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Page 1
Small-molecule WNK inhibition regulates cardiovascular and renal function.
Yamada K, Park HM, Rigel DF, DiPetrillo K, Whalen EJ, Anisowicz A, Beil M, Berstler J, Brocklehurst CE, Burdick DA, Caplan SL, Capparelli MP, Chen G, Chen W, Dale B, Deng L, Fu F, Hamamatsu N, Harasaki K, Herr T, Hoffmann P, Hu QY, Huang WJ, Idamakanti N, Imase H, Iwaki Y, Jain M, Jeyaseelan J, Kato M, Kaushik VK, Kohls D, Kunjathoor V, LaSala D, Lee J, Liu J, Luo Y, Ma F, Mo R, Mowbray S, Mogi M, Ossola F, Pandey P, Patel SJ, Raghavan S, Salem B, Shanado YH, Trakshel GM, Turner G, Wakai H, Wang C, Weldon S, Wielicki JB, Xie X, Xu L, Yagi YI, Yasoshima K, Yin J, Yowe D, Zhang JH, Zheng G, Monovich L. Yamada K, et al. Among authors: brocklehurst ce. Nat Chem Biol. 2016 Nov;12(11):896-898. doi: 10.1038/nchembio.2168. Epub 2016 Sep 5. Nat Chem Biol. 2016. PMID: 27595330
Development of autotaxin inhibitors: A series of zinc binding triazoles.
Thomson CG, Le Grand D, Dowling M, Brocklehurst CE, Chinn C, Elphick L, Faller M, Freeman M, Furminger V, Gasser C, Hamadi A, Hardaker E, Head V, Hill JC, Janus DI, Pearce D, Poulaud AS, Stanley E, Sviridenko L. Thomson CG, et al. Among authors: brocklehurst ce. Bioorg Med Chem Lett. 2018 Jul 15;28(13):2279-2284. doi: 10.1016/j.bmcl.2018.05.030. Epub 2018 May 21. Bioorg Med Chem Lett. 2018. PMID: 29798825
Building bridges.
Brocklehurst CE, Anderson EA. Brocklehurst CE, et al. Nat Chem. 2021 Oct;13(10):928-930. doi: 10.1038/s41557-021-00784-1. Nat Chem. 2021. PMID: 34584251 No abstract available.
Optimization of a Class of Dihydrobenzofurane Analogs toward Orally Efficacious YAP-TEAD Protein-Protein Interaction Inhibitors.
Sellner H, Chapeau E, Furet P, Voegtle M, Salem B, Le Douget M, Bordas V, Groell JM, Le Goff AL, Rouzet C, Wietlisbach T, Zimmermann T, McKenna J, Brocklehurst CE, Chène P, Wartmann M, Scheufler C, Kallen J, Williams G, Harlfinger S, Traebert M, Dumotier BM, Schmelzle T, Soldermann N. Sellner H, et al. Among authors: brocklehurst ce. ChemMedChem. 2023 Jun 1;18(11):e202300051. doi: 10.1002/cmdc.202300051. Epub 2023 Apr 13. ChemMedChem. 2023. PMID: 36988034
Calculation-assisted regioselective functionalization of the imidazo[1,2-a]pyrazine scaffold via zinc and magnesium organometallic intermediates.
Kastrati A, Kremsmair A, Sunagatullina AS, Korotenko V, Guersoy YC, Rout SK, Lima F, Brocklehurst CE, Karaghiosoff K, Zipse H, Knochel P. Kastrati A, et al. Among authors: brocklehurst ce. Chem Sci. 2023 Sep 28;14(40):11261-11266. doi: 10.1039/d3sc02893c. eCollection 2023 Oct 18. Chem Sci. 2023. PMID: 37860644 Free PMC article.
Discovery of Icenticaftor (QBW251), a Cystic Fibrosis Transmembrane Conductance Regulator Potentiator with Clinical Efficacy in Cystic Fibrosis and Chronic Obstructive Pulmonary Disease.
Grand DL, Gosling M, Baettig U, Bahra P, Bala K, Brocklehurst C, Budd E, Butler R, Cheung AK, Choudhury H, Collingwood SP, Cox B, Danahay H, Edwards L, Everatt B, Glaenzel U, Glotin AL, Groot-Kormelink P, Hall E, Hatto J, Howsham C, Hughes G, King A, Koehler J, Kulkarni S, Lightfoot M, Nicholls I, Page C, Pergl-Wilson G, Popa MO, Robinson R, Rowlands D, Sharp T, Spendiff M, Stanley E, Steward O, Taylor RJ, Tranter P, Wagner T, Watson H, Williams G, Wright P, Young A, Sandham DA. Grand DL, et al. J Med Chem. 2021 Jun 10;64(11):7241-7260. doi: 10.1021/acs.jmedchem.1c00343. Epub 2021 May 24. J Med Chem. 2021. PMID: 34028270
Reliable Functionalization of 5,6-Fused Bicyclic N-Heterocycles Pyrazolopyrimidines and Imidazopyridazines via Zinc and Magnesium Organometallics.
Kumar Rout S, Kastrati A, Jangra H, Schwärzer K, Sunagatullina AS, Garny M, Lima F, Brocklehurst CE, Karaghiosoff K, Zipse H, Knochel P. Kumar Rout S, et al. Among authors: brocklehurst ce. Chemistry. 2022 Jun 10;28(33):e202200733. doi: 10.1002/chem.202200733. Epub 2022 May 11. Chemistry. 2022. PMID: 35384103 Free PMC article.
18 results