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Page 1
Preclinical assessment of the PI3Kα selective inhibitor inavolisib and prediction of its pharmacokinetics and efficacious dose in human.
Salphati L, Pang J, Plise EG, Cheong J, Braun MG, Friedman LS, Hong Thibodeau R, Jaochico A, Johnson R, Liu N, Nannini M, Sampath D, Song K, Hannan EJ, Staben ST. Salphati L, et al. Among authors: braun mg. Xenobiotica. 2024 Oct;54(10):808-820. doi: 10.1080/00498254.2024.2415103. Epub 2024 Dec 4. Xenobiotica. 2024. PMID: 39387185
Discovery of Potent, Selective, and Orally Available IRE1α Inhibitors Demonstrating Comparable PD Modulation to IRE1 Knockdown in a Multiple Myeloma Model.
Braun MG, Ashkenazi A, Beveridge RE, Castanedo G, Wallweber HA, Beresini MH, Clark KR, De Bruyn T, Fu L, Gibbons P, Jiang F, Kaufman S, Kan D, Kiefer JR, Leclerc JP, Lemire A, Ly C, Segal E, Sims J, Wang W, Wei W, Zhao L, Schwarz JB, Rudolph J. Braun MG, et al. J Med Chem. 2024 Jun 13;67(11):8708-8729. doi: 10.1021/acs.jmedchem.3c02425. Epub 2024 May 15. J Med Chem. 2024. PMID: 38748820
Discovery and Optimization of Selective Brain-Penetrant EBP Inhibitors that Enhance Oligodendrocyte Formation.
Dorel R, Sun D, Carruthers N, Castanedo GM, Ung PM, Factor DC, Li T, Baumann H, Janota D, Pang J, Salphati L, Meklemburg R, Korman AJ, Harper HE, Stubblefield S, Payandeh J, McHugh D, Lang BT, Tesar PJ, Dere E, Masureel M, Adams DJ, Volgraf M, Braun MG. Dorel R, et al. Among authors: braun mg. J Med Chem. 2024 Mar 28;67(6):4819-4832. doi: 10.1021/acs.jmedchem.3c02396. Epub 2024 Mar 12. J Med Chem. 2024. PMID: 38470227
Discovery of GDC-0077 (Inavolisib), a Highly Selective Inhibitor and Degrader of Mutant PI3Kα.
Hanan EJ, Braun MG, Heald RA, MacLeod C, Chan C, Clausen S, Edgar KA, Eigenbrot C, Elliott R, Endres N, Friedman LS, Gogol E, Gu XH, Thibodeau RH, Jackson PS, Kiefer JR, Knight JD, Nannini M, Narukulla R, Pace A, Pang J, Purkey HE, Salphati L, Sampath D, Schmidt S, Sideris S, Song K, Sujatha-Bhaskar S, Ultsch M, Wallweber H, Xin J, Yeap S, Young A, Zhong Y, Staben ST. Hanan EJ, et al. Among authors: braun mg. J Med Chem. 2022 Dec 22;65(24):16589-16621. doi: 10.1021/acs.jmedchem.2c01422. Epub 2022 Dec 1. J Med Chem. 2022. PMID: 36455032
Identification of BRaf-Sparing Amino-Thienopyrimidines with Potent IRE1α Inhibitory Activity.
Beveridge RE, Wallweber HA, Ashkenazi A, Beresini M, Clark KR, Gibbons P, Ghiro E, Kaufman S, Larivée A, Leblanc M, Leclerc JP, Lemire A, Ly C, Rudolph J, Schwarz JB, Srivastava S, Wang W, Zhao L, Braun MG. Beveridge RE, et al. Among authors: braun mg. ACS Med Chem Lett. 2020 Oct 16;11(12):2389-2396. doi: 10.1021/acsmedchemlett.0c00344. eCollection 2020 Dec 10. ACS Med Chem Lett. 2020. PMID: 33335661 Free PMC article.
Unstable Mechanisms of Resistance to Inhibitors of Escherichia coli Lipoprotein Signal Peptidase.
Pantua H, Skippington E, Braun MG, Noland CL, Diao J, Peng Y, Gloor SL, Yan D, Kang J, Katakam AK, Reeder J, Castanedo GM, Garland K, Komuves L, Sagolla M, Austin CD, Murray J, Xu Y, Modrusan Z, Xu M, Hanan EJ, Kapadia SB. Pantua H, et al. Among authors: braun mg. mBio. 2020 Sep 8;11(5):e02018-20. doi: 10.1128/mBio.02018-20. mBio. 2020. PMID: 32900806 Free PMC article.
Optimization of globomycin analogs as novel gram-negative antibiotics.
Garland K, Pantua H, Braun MG, Burdick DJ, Castanedo GM, Chen YC, Cheng YX, Cheong J, Daniels B, Deshmukh G, Fu Y, Gibbons P, Gloor SL, Hua R, Labadie S, Liu X, Pastor R, Stivala C, Xu M, Xu Y, Zheng H, Kapadia SB, Hanan EJ. Garland K, et al. Among authors: braun mg. Bioorg Med Chem Lett. 2020 Oct 15;30(20):127419. doi: 10.1016/j.bmcl.2020.127419. Epub 2020 Aug 5. Bioorg Med Chem Lett. 2020. PMID: 32768648
Disruption of IRE1α through its kinase domain attenuates multiple myeloma.
Harnoss JM, Le Thomas A, Shemorry A, Marsters SA, Lawrence DA, Lu M, Chen YA, Qing J, Totpal K, Kan D, Segal E, Merchant M, Reichelt M, Ackerly Wallweber H, Wang W, Clark K, Kaufman S, Beresini MH, Laing ST, Sandoval W, Lorenzo M, Wu J, Ly J, De Bruyn T, Heidersbach A, Haley B, Gogineni A, Weimer RM, Lee D, Braun MG, Rudolph J, VanWyngarden MJ, Sherbenou DW, Gomez-Bougie P, Amiot M, Acosta-Alvear D, Walter P, Ashkenazi A. Harnoss JM, et al. Among authors: braun mg. Proc Natl Acad Sci U S A. 2019 Aug 13;116(33):16420-16429. doi: 10.1073/pnas.1906999116. Epub 2019 Aug 1. Proc Natl Acad Sci U S A. 2019. PMID: 31371506 Free PMC article.
31 results