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Page 1
Identification of highly selective SIK1/2 inhibitors that modulate innate immune activation and suppress intestinal inflammation.
Babbe H, Sundberg TB, Tichenor M, Seierstad M, Bacani G, Berstler J, Chai W, Chang L, Chung M, Coe K, Collins B, Finley M, Guletsky A, Lemke CT, Mak PA, Mathur A, Mercado-Marin EV, Metkar S, Raymond DD, Rives ML, Rizzolio M, Shaffer PL, Smith R, Smith J, Steele R, Steffens H, Suarez J, Tian G, Majewski N, Volak LP, Wei J, Desai PT, Ong LL, Koudriakova T, Goldberg SD, Hirst G, Kaushik VK, Ort T, Seth N, Graham DB, Plevy S, Venable JD, Xavier RJ, Towne JE. Babbe H, et al. Among authors: lemke ct. Proc Natl Acad Sci U S A. 2024 Jan 2;121(1):e2307086120. doi: 10.1073/pnas.2307086120. Epub 2023 Dec 26. Proc Natl Acad Sci U S A. 2024. PMID: 38147543 Free PMC article.
BRD-810 is a highly selective MCL1 inhibitor with optimized in vivo clearance and robust efficacy in solid and hematological tumor models.
Rauh U, Wei G, Serrano-Wu M, Kosmidis G, Kaulfuss S, Siegel F, Thede K, McFarland J, Lemke CT, Werbeck N, Nowak-Reppel K, Pilari S, Menz S, Ocker M, Zhang W, Davis K, Poncet-Montange G, Roth J, Daniels D, Kaushik VK, Hubbard B, Ziegelbauer K, Golub TR. Rauh U, et al. Among authors: lemke ct. Nat Cancer. 2024 Oct;5(10):1479-1493. doi: 10.1038/s43018-024-00814-0. Epub 2024 Aug 23. Nat Cancer. 2024. PMID: 39179926 Free PMC article.
Comprehensive structure-function analysis reveals gain- and loss-of-function mechanisms impacting oncogenic KRAS activity.
Kwon JJ, Dilly J, Liu S, Kim E, Bian Y, Dharmaiah S, Tran TH, Kapner KS, Ly SH, Yang X, Rabara D, Waybright TJ, Giacomelli AO, Hong AL, Misek S, Wang B, Ravi A, Doench JG, Beroukhim R, Lemke CT, Haigis KM, Esposito D, Root DE, Nissley DV, Stephen AG, McCormick F, Simanshu DK, Hahn WC, Aguirre AJ. Kwon JJ, et al. Among authors: lemke ct. bioRxiv [Preprint]. 2024 Oct 25:2024.10.22.618529. doi: 10.1101/2024.10.22.618529. bioRxiv. 2024. PMID: 39484452 Free PMC article. Preprint.
Discovery and characterization of orally bioavailable 4-chloro-6-fluoroisophthalamides as covalent PPARG inverse-agonists.
Orsi DL, Ferrara SJ, Siegel S, Friberg A, Bouché L, Pook E, Lienau P, Bluck JP, Lemke CT, Akcay G, Stellfeld T, Meyer H, Pütter V, Holton SJ, Korr D, Jerchel-Furau I, Pantelidou C, Strathdee CA, Meyerson M, Eis K, Goldstein JT. Orsi DL, et al. Among authors: lemke ct. Bioorg Med Chem. 2023 Jan 15;78:117130. doi: 10.1016/j.bmc.2022.117130. Epub 2022 Dec 13. Bioorg Med Chem. 2023. PMID: 36542958 Free article.
Correction to "Discovery and Structure-Based Design of Potent Covalent PPARγ Inverse-Agonists BAY-4931 and BAY-0069".
Orsi DL, Pook E, Bräuer N, Friberg A, Lienau P, Lemke CT, Stellfeld T, Brüggemeier U, Pütter V, Meyer H, Baco M, Tang S, Cherniack AD, Westlake L, Bender SA, Kocak M, Strathdee CA, Meyerson M, Eis K, Goldstein JT. Orsi DL, et al. Among authors: lemke ct. J Med Chem. 2023 Jan 12;66(1):1082. doi: 10.1021/acs.jmedchem.2c02002. Epub 2022 Dec 21. J Med Chem. 2023. PMID: 36542814 Free PMC article. No abstract available.
Discovery and Structure-Based Design of Potent Covalent PPARγ Inverse-Agonists BAY-4931 and BAY-0069.
Orsi DL, Pook E, Bräuer N, Friberg A, Lienau P, Lemke CT, Stellfeld T, Brüggemeier U, Pütter V, Meyer H, Baco M, Tang S, Cherniack AD, Westlake L, Bender SA, Kocak M, Strathdee CA, Meyerson M, Eis K, Goldstein JT. Orsi DL, et al. Among authors: lemke ct. J Med Chem. 2022 Nov 10;65(21):14843-14863. doi: 10.1021/acs.jmedchem.2c01379. Epub 2022 Oct 21. J Med Chem. 2022. PMID: 36270630 Free PMC article.
Structure-function analysis of the SHOC2-MRAS-PP1C holophosphatase complex.
Kwon JJ, Hajian B, Bian Y, Young LC, Amor AJ, Fuller JR, Fraley CV, Sykes AM, So J, Pan J, Baker L, Lee SJ, Wheeler DB, Mayhew DL, Persky NS, Yang X, Root DE, Barsotti AM, Stamford AW, Perry CK, Burgin A, McCormick F, Lemke CT, Hahn WC, Aguirre AJ. Kwon JJ, et al. Among authors: lemke ct. Nature. 2022 Sep;609(7926):408-415. doi: 10.1038/s41586-022-04928-2. Epub 2022 Jul 13. Nature. 2022. PMID: 35831509 Free PMC article.
Paralog knockout profiling identifies DUSP4 and DUSP6 as a digenic dependence in MAPK pathway-driven cancers.
Ito T, Young MJ, Li R, Jain S, Wernitznig A, Krill-Burger JM, Lemke CT, Monducci D, Rodriguez DJ, Chang L, Dutta S, Pal D, Paolella BR, Rothberg MV, Root DE, Johannessen CM, Parida L, Getz G, Vazquez F, Doench JG, Zamanighomi M, Sellers WR. Ito T, et al. Among authors: lemke ct. Nat Genet. 2021 Dec;53(12):1664-1672. doi: 10.1038/s41588-021-00967-z. Epub 2021 Dec 2. Nat Genet. 2021. PMID: 34857952
Structure of PDE3A-SLFN12 complex reveals requirements for activation of SLFN12 RNase.
Garvie CW, Wu X, Papanastasiou M, Lee S, Fuller J, Schnitzler GR, Horner SW, Baker A, Zhang T, Mullahoo JP, Westlake L, Hoyt SH, Toetzl M, Ranaghan MJ, de Waal L, McGaunn J, Kaplan B, Piccioni F, Yang X, Lange M, Tersteegen A, Raymond D, Lewis TA, Carr SA, Cherniack AD, Lemke CT, Meyerson M, Greulich H. Garvie CW, et al. Among authors: lemke ct. Nat Commun. 2021 Jul 16;12(1):4375. doi: 10.1038/s41467-021-24495-w. Nat Commun. 2021. PMID: 34272366 Free PMC article.
33 results