H. Koblish

发表

Discovery and cocrystal structure of benzodiazepinedione HDM2 antagonists that activate p53 in cells.

Maxwell D Cummings, B. Tomczuk, J. Spurlino, 2005, Journal of medicinal chemistry.

Hydroxyamidine Inhibitors of Indoleamine-2,3-dioxygenase Potently Suppress Systemic Tryptophan Catabolism and the Growth of IDO-Expressing Tumors

J. Fridman, H. Koblish, P. Scherle, 2010, Molecular Cancer Therapeutics.

INCB24360 (Epacadostat), a Highly Potent and Selective Indoleamine-2,3-dioxygenase 1 (IDO1) Inhibitor for Immuno-oncology

M. Bower, R. Wynn, Q. Wang, 2017, ACS medicinal chemistry letters.

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.

Parsaclisib Is a Next-Generation Phosphoinositide 3-Kinase δ Inhibitor with Reduced Hepatotoxicity and Potent Antitumor and Immunomodulatory Activities in Models of B-Cell Malignancy

H. Koblish, M. Stubbs, Q. Wang, 2020, The Journal of Pharmacology and Experimental Therapeutics.

The pan-PIM inhibitor INCB053914 displays potent synergy in combination with ruxolitinib in models of MPN.

L. Mazzacurati, H. Koblish, G. Reuther, 2019, Blood advances.

Preclinical characterization of INCB053914, a novel pan-PIM kinase inhibitor, alone and in combination with anticancer agents, in models of hematologic malignancies

R. Wynn, A. Margulis, H. Koblish, 2018, PloS one.

A Humanized Animal Model Predicts Clonal Evolution and Therapeutic Vulnerabilities in Myeloproliferative Neoplasms

Jared S. Fowles, H. Koblish, M. Stubbs, 2020, bioRxiv.

Selective inhibition of indoleamine 2 , 3-dioxygenase ( IDO 1 ) effectively regulates mediators of antitumor immunity

R. Wynn, Q. Wang, J. Fridman, 2010 .

Parsaclisib Is a Next-Generation PI3Kδ Inhibitor With Reduced Hepatotoxicity and Potent Antitumor and Immunomodulatory Activities in Models of B-Cell Malignancy a

Kathy, Qianqian Wang, H. Koblish, 2020 .

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.

Characterization of human cancer xenografts in humanized mice

H. Koblish, C. Stevens, J. Rios-Doria, 2020, Journal for ImmunoTherapy of Cancer.

The synthesis and SAR of 2-amino-pyrrolo[2,3-d]pyrimidines: a new class of Aurora-A kinase inhibitors.

H. Koblish, A. Maroney, Dana L. Johnson, 2006, Bioorganic & medicinal chemistry letters.

Novel 1,4-benzodiazepine-2,5-diones as Hdm2 antagonists with improved cellular activity.

Tianbao Lu, M. Player, J. Marugan, 2006, Bioorganic & medicinal chemistry letters.

Benzodiazepinedione inhibitors of the Hdm2:p53 complex suppress human tumor cell proliferation in vitro and sensitize tumors to doxorubicin in vivo

D. Parks, Tianbao Lu, J. Marugan, 2006, Molecular Cancer Therapeutics.

Structure-based design, synthesis, and biological evaluation of novel 1,4-diazepines as HDM2 antagonists.

Maxwell D Cummings, Mark R Player, D. Parks, 2005, Bioorganic & medicinal chemistry letters.

Treatment-Induced Tumor Cell Apoptosis and Secondary Necrosis Drive Tumor Progression in the Residual Tumor Microenvironment through MerTK and IDO1.

J. Balko, H. Koblish, P. Scherle, 2018, Cancer research.

Discovery of potent competitive inhibitors of indoleamine 2,3-dioxygenase with in vivo pharmacodynamic activity and efficacy in a mouse melanoma model.

Qian Wang, Michael Bower, Richard Wynn, 2009, Journal of medicinal chemistry.

Mechanism of tumor rejection with doublets of CTLA-4, PD-1/PD-L1, or IDO blockade involves restored IL-2 production and proliferation of CD8+ T cells directly within the tumor microenvironment

H. Koblish, P. Scherle, T. Gajewski, 2014, Journal of Immunotherapy for Cancer.

Immune Suppression by Recombinant Interleukin (rIL)-12 Involves Interferon γ Induction of Nitric Oxide Synthase 2 (iNOS) Activity: Inhibitors of NO Generation Reveal the Extent of rIL-12 Vaccine Adjuvant Effect

G. Trinchieri, C. Hunter, H. Koblish, 1998, The Journal of experimental medicine.

Selective inhibition of IDO1 effectively regulates mediators of antitumor immunity.

Qian Wang, Beth Thomas, Richard Wynn, 2010, Blood.

Progress in the Development of Agents to Control the Cell Cycle

H. Koblish, K. Moriarty, J. Dana, 2007 .

INCB040093 Is a Novel PI3Kδ Inhibitor for the Treatment of B Cell Lymphoid Malignancies

Jun Yu Li, Qianqian Wang, B. Rumberger, 2018, The Journal of Pharmacology and Experimental Therapeutics.

INCB054828 (pemigatinib), a potent and selective inhibitor of fibroblast growth factor receptors 1, 2, and 3, displays activity against genetically defined tumor models

R. Wynn, H. Koblish, Yue Zhang, 2020, PLoS ONE.

Abstract 2671: INCB050465, a novel PI3Kδ inhibitor, synergizes with PIM protein kinase inhibition to cause tumor regression in a model of DLBCL

H. Koblish, P. Scherle, T. Maduskuie, 2015 .

Enantiomerically pure 1,4-benzodiazepine-2,5-diones as Hdm2 antagonists.

Tianbao Lu, M. Player, J. Marugan, 2006, Bioorganic & medicinal chemistry letters.

Abstract 1761: Combination of a T cell activating immunotherapy with immune modulators alters the tumor microenvironment and promotes more effective tumor control in preclinical models

H. Koblish, P. Scherle, M. Stanford, 2018, Immunology.

Hematopoietic cytokines mediate resistance to targeted therapy in FLT3-ITD acute myeloid leukemia.

M. Carroll, H. Koblish, A. Perl, 2019, Blood advances.

Discovery of Potent and Selective Inhibitors of Wild-Type and Gatekeeper Mutant Fibroblast Growth Factor Receptor (FGFR) 2/3.

H. Koblish, M. Deller, R. Klabe, 2022, Journal of medicinal chemistry.

Stimulation of Platelet Production in Healthy Volunteers by a Novel Pegylated Peptide-Based Thrombopoietin (TPO) Receptor Agonist.

H. Koblish, C. Molloy, C. Franks, 2005 .

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

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

Hypoxia-mediated apoptosis from angiogenesis inhibition underlies tumor control by recombinant interleukin 12.

G. Trinchieri, C. Koch, W. T. Jenkins, 1999, Cancer research.

Dihydroquinone ansamycins: toward resolving the conflict between low in vitro affinity and high cellular potency of geldanamycin derivatives.

J. Marugan, H. Koblish, I. Deckman, 2006, Biochemistry.

Abstract 4904: The BET inhibitor INCB054329 enhances the activity of checkpoint modulation in syngeneic tumor models

H. Koblish, Yue Zhang, M. Stubbs, 2016 .

Enhanced pharmacokinetic properties of 1,4-benzodiazepine-2,5-dione antagonists of the HDM2-p53 protein-protein interaction through structure-based drug design.

Maxwell D Cummings, D. Parks, Tianbao Lu, 2006, Bioorganic & medicinal chemistry letters.

A Humanized Animal Model Predicts Clonal Evolution and Therapeutic Vulnerabilities in Myeloproliferative Neoplasms.

H. Koblish, M. Stubbs, Tiandao Li, 2021, Cancer discovery.

Discovery of Potent and Selective Inhibitors of Wild-Type and Gatekeeper Mutant Fibroblast Growth Factor Receptor (FGFR) 2/3

H. Koblish, M. Deller, R. Klabe, 2022, Journal of Medicinal Chemistry.

Abstract 2648: L-arginine regulates chemotherapy sensitivity via ER stress and autophagic pathways in arginine prototrophic cancer cells

H. Koblish, T. Burn, M. Covington, 2020 .

Treatment-Induced Tumor Cell Apoptosis and Secondary Necrosis Drive Tumor Progression in the Residual Tumor Microenvironment through MerTK and IDO1.

J. Balko, H. Koblish, P. Scherle, 2018, Cancer research.

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 .

Hydroxyamidine Inhibitors of Indoleamine-2,3-dioxygenase Potently Suppress Systemic Tryptophan Catabolism and the Growth of IDO-Expressing Tumors

J. Fridman, H. Koblish, P. Scherle, 2010, Molecular Cancer Therapeutics.

INCB040093 Is a Novel PI3Kδ Inhibitor for the Treatment of B Cell Lymphoid Malignancies

Jun Yu Li, Qianqian Wang, B. Rumberger, 2018, The Journal of Pharmacology and Experimental Therapeutics.

Characterization of INCB086550: A Potent and Novel Small-Molecule PD-L1 Inhibitor

R. Wynn, Yue Zhang, H. Koblish, 2022, Cancer discovery.

Abstract C103: The combination of PI3kδ-selective inhibition and immunomodulation shows efficacy in solid tumor models

H. Koblish, Yue Zhang, P. Scherle, 2015 .