Chunhong He

发表

A Novel Kinase Inhibitor, INCB28060, Blocks c-MET–Dependent Signaling, Neoplastic Activities, and Cross-Talk with EGFR and HER-3

Qian Wang, Yu Li, Richard Wynn, 2011, Clinical Cancer Research.

Discovery of 1'-(1-phenylcyclopropane-carbonyl)-3H-spiro[isobenzofuran-1,3'-pyrrolidin]-3-one as a novel steroid mimetic scaffold for the potent and tissue-specific inhibition of 11β-HSD1 using a scaffold-hopping approach.

R. Wynn, P. Scherle, K. Vaddi, 2022, Bioorganic & medicinal chemistry letters.

A Potent and Selective Dual Inhibitor of AXL and MERTK Possesses Both Immunomodulatory and Tumor-Targeted Activity

R. Wynn, H. Koblish, X. Wen, 2020, Frontiers in Oncology.

Abstract 3759: Characterization of INCB081776, a potent and selective dual AXL/MER kinase inhibitor

R. Wynn, X. Liu, H. Koblish, 2018, Immunology.

INCB050465 (Parsaclisib), a Novel Next-Generation Inhibitor of Phosphoinositide 3-Kinase Delta (PI3Kδ).

H. Koblish, P. Scherle, T. Maduskuie, 2019, ACS medicinal chemistry letters.

Discovery of a novel 2-spiro-proline steroid mimetic scaffold for the potent inhibition of 11β-HSD1.

R. Wynn, P. Scherle, Yanlong Li, 2022, Bioorganic & medicinal chemistry letters.

Discovery of Novel Pyrazolopyrimidines as Potent, Selective, and Orally Bioavailable Inhibitors of ALK2.

M. Covington, S. Diamond, S. Yeleswaram, 2022, ACS medicinal chemistry letters.

Identification of ADAM10 as a major source of HER2 ectodomain sheddase activity in HER2 overexpressing breast cancer cells

R. Wynn, P. Scherle, Phillip C. C. Liu, 2006, Cancer biology & therapy.

Compelling P1 substituent affect on metalloprotease binding profile enables the design of a novel cyclohexyl core scaffold with excellent MMP selectivity and HER-2 sheddase inhibition.

R. Wynn, J. Fridman, P. Scherle, 2009, Bioorganic & Medicinal Chemistry Letters.

Conversion of an MMP-potent scaffold to an MMP-selective HER-2 sheddase inhibitor via scaffold hybridization and subtle P1' permutations.

J. Fridman, P. Scherle, K. Vaddi, 2008, Bioorganic & medicinal chemistry letters.

Discovery of Pemigatinib: A Potent and Selective Fibroblast Growth Factor Receptor (FGFR) Inhibitor.

R. Wynn, H. Koblish, Yue Zhang, 2021, Journal of medicinal chemistry.

Design and identification of selective HER-2 sheddase inhibitors via P1' manipulation and unconventional P2' perturbations to induce a molecular metamorphosis.

J. Fridman, P. Scherle, K. Vaddi, 2008, Bioorganic & medicinal chemistry letters.

Discovery of a potent, selective, and orally active human epidermal growth factor receptor-2 sheddase inhibitor for the treatment of cancer.

M. Bower, R. Wynn, J. Fridman, 2007, Journal of medicinal chemistry.

Abstract 4712: Discovery of INCB059872, a novel FAD-directed LSD1 inhibitor that is effective in preclinical models of human and murine AML

R. Wynn, A. Margulis, X. Liu, 2016 .

Abstract 1162: The evaluation of INCB059872, an FAD-directed covalent inhibitor of LSD1, in preclinical models of Ewing sarcoma

R. Wynn, X. Liu, P. Scherle, 2017 .

Abstract 2032: Combination of epigenetic regulation via LSD1 inhibition with signal transduction inhibitors significantly enhances anti-tumor activity in models of hematologic malignancies

R. Wynn, H. Koblish, X. Wen, 2017 .

Discovery of 1'-(1-phenylcyclopropane-carbonyl)-3H-spiro[isobenzofuran-1,3'-pyrrolidin]-3-one as a novel steroid mimetic scaffold for the potent and tissue-specific inhibition of 11β-HSD1 using a scaffold-hopping approach.

R. Wynn, P. Scherle, K. Vaddi, 2022, Bioorganic & medicinal chemistry letters.