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The Pharmacokinetic-Pharmacodynamic (PKPD) Relationships of AZD3229, a Novel and Selective Inhibitor of KIT, in a Range of Mouse Xenograft Models of GIST.
Pilla Reddy V, Anjum R, Grondine M, Smith A, Bhavsar D, Barry E, Guichard SM, Shao W, Kettle JG, Brown C, Banks E, Jones RDO. Pilla Reddy V, et al. Among authors: shao w. Clin Cancer Res. 2020 Jul 15;26(14):3751-3759. doi: 10.1158/1078-0432.CCR-19-2848. Epub 2020 Mar 27. Clin Cancer Res. 2020. PMID: 32220888
Inhibiting Tankyrases sensitizes KRAS-mutant cancer cells to MEK inhibitors via FGFR2 feedback signaling.
Schoumacher M, Hurov KE, Lehár J, Yan-Neale Y, Mishina Y, Sonkin D, Korn JM, Flemming D, Jones MD, Antonakos B, Cooke VG, Steiger J, Ledell J, Stump MD, Sellers WR, Danial NN, Shao W. Schoumacher M, et al. Among authors: shao w. Cancer Res. 2014 Jun 15;74(12):3294-305. doi: 10.1158/0008-5472.CAN-14-0138-T. Epub 2014 Apr 18. Cancer Res. 2014. PMID: 24747911
Tankyrase Inhibition Blocks Wnt/β-Catenin Pathway and Reverts Resistance to PI3K and AKT Inhibitors in the Treatment of Colorectal Cancer.
Arqués O, Chicote I, Puig I, Tenbaum SP, Argilés G, Dienstmann R, Fernández N, Caratù G, Matito J, Silberschmidt D, Rodon J, Landolfi S, Prat A, Espín E, Charco R, Nuciforo P, Vivancos A, Shao W, Tabernero J, Palmer HG. Arqués O, et al. Among authors: shao w. Clin Cancer Res. 2016 Feb 1;22(3):644-56. doi: 10.1158/1078-0432.CCR-14-3081. Epub 2015 Jul 29. Clin Cancer Res. 2016. PMID: 26224873
Antitumor Properties of RAF709, a Highly Selective and Potent Inhibitor of RAF Kinase Dimers, in Tumors Driven by Mutant RAS or BRAF.
Shao W, Mishina YM, Feng Y, Caponigro G, Cooke VG, Rivera S, Wang Y, Shen F, Korn JM, Mathews Griner LA, Nishiguchi G, Rico A, Tellew J, Haling JR, Aversa R, Polyakov V, Zang R, Hekmat-Nejad M, Amiri P, Singh M, Keen N, Dillon MP, Lees E, Ramurthy S, Sellers WR, Stuart DD. Shao W, et al. Cancer Res. 2018 Mar 15;78(6):1537-1548. doi: 10.1158/0008-5472.CAN-17-2033. Epub 2018 Jan 17. Cancer Res. 2018. PMID: 29343524
Discovery of N-(4-{[5-Fluoro-7-(2-methoxyethoxy)quinazolin-4-yl]amino}phenyl)-2-[4-(propan-2-yl)-1 H-1,2,3-triazol-1-yl]acetamide (AZD3229), a Potent Pan-KIT Mutant Inhibitor for the Treatment of Gastrointestinal Stromal Tumors.
Kettle JG, Anjum R, Barry E, Bhavsar D, Brown C, Boyd S, Campbell A, Goldberg K, Grondine M, Guichard S, Hardy CJ, Hunt T, Jones RDO, Li X, Moleva O, Ogg D, Overman RC, Packer MJ, Pearson S, Schimpl M, Shao W, Smith A, Smith JM, Stead D, Stokes S, Tucker M, Ye Y. Kettle JG, et al. Among authors: shao w. J Med Chem. 2018 Oct 11;61(19):8797-8810. doi: 10.1021/acs.jmedchem.8b00938. Epub 2018 Sep 24. J Med Chem. 2018. PMID: 30204441
Design and Discovery of N-(3-(2-(2-Hydroxyethoxy)-6-morpholinopyridin-4-yl)-4-methylphenyl)-2-(trifluoromethyl)isonicotinamide, a Selective, Efficacious, and Well-Tolerated RAF Inhibitor Targeting RAS Mutant Cancers: The Path to the Clinic.
Ramurthy S, Taft BR, Aversa RJ, Barsanti PA, Burger MT, Lou Y, Nishiguchi GA, Rico A, Setti L, Smith A, Subramanian S, Tamez V, Tanner H, Wan L, Hu C, Appleton BA, Mamo M, Tandeske L, Tellew JE, Huang S, Yue Q, Chaudhary A, Tian H, Iyer R, Hassan AQ, Mathews Griner LA, La Bonte LR, Cooke VG, Van Abbema A, Merritt H, Gampa K, Feng F, Yuan J, Mishina Y, Wang Y, Haling JR, Vaziri S, Hekmat-Nejad M, Polyakov V, Zang R, Sethuraman V, Amiri P, Singh M, Sellers WR, Lees E, Shao W, Dillon MP, Stuart DD. Ramurthy S, et al. Among authors: shao w. J Med Chem. 2020 Mar 12;63(5):2013-2027. doi: 10.1021/acs.jmedchem.9b00161. Epub 2019 May 16. J Med Chem. 2020. PMID: 31059256
AZD4573 Is a Highly Selective CDK9 Inhibitor That Suppresses MCL-1 and Induces Apoptosis in Hematologic Cancer Cells.
Cidado J, Boiko S, Proia T, Ferguson D, Criscione SW, San Martin M, Pop-Damkov P, Su N, Roamio Franklin VN, Sekhar Reddy Chilamakuri C, D'Santos CS, Shao W, Saeh JC, Koch R, Weinstock DM, Zinda M, Fawell SE, Drew L. Cidado J, et al. Among authors: shao w. Clin Cancer Res. 2020 Feb 15;26(4):922-934. doi: 10.1158/1078-0432.CCR-19-1853. Epub 2019 Nov 7. Clin Cancer Res. 2020. PMID: 31699827
Discovery and pharmacological characterization of AZD3229, a potent KIT/PDGFRα inhibitor for treatment of gastrointestinal stromal tumors.
Banks E, Grondine M, Bhavsar D, Barry E, Kettle JG, Reddy VP, Brown C, Wang H, Mettetal JT, Collins T, Adeyemi O, Overman R, Lawson D, Harmer AR, Reimer C, Drew L, Packer MJ, Cosulich S, Jones RD, Shao W, Wilson D, Guichard S, Fawell S, Anjum R. Banks E, et al. Among authors: shao w. Sci Transl Med. 2020 Apr 29;12(541):eaaz2481. doi: 10.1126/scitranslmed.aaz2481. Sci Transl Med. 2020. PMID: 32350132
Discovery of AZD4573, a Potent and Selective Inhibitor of CDK9 That Enables Short Duration of Target Engagement for the Treatment of Hematological Malignancies.
Barlaam B, Casella R, Cidado J, Cook C, De Savi C, Dishington A, Donald CS, Drew L, Ferguson AD, Ferguson D, Glossop S, Grebe T, Gu C, Hande S, Hawkins J, Hird AW, Holmes J, Horstick J, Jiang Y, Lamb ML, McGuire TM, Moore JE, O'Connell N, Pike A, Pike KG, Proia T, Roberts B, San Martin M, Sarkar U, Shao W, Stead D, Sumner N, Thakur K, Vasbinder MM, Varnes JG, Wang J, Wang L, Wu D, Wu L, Yang B, Yao T. Barlaam B, et al. Among authors: shao w. J Med Chem. 2020 Dec 24;63(24):15564-15590. doi: 10.1021/acs.jmedchem.0c01754. Epub 2020 Dec 11. J Med Chem. 2020. PMID: 33306391
2,401 results