R. Newton

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Clinical Benefit of INCB7839, a Potent and Selective Inhibitor of ADAM10 and ADAM17, in Combination with Trastuzumab in Metastatic HER2 Positive Breast Cancer Patients.

D. Doval, S. Nag, G. Bhattacharyya, 2009 .

Discovery of γ-Lactam Hydroxamic Acids as Selective Inhibitors of Tumor Necrosis Factor α Converting Enzyme: Design, Synthesis, and Structure−Activity Relationships

Chen Lihua, Zelda R. Wasserman, Karl D. Hardman, 2002 .

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.

Abstract CT085: Pharmacodynamic correlates in a phase I study of INCMGA00012, a PD-1 antagonistic monoclonal antibody

P. Moore, T. Condamine, R. Newton, 2019, Clinical Trials.

Induction of aggrecanase 1 (ADAM-TS4) by interleukin-1 occurs through activation of constitutively produced protein.

P. Scherle, Gengjie Yang, R. Newton, 2003, Arthritis and rheumatism.

Preliminary results from a phase 1/2 study of INCB024360 combined with ipilimumab (ipi) in patients (pts) with melanoma.

G. Gibney, P. Scherle, O. Hamid, 2014 .

Pharmacokinetics and Pharmacodynamics of DPC 333 ((2R)-2-((3R)-3-Amino-3{4-[2-methyl-4-quinolinyl) methoxy] phenyl}-2-oxopyrrolidinyl)-N-hydroxy-4-methylpentanamide)), a Potent and Selective Inhibitor of Tumor Necrosis Factor α-Converting Enzyme in Rodents, Dogs, Chimpanzees, and Humans

J. Trzăskos, T. Maduskuie, C. Garner, 2007, Drug Metabolism and Disposition.

Phase 2 study of the JAK kinase inhibitor ruxolitinib in patients with refractory leukemias, including postmyeloproliferative neoplasm acute myeloid leukemia.

Z. Estrov, H. Kantarjian, J. Cortes, 2012, Blood.

Discovery of N-hydroxy-2-(2-oxo-3-pyrrolidinyl)acetamides as potent and selective inhibitors of tumor necrosis factor-alpha converting enzyme (TACE).

R. Magolda, J. Trzăskos, M. Covington, 2003, Bioorganic & medicinal chemistry letters.

Identification and Characterization of INCB 9471 , an Allosteric Noncompetitive Small-Molecule Antagonist of C-C Chemokine Receptor 5 with Potent Inhibitory Activity against Monocyte Migration and HIV-1 Infection

P. Scherle, N. Zhou, F. Baribaud, 2011 .

Identification and Characterization of INCB9471, an Allosteric Noncompetitive Small-Molecule Antagonist of C-C Chemokine Receptor 5 with Potent Inhibitory Activity against Monocyte Migration and HIV-1 Infection

P. Scherle, N. Zhou, F. Baribaud, 2011, Journal of Pharmacology and Experimental Therapeutics.

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.

Selective JAK inhibition proves efficacious in epithelial cancer models

J. Fridman, Jun Li, X. Wen, 2008 .

The IDO1 selective inhibitor epacadostat enhances dendritic cell immunogenicity and lytic ability of tumor antigen-specific T cells

M. Brechbiel, J. Schlom, R. Madan, 2016, Oncotarget.

Internalization and nuclear localization of interleukin 1 are not sufficient for function.

A. Heguy, C. Baldari, M. Melli, 1991, Cell growth & differentiation : the molecular biology journal of the American Association for Cancer Research.

Aggrecanase: A Target for the Design of Inhibitors of Cartilage Degradation

R. Magolda, J. Trzăskos, C. Decicco, 1999, Annals of the New York Academy of Sciences.

Design and synthesis of a series of (2R)-N(4)-hydroxy-2-(3-hydroxybenzyl)-N(1)- [(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]butanediamide derivatives as potent, selective, and orally bioavailable aggrecanase inhibitors.

R. Magolda, M. Covington, C. Decicco, 2001, Journal of medicinal chemistry.

Characterization of human aggrecanase 2 (ADAM-TS5): substrate specificity studies and comparison with aggrecanase 1 (ADAM-TS4).

T. Burn, R. Newton, M. Tortorella, 2002, Matrix biology : journal of the International Society for Matrix Biology.

Potent P1' biphenylmethyl substituted aggrecanase inhibitors.

M. Covington, C. Decicco, R. Wexler, 2002, Bioorganic & medicinal chemistry letters.

The chemokine factsbook

K. Vaddi, R. Newton, M. Keller, 1997 .

Discovery of INCB3284, a Potent, Selective, and Orally Bioavailable hCCR2 Antagonist.

P. Scherle, K. Vaddi, M. Covington, 2011, ACS medicinal chemistry letters.

First-in-Human Phase I Study of the Oral Inhibitor of Indoleamine 2,3-Dioxygenase-1 Epacadostat (INCB024360) in Patients with Advanced Solid Malignancies

P. O'dwyer, P. Scherle, T. Gajewski, 2017, Clinical Cancer Research.

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

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

Discovery of CC chemokine receptor-3 (CCR3) antagonists with picomolar potency.

G. Trainor, M. Covington, C. Decicco, 2005, Journal of medicinal chemistry.

Cutting edge: a dominant negative form of TNF-alpha converting enzyme inhibits proTNF and TNFRII secretion.

G. Wu, R. Newton, K. Solomon, 1999, Journal of immunology.

Clinicogenomic analysis of FGFR2-rearranged cholangiocarcinoma identifies correlates of response and mechanisms of resistance to pemigatinib.

D. Melisi, T. Burn, I. Silverman, 2020, Cancer discovery.

Pharmacodynamic assessment of INCB024360, an inhibitor of indoleamine 2,3-dioxygenase 1 (IDO1), in advanced cancer patients.

P. O'dwyer, P. Scherle, T. Gajewski, 2012 .

Phase I study of the safety, pharmacokinetics (PK), and pharmacodynamics (PD) of the oral inhibitor of indoleamine 2,3-dioxygenase (IDO1) INCB024360 in patients (pts) with advanced malignancies.

P. O'dwyer, T. Gajewski, L. Leopold, 2013 .

Modification of tumor necrosis factor-α (TNF-α) production by the Na+-dependent HCO3− cotransport in lipopolysaccharide-activated human monocytes

R. Newton, U. Orlinska, 1995 .

CC chemokine receptor-3 (CCR3) antagonists: improving the selectivity of DPC168 by reducing central ring lipophilicity.

I. Kariv, K. Vaddi, M. Covington, 2007, Bioorganic & medicinal chemistry letters.

High-level expression in Escherichia coli of a soluble and fully active recombinant interleukin-1 beta.

Y. Lin, M. Covington, R. Newton, 1987, Molecular biology & medicine.

ADAM17 cleaves CD16b (FcγRIIIb) in human neutrophils.

R. Newton, Yue Wang, Jianming Wu, 2013, Biochimica et biophysica acta.

Type I interleukin-1 receptors in the mouse brain-endocrine-immune axis labelled with [125I]recombinant human interleukin-1 receptor antagonist

T. Takao, R. Newton, S. Culp, 1992, Journal of Neuroimmunology.

Selective Inhibition of Eosinophil Influx into the Lung by Small Molecule CC Chemokine Receptor 3 Antagonists in Mouse Models of Allergic Inflammation

K. McIntyre, S. Mandlekar, J. Trzăskos, 2006, Journal of Pharmacology and Experimental Therapeutics.

Discovery of BRL 50481, a Selective Inhibitor of Phosphodiesterase 7: In vitro Studies in Human Monocytes, Lung Macrophages and CD8 + T-Lymphocytes

A. Nicholson, L. Donnelly, Susan J. Smith, 2004 .

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 .

Clinical benefit of INCB7839, a potent and selective ADAM inhibitor, in combination with trastuzumab in patients with metastatic HER2+ breast cancer.

D. Doval, D. Lokanatha, P. Julka, 2010 .

A randomized, double-blind, placebo-controlled, dose-escalation study of the safety and efficacy of INCB039110, an oral janus kinase 1 inhibitor, in patients with stable, chronic plaque psoriasis

Haifeng Zhang, A. Menter, P. Scherle, 2016, The Journal of dermatological treatment.

Activation and distribution of inflammatory cells in the mouse uterus during the preimplantation period.

S. Dey, G. Andrews, R. Newton, 1992, Journal of immunology.

Identification of soluble interleukin-1 binding protein in cell-free supernatants. Evidence for soluble interleukin-1 receptor.

R. Horuk, J. Giri, R. Newton, 1990, The Journal of biological chemistry.

Selective Inhibition of JAK1 and JAK2 Is Efficacious in Rodent Models of Arthritis: Preclinical Characterization of INCB028050

J. Fridman, Jun Li, X. Wen, 2010, The Journal of Immunology.

Selective Inhibition of JAK 1 and JAK 2 Is Efficacious in Rodent Models of Arthritis : Preclinical Characterization of INCB 028050

J. Fridman, Jun Li, X. Wen, 2010 .

Preclinical Characterization of INCB 028050 Efficacious in Rodent Models of Arthritis : Selective Inhibition of JAK 1 and JAK 2 Is

J. Fridman, Jun Li, X. Wen, 2010 .

CCR3 antagonists: a potential new therapy for the treatment of asthma. Discovery and structure-activity relationships.

G. Trainor, M. Covington, C. Decicco, 2002, Bioorganic & medicinal chemistry letters.

INCB38579, a novel and potent histamine H₄ receptor small molecule antagonist with anti-inflammatory pain and anti-pruritic functions.

P. Scherle, L. Leffet, Yanlong Li, 2012, European journal of pharmacology.

Preclinical characterization of itacitinib (INCB039110), a novel selective inhibitor of JAK1, for the treatment of inflammatory diseases.

Jun Yu Li, M. Favata, P. Scherle, 2020, European journal of pharmacology.

Biological responses to C-C chemokines.

K. Vaddi, R. Newton, 1997, Methods in enzymology.

Alpha,Beta-cyclic-beta-benzamido hydroxamic acids: Novel oxaspiro[4.4]nonane templates for the discovery of potent, selective, orally bioavailable inhibitors of tumor necrosis factor-alpha converting enzyme (TACE).

J. Trzăskos, W. Marshall, K. Vaddi, 2008, Bioorganic & medicinal chemistry letters.

The Clinical Phenotype of Myelofibrosis Encompasses a Chronic Inflammatory State That Is Favorably Altered by INCB018424, a Selective Inhibitor of JAK1/2

H. Kantarjian, S. Verstovsek, R. Mesa, 2008 .

MIG – Monokine induced by interferon gamma

K. Vaddi, R. Newton, M. Keller, 1997 .

Quantitation of related proteins by Western blot analysis.

R. Newton, J. Uhl, 1988, Journal of immunological methods.

Comprehensive genomic profiling in FIGHT-202 reveals the landscape of actionable alterations in advanced cholangiocarcinoma.

G. Frampton, T. Burn, I. Silverman, 2019, Journal of Clinical Oncology.

Design, synthesis, and structure-activity relationships of macrocyclic hydroxamic acids that inhibit tumor necrosis factor alpha release in vitro and in vivo.

D. J. Nelson, K. D. Hardman, R. Copeland, 2001, Journal of medicinal chemistry.

Preclinical evaluation of local JAK1 and JAK2 inhibition in cutaneous inflammation.

J. Fridman, P. Scherle, C. Neilan, 2011, The Journal of investigative dermatology.

An ELISA assay for murine interleukin-1β

A. J. Daulerio, R. Newton, R. Dowling, 1993 .

Genetic and cellular aspects of the immune response of mice to highly substituted dinitrophenylated gamma globulin

R. Newton, 1978 .

Potent and selective aggrecanase inhibitors containing cyclic P1 substituents.

R. Magolda, J. Trzăskos, M. Covington, 2003, Bioorganic & medicinal chemistry letters.

Purification and cloning of aggrecanase-1: a member of the ADAMTS family of proteins.

R. Wynn, R. Copeland, R. Wynn, 1999, Science.

The Total Chemical Synthesis of Monocyte Chemotactic Protein‐1 (MCP‐1)

M. Covington, R. Newton, Angus R. Brown, 1996, Journal of peptide science : an official publication of the European Peptide Society.

Regulation of monocyte integrin expression by beta-family chemokines.

K. Vaddi, R. Newton, 1994, Journal of immunology.

Comparison of biological responses of human monocytes and THP‐1 cells to chemokines of the intercrine‐β family

K. Vaddi, R. Newton, 1994, Journal of leukocyte biology.

Species differences in [125I]interleukin-1 binding in brain, endocrine and immune tissues

T. Takao, R. Newton, E. Souza, 1993, Brain Research.

Discovery of INCB9471, a Potent, Selective, and Orally Bioavailable CCR5 Antagonist with Potent Anti-HIV-1 Activity.

P. Scherle, K. Vaddi, Joseph Glenn, 2010, ACS medicinal chemistry letters.

The production of human interleukin-1 beta by blood monocytes.

R. Newton, 1990, Progress in clinical and biological research.

The immune response of inbred mouse strains to DNP-BGG

C. Warner, R. Newton, 1977, Immunogenetics.

2,4-Disubstituted piperidines as selective CC chemokine receptor 3 (CCR3) antagonists: synthesis and selectivity.

G. Trainor, M. Covington, C. Decicco, 2006, Bioorganic & medicinal chemistry letters.

Discovery of N-propylurea 3-benzylpiperidines as selective CC chemokine receptor-3 (CCR3) antagonists.

G. Trainor, M. Covington, C. Decicco, 2004, Bioorganic & medicinal chemistry letters.

Discovery and Preclinical Characterization of INCB018424, a Selective JAK2 Inhibitor for the Treatment of Myeloproliferative Disorders.

S. Verstovsek, J. Fridman, P. Scherle, 2007 .

Design and synthesis of novel CCR2 antagonists: investigation of non-aryl/heteroaryl binding motifs.

D. J. Rogier, Wei Huang, R. Devraj, 2011, Bioorganic & medicinal chemistry letters.

Targeting the c-MET signaling pathway for cancer therapy.

P. Scherle, Xiangdong Liu, W. Yao, 2008, Expert opinion on investigational drugs.

Discovery of INCB3344, a potent, selective and orally bioavailable antagonist of human and murine CCR2.

P. Scherle, K. Vaddi, M. Covington, 2010, Bioorganic & medicinal chemistry letters.

Effect of antiinflammatory drugs on human interleukin-1-induced cartilage degradation

N. Ackerman, R. Newton, E. Arner, 1987, Agents and Actions.

2'-substituted chalcone derivatives as inhibitors of interleukin-1 biosynthesis.

D. G. Jones, M. Covington, R. Newton, 1993, Journal of medicinal chemistry.

Photochemically enhanced binding of small molecules to the tumor necrosis factor receptor-1 inhibits the binding of TNF-α

D. Underwood, P. Domaille, K. Ramnarayan, 2001, Proceedings of the National Academy of Sciences of the United States of America.

α,β-Cyclic-β-benzamido hydroxamic acids: Novel templates for the design, synthesis, and evaluation of selective inhibitors of TNF-α converting enzyme (TACE)

David D. Christ, K. Vaddi, M. Covington, 2008 .

Discovery of beta-benzamido hydroxamic acids as potent, selective, and orally bioavailable TACE inhibitors.

Zelda R Wasserman, J. Trzăskos, K. Vaddi, 2008, Bioorganic & medicinal chemistry letters.

Potent, selective, orally bioavailable inhibitors of tumor necrosis factor-alpha converting enzyme (TACE): discovery of indole, benzofuran, imidazopyridine and pyrazolopyridine P1' substituents.

J. Trzăskos, K. Vaddi, M. Covington, 2008, Bioorganic & medicinal chemistry letters.

Design, Synthesis, and Evaluation of Benzothiadiazepine Hydroxamates as Selective Tumor Necrosis Factor-α Converting Enzyme Inhibitors

S. Mandlekar, K. D. Hardman, R. Magolda, 2003 .

Synthesis and structure-activity relationship of a novel sulfone series of TNF-alpha converting enzyme inhibitors.

Xiaohua He, John Roderick, J. Trzăskos, 2004, Bioorganic & medicinal chemistry letters.

Potent, exceptionally selective, orally bioavailable inhibitors of TNF-alpha Converting Enzyme (TACE): novel 2-substituted-1H-benzo[d]imidazol-1-yl)methyl)benzamide P1' substituents.

J. Trzăskos, K. Vaddi, M. Covington, 2008, Bioorganic & medicinal chemistry letters.

Development of c-MET pathway inhibitors

P. Scherle, Xiangdong Liu, R. Newton, 2011, Expert opinion on investigational drugs.

Discovery of macrocyclic hydroxamic acids containing biphenylmethyl derivatives at P1', a series of selective TNF-alpha converting enzyme inhibitors with potent cellular activity in the inhibition of TNF-alpha release.

B. Jaffee, R. Magolda, J. Trzăskos, 2001, Journal of Medicinal Chemistry.

A new 4-(2-methylquinolin-4-ylmethyl)phenyl P1' group for the beta-amino hydroxamic acid derived TACE inhibitors.

J. Trzăskos, Xiao-tao Chen, K. Vaddi, 2007, Bioorganic & medicinal chemistry letters.

Synthesis and structure–activity relationship of a novel, achiral series of TNF-α converting enzyme inhibitors

J. Trzăskos, T. Maduskuie, B. W. King, 2004 .

Rational design, synthesis and structure-activity relationships of a cyclic succinate series of TNF-alpha converting enzyme inhibitors. Part 1: lead identification.

Xiaohua He, John Roderick, R. Magolda, 2003, Bioorganic & medicinal chemistry letters.

Discovery of N-propylurea 3-benzylpiperidines as selective CC chemokine receptor-3 (CCR3) antagonists.

G. Trainor, M. Covington, C. Decicco, 2004, Bioorganic & medicinal chemistry letters.

A biochemical and kinetic analysis of the interleukin-1 receptor. Evidence for differences in molecular properties of IL-1 receptors.

R. Horuk, M. Covington, R. Newton, 1987, The Journal of biological chemistry.

Discrimination between nonmalignant and malignant cells by combinations of IFN-gamma and IFN-alpha/beta.

C. M. Fleischmann, N. Colburn, R. Newton, 1984, Journal of biological response modifiers.

Indoleamine 2,3-dioxygenase, an emerging target for anti-cancer therapy.

P. Scherle, R. Newton, Xiangdong Liu, 2009, Current cancer drug targets.

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.

Design, synthesis, and evaluation of benzothiadiazepine hydroxamates as selective tumor necrosis factor-alpha converting enzyme inhibitors.

S. Mandlekar, K. D. Hardman, R. Magolda, 2003, Journal of medicinal chemistry.

Permuteins of interleukin 1 beta--a simplified approach for the construction of permutated proteins having new termini.

F. Salemme, P. C. Weber, R. Horuk, 1992, Protein engineering.

Interleukin 1-induced, T cell-mediated regression of immunogenic murine tumors. Requirement for an adequate level of already acquired host concomitant immunity

R. Newton, R. North, S. Loveless, 1988, The Journal of experimental medicine.

Discovery of INCB10820/PF-4178903, a potent, selective, and orally bioavailable dual CCR2 and CCR5 antagonist.

D. J. Rogier, P. Scherle, R. Devraj, 2011, Bioorganic & medicinal chemistry letters.

Aggrecan Protects Cartilage Collagen from Proteolytic Cleavage*

R. Copeland, R. Magolda, J. Trzăskos, 2003, Journal of Biological Chemistry.

Therapeutic potential and strategies for inhibiting tumor necrosis factor-alpha.

C. Decicco, R. Newton, 1999, Journal of medicinal chemistry.

Discovery and structure-activity relationship of N-(ureidoalkyl)-benzyl-piperidines as potent small molecule CC chemokine receptor-3 (CCR3) antagonists.

G. Trainor, M. Covington, C. Decicco, 2002, Journal of medicinal chemistry.

Discovery of INCB8761/PF-4136309, a Potent, Selective, and Orally Bioavailable CCR2 Antagonist.

Lixin Shao, Michael Xia, D. J. Rogier, 2011, ACS medicinal chemistry letters.

Pharmacological characterization of INCB3344, a small molecule antagonist of human CCR2.

R. Wynn, P. Scherle, F. Baribaud, 2009, Biochemical and biophysical research communications.

Discovery and Pharmacological Characterization of a Novel Rodent-Active CCR2 Antagonist, INCB3344

P. Scherle, F. Baribaud, T. Burn, 2005, The Journal of Immunology.

Targeting ADAM-mediated ligand cleavage to inhibit HER3 and EGFR pathways in non-small cell lung cancer.

J. Minna, L. Girard, M. Peyton, 2006, Cancer cell.

Muteins of human interleukin‐1 that show enhanced bioactivities

R. Horuk, J. B. Matthew, M. Covington, 1987, FEBS letters.

Lack of a central role for calcium in the induction and release of human interleukin-1.

R. Newton, 1987, Biochemical and biophysical research communications.

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.

INCB16562, a JAK1/2 selective inhibitor, is efficacious against multiple myeloma cells and reverses the protective effects of cytokine and stromal cell support.

J. Fridman, Jun Li, X. Wen, 2010, Neoplasia.

Selective inhibition of IDO1 effectively regulates mediators of antitumor immunity.

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

Developing c-MET pathway inhibitors for cancer therapy: progress and challenges.

P. Scherle, Xiangdong Liu, R. Newton, 2010, Trends in molecular medicine.

Flow cytometric analysis of the effect of interleukin-1 administration on bone marrow populations in mice.

R. Newton, J. Mckearn, G. Sandlin, 1989, Journal of biological response modifiers.

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.

Targeting the c-MET signaling pathway for cancer therapy

P. Scherle, Xiangdong Liu, W. Yao, 2008 .

A randomised, open-label, phase 2 study of the IDO1 inhibitor epacadostat (INCB024360) versus tamoxifen as therapy for biochemically recurrent (CA-125 relapse)-only epithelial ovarian cancer, primary peritoneal carcinoma, or fallopian tube cancer.

C. Penning, M. Goodheart, R. Schilder, 2017, Gynecologic oncology.

Cloning and Characterization of ADAMTS11, an Aggrecanase from the ADAMTS Family*

R. Wynn, R. Copeland, Y. Itoh, 1999, The Journal of Biological Chemistry.

The distribution and clearance of radiolabeled human interleukin-1 beta in mice.

M. Covington, R. Newton, J. Uhl, 1988, Lymphokine research.

Systemic interleukin 1 administration suppresses arachidonic acid‐induced ear oedema in the mouse

R. Newton, T. Linna, O. Bäck, 1989, The British journal of dermatology.

Phase 1/2 study of epacadostat in combination with ipilimumab in patients with unresectable or metastatic melanoma

G. Gibney, O. Hamid, J. Weber, 2019, Journal of Immunotherapy for Cancer.

Pan-cancer analysis of FGFR1-3 genomic alterations to reveal a complex molecular landscape.

G. Frampton, M. Wing, S. Roychowdhury, 2020 .

Synergistic inhibition with a dual epidermal growth factor receptor/HER-2/neu tyrosine kinase inhibitor and a disintegrin and metalloprotease inhibitor.

J. Fridman, P. Scherle, E. Caulder, 2008, Cancer research.

ADAM proteases, ErbB pathways and cancer

J. Fridman, Bin-Bing S. Zhou, P. Scherle, 2005, Expert opinion on investigational drugs.

511 Updated results from a phase 1/2 study of epacadostat (INCB024360) in combination with ipilimumab in patients with metastatic melanoma

G. Gibney, O. Hamid, J. Weber, 2015 .

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 .

Selective inhibition of ADAM metalloproteases blocks HER-2 extracellular domain (ECD) cleavage and potentiates the anti-tumor effects of trastuzumab

J. Fridman, P. Scherle, K. Vaddi, 2006, Journal of clinical oncology : official journal of the American Society of Clinical Oncology.

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.

Severe retinal degeneration associated with disruption of semaphorin 4A.

D. Rice, A. Sands, G. Hansen, 2004, Investigative ophthalmology & visual science.

Sultam hydroxamates as novel matrix metalloproteinase inhibitors.

K. D. Hardman, J. Trzăskos, M. Covington, 2004, Journal of medicinal chemistry.

Biology of TACE inhibition

K. Vaddi, M. Covington, P. Haley, 2001, Annals of the rheumatic diseases.

The activation of human fibroblast prostaglandin E production by interleukin 1.

M. Covington, R. Newton, 1987, Cellular immunology.

Role of glucose in interleukin‐1β production by lipopolysaccharide‐activated human monocytes

R. Newton, U. Orlinska, 1993, Journal of cellular physiology.

Identification of IL-1 receptors on human monocytes.

R. Horuk, J. Giri, R. Newton, 1989, Journal of immunology.

Design, Synthesis, and Structure−Activity Relationships of Macrocyclic Hydroxamic Acids That Inhibit Tumor Necrosis Factor α Release in Vitro and in Vivo

Chen Lihua, Robert A. Copeland, David J. Nelson, 2001 .

Effects of intracellular ions on interleukin-1 beta production by lipopolysaccharide-activated human monocytes.

R. Newton, U. Orlinska, 1992, The American journal of physiology.

Selective Inhibition of ADAM Metalloproteases as a Novel Approach for Modulating ErbB Pathways in Cancer

J. Grandis, J. Fridman, Bin-Bing S. Zhou, 2007, Clinical Cancer Research.

Selective Inhibition of ADAMMetalloproteases as a Novel Approach for Modulating ErbBPathways in Cancer

J. Grandis, J. Fridman, Bin-Bing S. Zhou, 2007 .

Rational design, synthesis and structure-activity relationships of a cyclic succinate series of TNF-alpha converting enzyme inhibitors. Part 2: lead optimization.

R. Magolda, J. Trzăskos, K. Vaddi, 2004, Bioorganic & medicinal chemistry letters.

Significant Activity of the JAK2 Inhibitor, INCB018424 in Patients with Secondary, Post-Myeloproliferative Disorder (MPD) Acute Myeloid Leukemia (sAML): Results of An Exploratory Phase II Study.

Z. Estrov, H. Kantarjian, S. Verstovsek, 2009 .

28 Retrospective pooled analysis of epacadostat clinical studies identifies doses required for maximal pharmacodynamic effect in anti-PD-1 combination studies

L. Leopold, J. Maleski, R. Newton, 2020, Journal for ImmunoTherapy of Cancer.

Comprehensive genomic profiling and clinical outcomes in patients (pts) with fibroblast growth factor receptor rearrangement-positive (FGFR2+) cholangiocarcinoma (CCA) treated with pemigatinib in the fight-202 trial

D. Melisi, T. Burn, I. Silverman, 2019, Annals of Oncology.

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.

Association of interleukin-1-induced, NF kappa B DNA-binding activity with collagenase gene expression in human gingival fibroblasts.

C. Reddy, R. Taub, M. Tewari, 1996, Archives of oral biology.

The fate of pro-TNF-alpha following inhibition of metalloprotease-dependent processing to soluble TNF-alpha in human monocytes.

M. Covington, C. Decicco, R. Newton, 1997, Journal of immunology.

Treatment with the IDO inhibitor INCB024360 increased lysis of human tumor cell targets by peptide-specific CTL

M. Brechbiel, J. Schlom, P. Kim, 2015, Journal of Immunotherapy for Cancer.

Characterization of murine IL-1 beta. Isolation, expression, and purification.

Y. Lin, R. Horuk, M. Covington, 1988, Journal of immunology.

Discovery of ((1S,3R)-1-isopropyl-3-((3S,4S)-3-methoxy-tetrahydro-2H-pyran-4-ylamino)cyclopentyl)(4-(5-(trifluoromethyl)pyridazin-3-yl)piperazin-1-yl)methanone, PF-4254196, a CCR2 antagonist with an improved cardiovascular profile.

D. J. Rogier, A. Bahinski, P. Scherle, 2011, Bioorganic & medicinal chemistry letters.

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.

Selective inhibition of ADAM metalloproteases blocks HER-2 extracellular domain (ECD) cleavage and potentiates the anti-tumor effects of trastuzumab.

J. Fridman, P. Scherle, K. Vaddi, 2006, Cancer Biology & Therapy.

Discovery of INCB3344, a potent, selective and orally bioavailable antagonist of human and murine CCR2.

P. Scherle, K. Vaddi, M. Covington, 2010, Bioorganic & medicinal chemistry letters.

Effect of interferon on the induction of human monocyte secretion of interleukin-1 activity.

R. Newton, 1985, Immunology.

INCB018424, a Selective JAK1/2 Inhibitor, Significantly Improves the Compromised Nutritional Status and Frank Cachexia in Patients with Myelofibrosis (MF).

H. Kantarjian, S. Verstovsek, R. Mesa, 2008 .