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Page 1
Snapshots and ensembles of BTK and cIAP1 protein degrader ternary complexes.
Schiemer J, Horst R, Meng Y, Montgomery JI, Xu Y, Feng X, Borzilleri K, Uccello DP, Leverett C, Brown S, Che Y, Brown MF, Hayward MM, Gilbert AM, Noe MC, Calabrese MF. Schiemer J, et al. Among authors: calabrese mf. Nat Chem Biol. 2021 Feb;17(2):152-160. doi: 10.1038/s41589-020-00686-2. Epub 2020 Nov 16. Nat Chem Biol. 2021. PMID: 33199914
Structural basis for AMPK activation: natural and synthetic ligands regulate kinase activity from opposite poles by different molecular mechanisms.
Calabrese MF, Rajamohan F, Harris MS, Caspers NL, Magyar R, Withka JM, Wang H, Borzilleri KA, Sahasrabudhe PV, Hoth LR, Geoghegan KF, Han S, Brown J, Subashi TA, Reyes AR, Frisbie RK, Ward J, Miller RA, Landro JA, Londregan AT, Carpino PA, Cabral S, Smith AC, Conn EL, Cameron KO, Qiu X, Kurumbail RG. Calabrese MF, et al. Structure. 2014 Aug 5;22(8):1161-1172. doi: 10.1016/j.str.2014.06.009. Epub 2014 Jul 24. Structure. 2014. PMID: 25066137 Free article.
Discovery and Preclinical Characterization of 6-Chloro-5-[4-(1-hydroxycyclobutyl)phenyl]-1H-indole-3-carboxylic Acid (PF-06409577), a Direct Activator of Adenosine Monophosphate-activated Protein Kinase (AMPK), for the Potential Treatment of Diabetic Nephropathy.
Cameron KO, Kung DW, Kalgutkar AS, Kurumbail RG, Miller R, Salatto CT, Ward J, Withka JM, Bhattacharya SK, Boehm M, Borzilleri KA, Brown JA, Calabrese M, Caspers NL, Cokorinos E, Conn EL, Dowling MS, Edmonds DJ, Eng H, Fernando DP, Frisbie R, Hepworth D, Landro J, Mao Y, Rajamohan F, Reyes AR, Rose CR, Ryder T, Shavnya A, Smith AC, Tu M, Wolford AC, Xiao J. Cameron KO, et al. J Med Chem. 2016 Sep 8;59(17):8068-81. doi: 10.1021/acs.jmedchem.6b00866. Epub 2016 Aug 20. J Med Chem. 2016. PMID: 27490827
Optimization of Metabolic and Renal Clearance in a Series of Indole Acid Direct Activators of 5'-Adenosine Monophosphate-Activated Protein Kinase (AMPK).
Edmonds DJ, Kung DW, Kalgutkar AS, Filipski KJ, Ebner DC, Cabral S, Smith AC, Aspnes GE, Bhattacharya SK, Borzilleri KA, Brown JA, Calabrese MF, Caspers NL, Cokorinos EC, Conn EL, Dowling MS, Eng H, Feng B, Fernando DP, Genung NE, Herr M, Kurumbail RG, Lavergne SY, Lee EC, Li Q, Mathialagan S, Miller RA, Panteleev J, Polivkova J, Rajamohan F, Reyes AR, Salatto CT, Shavnya A, Thuma BA, Tu M, Ward J, Withka JM, Xiao J, Cameron KO. Edmonds DJ, et al. Among authors: calabrese mf. J Med Chem. 2018 Mar 22;61(6):2372-2383. doi: 10.1021/acs.jmedchem.7b01641. Epub 2018 Feb 28. J Med Chem. 2018. PMID: 29466005
Biophysical Interactions of Direct AMPK Activators.
Kurumbail RG, West GM, Dharmarajan V, Borzilleri KA, Withka JM, Ward J, Reyes AR, Rajamohan F, Griffin PR, Calabrese MF. Kurumbail RG, et al. Among authors: calabrese mf. Methods Mol Biol. 2018;1732:29-55. doi: 10.1007/978-1-4939-7598-3_3. Methods Mol Biol. 2018. PMID: 29480467
Delineating the role of cooperativity in the design of potent PROTACs for BTK.
Zorba A, Nguyen C, Xu Y, Starr J, Borzilleri K, Smith J, Zhu H, Farley KA, Ding W, Schiemer J, Feng X, Chang JS, Uccello DP, Young JA, Garcia-Irrizary CN, Czabaniuk L, Schuff B, Oliver R, Montgomery J, Hayward MM, Coe J, Chen J, Niosi M, Luthra S, Shah JC, El-Kattan A, Qiu X, West GM, Noe MC, Shanmugasundaram V, Gilbert AM, Brown MF, Calabrese MF. Zorba A, et al. Among authors: calabrese mf. Proc Natl Acad Sci U S A. 2018 Jul 31;115(31):E7285-E7292. doi: 10.1073/pnas.1803662115. Epub 2018 Jul 16. Proc Natl Acad Sci U S A. 2018. PMID: 30012605 Free PMC article.
Acyl Glucuronide Metabolites of 6-Chloro-5-[4-(1-hydroxycyclobutyl)phenyl]-1 H-indole-3-carboxylic Acid (PF-06409577) and Related Indole-3-carboxylic Acid Derivatives are Direct Activators of Adenosine Monophosphate-Activated Protein Kinase (AMPK).
Ryder TF, Calabrese MF, Walker GS, Cameron KO, Reyes AR, Borzilleri KA, Delmore J, Miller R, Kurumbail RG, Ward J, Kung DW, Brown JA, Edmonds DJ, Eng H, Wolford AC, Kalgutkar AS. Ryder TF, et al. Among authors: calabrese mf. J Med Chem. 2018 Aug 23;61(16):7273-7288. doi: 10.1021/acs.jmedchem.8b00807. Epub 2018 Aug 2. J Med Chem. 2018. PMID: 30036059
Targeted protein degradation: expanding the toolbox.
Schapira M, Calabrese MF, Bullock AN, Crews CM. Schapira M, et al. Among authors: calabrese mf. Nat Rev Drug Discov. 2019 Dec;18(12):949-963. doi: 10.1038/s41573-019-0047-y. Epub 2019 Oct 30. Nat Rev Drug Discov. 2019. PMID: 31666732
A covalent BTK ternary complex compatible with targeted protein degradation.
Schiemer J, Maxwell A, Horst R, Liu S, Uccello DP, Borzilleri K, Rajamohan N, Brown MF, Calabrese MF. Schiemer J, et al. Among authors: calabrese mf. Nat Commun. 2023 Mar 2;14(1):1189. doi: 10.1038/s41467-023-36738-z. Nat Commun. 2023. PMID: 36864023 Free PMC article.
29 results