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Page 1
Design and identification of selective HER-2 sheddase inhibitors via P1' manipulation and unconventional P2' perturbations to induce a molecular metamorphosis.
Yao W, Zhuo J, Burns DM, Li YL, Qian DQ, Zhang C, He C, Xu M, Shi E, Li Y, Marando CA, Covington MB, Yang G, Liu X, Pan M, Fridman JS, Scherle P, Wasserman ZR, Hollis G, Vaddi K, Yeleswaram S, Newton R, Friedman S, Metcalf B. Yao W, et al. Among authors: yang g. Bioorg Med Chem Lett. 2008 Jan 1;18(1):159-63. doi: 10.1016/j.bmcl.2007.10.108. Epub 2007 Nov 4. Bioorg Med Chem Lett. 2008. PMID: 18036818
Identification of ADAM10 as a major source of HER2 ectodomain sheddase activity in HER2 overexpressing breast cancer cells.
Liu PC, Liu X, Li Y, Covington M, Wynn R, Huber R, Hillman M, Yang G, Ellis D, Marando C, Katiyar K, Bradley J, Abremski K, Stow M, Rupar M, Zhuo J, Li YL, Lin Q, Burns D, Xu M, Zhang C, Qian DQ, He C, Sharief V, Weng L, Agrios C, Shi E, Metcalf B, Newton R, Friedman S, Yao W, Scherle P, Hollis G, Burn TC. Liu PC, et al. Among authors: yang g. Cancer Biol Ther. 2006 Jun;5(6):657-64. doi: 10.4161/cbt.5.6.2708. Epub 2006 Jun 14. Cancer Biol Ther. 2006. PMID: 16627989 Free article.
Conversion of an MMP-potent scaffold to an MMP-selective HER-2 sheddase inhibitor via scaffold hybridization and subtle P1' permutations.
Burns DM, He C, Li Y, Scherle P, Liu X, Marando CA, Covington MB, Yang G, Pan M, Turner S, Fridman JS, Hollis G, Vaddi K, Yeleswaram S, Newton R, Friedman S, Metcalf B, Yao W. Burns DM, et al. Among authors: yang g. Bioorg Med Chem Lett. 2008 Jan 15;18(2):560-4. doi: 10.1016/j.bmcl.2007.11.086. Epub 2007 Nov 28. Bioorg Med Chem Lett. 2008. PMID: 18068976
Selective inhibition of ADAM metalloproteases blocks HER-2 extracellular domain (ECD) cleavage and potentiates the anti-tumor effects of trastuzumab.
Liu X, Fridman JS, Wang Q, Caulder E, Yang G, Covington M, Liu C, Marando C, Zhuo J, Li Y, Yao W, Vaddi K, Newton RC, Scherle PA, Friedman SM. Liu X, et al. Among authors: yang g. Cancer Biol Ther. 2006 Jun;5(6):648-56. doi: 10.4161/cbt.5.6.2707. Epub 2006 Jun 14. Cancer Biol Ther. 2006. PMID: 16627988 Free article.
Targeting ADAM-mediated ligand cleavage to inhibit HER3 and EGFR pathways in non-small cell lung cancer.
Zhou BB, Peyton M, He B, Liu C, Girard L, Caudler E, Lo Y, Baribaud F, Mikami I, Reguart N, Yang G, Li Y, Yao W, Vaddi K, Gazdar AF, Friedman SM, Jablons DM, Newton RC, Fridman JS, Minna JD, Scherle PA. Zhou BB, et al. Among authors: yang g. Cancer Cell. 2006 Jul;10(1):39-50. doi: 10.1016/j.ccr.2006.05.024. Cancer Cell. 2006. PMID: 16843264 Free PMC article.
A novel kinase inhibitor, INCB28060, blocks c-MET-dependent signaling, neoplastic activities, and cross-talk with EGFR and HER-3.
Liu X, Wang Q, Yang G, Marando C, Koblish HK, Hall LM, Fridman JS, Behshad E, Wynn R, Li Y, Boer J, Diamond S, He C, Xu M, Zhuo J, Yao W, Newton RC, Scherle PA. Liu X, et al. Among authors: yang g. Clin Cancer Res. 2011 Nov 15;17(22):7127-38. doi: 10.1158/1078-0432.CCR-11-1157. Epub 2011 Sep 14. Clin Cancer Res. 2011. PMID: 21918175
Both 5-arylidene-2-thioxodihydropyrimidine-4,6(1H,5H)-diones and 3-thioxo-2,3-dihydro-1H-imidazo[1,5-a]indol-1-ones are light-dependent tumor necrosis factor-alpha antagonists.
Voss ME, Carter PH, Tebben AJ, Scherle PA, Brown GD, Thompson LA, Xu M, Lo YC, Yang G, Liu RQ, Strzemienski P, Everlof JG, Trzaskos JM, Decicco CP. Voss ME, et al. Among authors: yang g. Bioorg Med Chem Lett. 2003 Feb 10;13(3):533-8. doi: 10.1016/s0960-894x(02)00941-1. Bioorg Med Chem Lett. 2003. PMID: 12565966
INCB040093 Is a Novel PI3Kδ Inhibitor for the Treatment of B Cell Lymphoid Malignancies.
Shin N, Li YL, Mei S, Wang KH, Hall L, Katiyar K, Wang Q, Yang G, Rumberger B, Leffet L, He X, Rupar M, Bowman K, Favata M, Li J, Liu M, Li Y, Covington M, Koblish H, Soloviev M, Shuey D, Burn T, Diamond S, Fridman J, Combs A, Yao W, Yeleswaram S, Hollis G, Vaddi K, Huber R, Newton R, Scherle P. Shin N, et al. Among authors: yang g. J Pharmacol Exp Ther. 2018 Jan;364(1):120-130. doi: 10.1124/jpet.117.244947. Epub 2017 Nov 10. J Pharmacol Exp Ther. 2018. PMID: 29127109
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