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Page 1
Discovery of (2R,4R)-4-((S)-2-Amino-3-methylbutanamido)-2-(4-boronobutyl)pyrrolidine-2-carboxylic Acid (AZD0011), an Actively Transported Prodrug of a Potent Arginase Inhibitor to Treat Cancer.
Mlynarski SN, Aquila BM, Cantin S, Cook S, Doshi A, Finlay MRV, Gangl ET, Grebe T, Gu C, Kawatkar SP, Petersen J, Pop-Damkov P, Schuller AG, Shao W, Shields JD, Simpson I, Tavakoli S, Tentarelli S, Throner S, Wang H, Wang J, Wu D, Ye Q. Mlynarski SN, et al. Among authors: tentarelli s. J Med Chem. 2024 Nov 21. doi: 10.1021/acs.jmedchem.4c02309. Online ahead of print. J Med Chem. 2024. PMID: 39572889
Design and Synthesis of Acyclic Boronic Acid Arginase Inhibitors.
Shields JD, Aquila BM, Emmons D, Finlay MRV, Gangl ET, Gu C, Mlynarski SN, Petersen J, Pop-Damkov P, Sha L, Simpson I, Tavakoli S, Tentarelli S, Wang H, Ye Q, Zheng X. Shields JD, et al. Among authors: tentarelli s. J Med Chem. 2024 Nov 14. doi: 10.1021/acs.jmedchem.4c02295. Online ahead of print. J Med Chem. 2024. PMID: 39540340
Optimization of Potent, Efficacious, Selective and Blood-Brain Barrier Penetrating Inhibitors Targeting EGFR Exon20 Insertion Mutations.
Thomson C, Braybrooke E, Colclough N, Davies NL, Floc'h N, Greenwood R, Guérot C, Hargreaves D, Johnstrom P, Khurana P, Kostomiris DH, Li S, Lister A, Lorthioir O, Martin S, McCoull W, McLean NJ, McWilliams L, Orme JP, Packer MJ, Pearson S, Swaih AM, Tentarelli S, Tucker MJ, Ward RA, Wilkinson S, Winlow P, Wood IL. Thomson C, et al. Among authors: tentarelli s. J Med Chem. 2024 Sep 28. doi: 10.1021/acs.jmedchem.4c01792. Online ahead of print. J Med Chem. 2024. PMID: 39340451
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: tentarelli s. 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
Novel Arginase Inhibitor, AZD0011, Demonstrates Immune Cell Stimulation and Antitumor Efficacy with Diverse Combination Partners.
Doshi AS, Cantin S, Hernandez M, Srinivasan S, Tentarelli S, Griffin M, Wang Y, Pop-Damkov P, Prickett LB, Kankkonen C, Shen M, Martin MS, Wu S, Castaldi MP, Ghadially H, Varnes J, Gales S, Henry D, Hoover C, Mele DA, Simpson I, Gangl ET, Mlynarski SN, Finlay MRV, Drew L, Fawell SE, Shao W, Schuller AG. Doshi AS, et al. Among authors: tentarelli s. Mol Cancer Ther. 2023 May 4;22(5):630-645. doi: 10.1158/1535-7163.MCT-22-0431. Mol Cancer Ther. 2023. PMID: 36912782
Optimization of an Imidazo[1,2-a]pyridine Series to Afford Highly Selective Type I1/2 Dual Mer/Axl Kinase Inhibitors with In Vivo Efficacy.
McCoull W, Boyd S, Brown MR, Coen M, Collingwood O, Davies NL, Doherty A, Fairley G, Goldberg K, Hardaker E, He G, Hennessy EJ, Hopcroft P, Hodgson G, Jackson A, Jiang X, Karmokar A, Lainé AL, Lindsay N, Mao Y, Markandu R, McMurray L, McLean N, Mooney L, Musgrove H, Nissink JWM, Pflug A, Reddy VP, Rawlins PB, Rivers E, Schimpl M, Smith GF, Tentarelli S, Travers J, Troup RI, Walton J, Wang C, Wilkinson S, Williamson B, Winter-Holt J, Yang D, Zheng Y, Zhu Q, Smith PD. McCoull W, et al. Among authors: tentarelli s. J Med Chem. 2021 Sep 23;64(18):13524-13539. doi: 10.1021/acs.jmedchem.1c00920. Epub 2021 Sep 3. J Med Chem. 2021. PMID: 34478292
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: tentarelli s. 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.
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