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Page 1
Development of a Series of Pyrrolopyridone MAT2A Inhibitors.
Atkinson SJ, Bagal SK, Argyrou A, Askin S, Cheung T, Chiarparin E, Coen M, Collie IT, Dale IL, De Fusco C, Dillman K, Evans L, Feron LJ, Foster AJ, Grondine M, Kantae V, Lamont GM, Lamont S, Lynch JT, Nilsson Lill S, Robb GR, Saeh J, Schimpl M, Scott JS, Smith J, Srinivasan B, Tentarelli S, Vazquez-Chantada M, Wagner D, Walsh JJ, Watson D, Williamson B. Atkinson SJ, et al. Among authors: vazquez chantada m. J Med Chem. 2024 Mar 28;67(6):4541-4559. doi: 10.1021/acs.jmedchem.3c01860. Epub 2024 Mar 11. J Med Chem. 2024. PMID: 38466661
Discovery and In Vivo Efficacy of AZ-PRMT5i-1, a Novel PRMT5 Inhibitor with High MTA Cooperativity.
Smith JM, Barlaam B, Beattie D, Bradshaw L, Chan HM, Chiarparin E, Collingwood O, Cooke SL, Cronin A, Cumming I, Dean E, Debreczeni JÉ, Del Barco Barrantes I, Diene C, Gianni D, Guerot C, Guo X, Guven S, Hayhow TG, Hong T, Kemmitt PD, Lamont GM, Lamont S, Lynch JT, McWilliams L, Moore S, Raubo P, Robb GR, Robinson J, Scott JS, Srinivasan B, Steward O, Stubbs CJ, Syson K, Tan L, Turner O, Underwood E, Urosevic J, Vazquez-Chantada M, Whittaker AL, Wilson DM, Winter-Holt JJ. Smith JM, et al. Among authors: vazquez chantada m. J Med Chem. 2024 Aug 22;67(16):13604-13638. doi: 10.1021/acs.jmedchem.4c00097. Epub 2024 Jul 30. J Med Chem. 2024. PMID: 39080842
Impaired Function of Solute Carrier Family 19 Leads to Low Folate Levels and Lipid Droplet Accumulation in Hepatocytes.
Cano A, Vazquez-Chantada M, Conde-Vancells J, Gonzalez-Lahera A, Mosen-Ansorena D, Blanco FJ, Clément K, Aron-Wisnewsky J, Tran A, Gual P, García-Monzón C, Caballería J, Castro A, Martínez-Chantar ML, Mato JM, Zhu H, Finnell RH, Aransay AM. Cano A, et al. Among authors: vazquez chantada m. Biomedicines. 2023 Jan 31;11(2):337. doi: 10.3390/biomedicines11020337. Biomedicines. 2023. PMID: 36830876 Free PMC article.
Targeting DNA damage response components induces enhanced STING-dependent type-I IFN response in ATM deficient cancer cells and drives dendritic cell activation.
Lopez-Pelaez M, Young L, Vazquez-Chantada M, Nelson N, Durant S, Wilkinson RW, Poon E, Gaspar M, Valge-Archer V, Smith P, Dovedi SJ. Lopez-Pelaez M, et al. Among authors: vazquez chantada m. Oncoimmunology. 2022 Sep 13;11(1):2117321. doi: 10.1080/2162402X.2022.2117321. eCollection 2022. Oncoimmunology. 2022. PMID: 36117525 Free PMC article.
Optimization of hERG and Pharmacokinetic Properties for Basic Dihydro-8H-purin-8-one Inhibitors of DNA-PK.
Goldberg FW, Ting AKT, Beattie D, Lamont GM, Fallan C, Finlay MRV, Williamson B, Schimpl M, Harmer AR, Adeyemi OB, Nordell P, Cronin AS, Vazquez-Chantada M, Barratt D, Ramos-Montoya A, Cadogan EB, Davies BR. Goldberg FW, et al. Among authors: vazquez chantada m. ACS Med Chem Lett. 2022 Jul 7;13(8):1295-1301. doi: 10.1021/acsmedchemlett.2c00172. eCollection 2022 Aug 11. ACS Med Chem Lett. 2022. PMID: 35978693 Free PMC article.
Fragment-Based Design of a Potent MAT2a Inhibitor and in Vivo Evaluation in an MTAP Null Xenograft Model.
De Fusco C, Schimpl M, Börjesson U, Cheung T, Collie I, Evans L, Narasimhan P, Stubbs C, Vazquez-Chantada M, Wagner DJ, Grondine M, Sanders MG, Tentarelli S, Underwood E, Argyrou A, Smith JM, Lynch JT, Chiarparin E, Robb G, Bagal SK, Scott JS. De Fusco C, et al. Among authors: vazquez chantada m. J Med Chem. 2021 May 27;64(10):6814-6826. doi: 10.1021/acs.jmedchem.1c00067. Epub 2021 Apr 26. J Med Chem. 2021. PMID: 33900758 Free article.
Bicyclic β-Sheet Mimetics that Target the Transcriptional Coactivator β-Catenin and Inhibit Wnt Signaling.
Wendt M, Bellavita R, Gerber A, Efrém NL, van Ramshorst T, Pearce NM, Davey PRJ, Everard I, Vazquez-Chantada M, Chiarparin E, Grieco P, Hennig S, Grossmann TN. Wendt M, et al. Among authors: vazquez chantada m. Angew Chem Int Ed Engl. 2021 Jun 14;60(25):13937-13944. doi: 10.1002/anie.202102082. Epub 2021 May 5. Angew Chem Int Ed Engl. 2021. PMID: 33783110 Free PMC article.
A protein tertiary structure mimetic modulator of the Hippo signalling pathway.
Adihou H, Gopalakrishnan R, Förster T, Guéret SM, Gasper R, Geschwindner S, Carrillo García C, Karatas H, Pobbati AV, Vazquez-Chantada M, Davey P, Wassvik CM, Pang JKS, Soh BS, Hong W, Chiarparin E, Schade D, Plowright AT, Valeur E, Lemurell M, Grossmann TN, Waldmann H. Adihou H, et al. Among authors: vazquez chantada m. Nat Commun. 2020 Oct 27;11(1):5425. doi: 10.1038/s41467-020-19224-8. Nat Commun. 2020. PMID: 33110077 Free PMC article.
The Discovery of 7-Methyl-2-[(7-methyl[1,2,4]triazolo[1,5-a]pyridin-6-yl)amino]-9-(tetrahydro-2H-pyran-4-yl)-7,9-dihydro-8H-purin-8-one (AZD7648), a Potent and Selective DNA-Dependent Protein Kinase (DNA-PK) Inhibitor.
Goldberg FW, Finlay MRV, Ting AKT, Beattie D, Lamont GM, Fallan C, Wrigley GL, Schimpl M, Howard MR, Williamson B, Vazquez-Chantada M, Barratt DG, Davies BR, Cadogan EB, Ramos-Montoya A, Dean E. Goldberg FW, et al. Among authors: vazquez chantada m. J Med Chem. 2020 Apr 9;63(7):3461-3471. doi: 10.1021/acs.jmedchem.9b01684. Epub 2020 Jan 15. J Med Chem. 2020. PMID: 31851518
30 results