Oct 30. Nature. 2019. PMID: 31666701 Clinical Trial.
Diverse alterations associated with resistance to KRAS(G12C) inhibition.
Zhao Y, Murciano-Goroff YR, Xue JY, Ang A, Lucas J, Mai TT, Da Cruz Paula AF, Saiki AY, Mohn D, Achanta P, Sisk AE, Arora KS, Roy RS, Kim D, Li C, Lim LP, Li M, Bahr A, Loomis BR, de Stanchina E, Reis-Filho JS, Weigelt B, Berger M, Riely G, Arbour KC, Lipford JR, Li BT, Lito P. Zhao Y, et al. Among authors: lipford jr. Nature. 2021 Nov;599(7886):679-683. doi: 10.1038/s41586-021-04065-2. Epub 2021 Nov 10. Nature. 2021. PMID: 34759319 Free PMC article.
Mercapturate pathway metabolites of sotorasib, a covalent inhibitor of KRASG12C, are associated with renal toxicity in the Sprague Dawley rat.
Werner JA, Davies R, Wahlstrom J, Dahal UP, Jiang M, Stauber J, David B, Siska W, Thomas B, Ishida K, Humphreys WG, Lipford JR, Monticello TM. Werner JA, et al. Among authors: lipford jr. Toxicol Appl Pharmacol. 2021 Jul 15;423:115578. doi: 10.1016/j.taap.2021.115578. Epub 2021 May 15. Toxicol Appl Pharmacol. 2021. PMID: 34004237
Discovery of a Covalent Inhibitor of KRASG12C (AMG 510) for the Treatment of Solid Tumors.
Lanman BA, Allen JR, Allen JG, Amegadzie AK, Ashton KS, Booker SK, Chen JJ, Chen N, Frohn MJ, Goodman G, Kopecky DJ, Liu L, Lopez P, Low JD, Ma V, Minatti AE, Nguyen TT, Nishimura N, Pickrell AJ, Reed AB, Shin Y, Siegmund AC, Tamayo NA, Tegley CM, Walton MC, Wang HL, Wurz RP, Xue M, Yang KC, Achanta P, Bartberger MD, Canon J, Hollis LS, McCarter JD, Mohr C, Rex K, Saiki AY, San Miguel T, Volak LP, Wang KH, Whittington DA, Zech SG, Lipford JR, Cee VJ. Lanman BA, et al. Among authors: lipford jr. J Med Chem. 2020 Jan 9;63(1):52-65. doi: 10.1021/acs.jmedchem.9b01180. Epub 2019 Dec 24. J Med Chem. 2020. PMID: 31820981
Discovery of N-(1-Acryloylazetidin-3-yl)-2-(1H-indol-1-yl)acetamides as Covalent Inhibitors of KRASG12C.
Shin Y, Jeong JW, Wurz RP, Achanta P, Arvedson T, Bartberger MD, Campuzano IDG, Fucini R, Hansen SK, Ingersoll J, Iwig JS, Lipford JR, Ma V, Kopecky DJ, McCarter J, San Miguel T, Mohr C, Sabet S, Saiki AY, Sawayama A, Sethofer S, Tegley CM, Volak LP, Yang K, Lanman BA, Erlanson DA, Cee VJ. Shin Y, et al. Among authors: lipford jr. ACS Med Chem Lett. 2019 Aug 20;10(9):1302-1308. doi: 10.1021/acsmedchemlett.9b00258. eCollection 2019 Sep 12. ACS Med Chem Lett. 2019. PMID: 31531201 Free PMC article.
Discovery of imidazopyridazines as potent Pim-1/2 kinase inhibitors.
Wurz RP, Sastri C, D'Amico DC, Herberich B, Jackson CLM, Pettus LH, Tasker AS, Wu B, Guerrero N, Lipford JR, Winston JT, Yang Y, Wang P, Nguyen Y, Andrews KL, Huang X, Lee MR, Mohr C, Zhang JD, Reid DL, Xu Y, Zhou Y, Wang HL. Wurz RP, et al. Among authors: lipford jr. Bioorg Med Chem Lett. 2016 Nov 15;26(22):5580-5590. doi: 10.1016/j.bmcl.2016.09.067. Epub 2016 Oct 1. Bioorg Med Chem Lett. 2016. PMID: 27769621
Discovery of ( R)-8-(6-Methyl-4-oxo-1,4,5,6-tetrahydropyrrolo[3,4- b]pyrrol-2-yl)-3-(1-methylcyclopropyl)-2-((1-methylcyclopropyl)amino)quinazolin-4(3 H)-one, a Potent and Selective Pim-1/2 Kinase Inhibitor for Hematological Malignancies.
Wang HL, Andrews KL, Booker SK, Canon J, Cee VJ, Chavez F Jr, Chen Y, Eastwood H, Guerrero N, Herberich B, Hickman D, Lanman BA, Laszlo J 3rd, Lee MR, Lipford JR, Mattson B, Mohr C, Nguyen Y, Norman MH, Pettus LH, Powers D, Reed AB, Rex K, Sastri C, Tamayo N, Wang P, Winston JT, Wu B, Wu Q, Wu T, Wurz RP, Xu Y, Zhou Y, Tasker AS. Wang HL, et al. Among authors: lipford jr. J Med Chem. 2019 Feb 14;62(3):1523-1540. doi: 10.1021/acs.jmedchem.8b01733. Epub 2019 Jan 17. J Med Chem. 2019. PMID: 30624936
40 results