Abstracts tagged "kinase and rheumatoid arthritis (RA)"

Abstract Number: 484 • 2016 ACR/ARHP Annual Meeting
Targeting the BTK-JAK Axis in Preclinical Models of Rat Collagen-Induced Arthritis with GS-4059 in Combination with a JAK Inhibitor
Julie Di Paolo¹, Christian Franci², Terry Gentzler¹, Bernard Murray³ and Li Li⁴, ¹Biology, Gilead Sciences, Foster City, CA, ²Biology, Gilead Sciences, Foster, CA, ³DMPK, Gilead Sciences, Foster City, CA, ⁴Gilead Sciences, South San Francisco, CA
Background/Purpose: Bruton’s Tyrosine Kinase (BTK) mediates signaling in hematopoietic cells important for the initiation and progression of rheumatoid arthritis (RA). GS-4059 is an oral,…
Abstract Number: 1671 • 2015 ACR/ARHP Annual Meeting
Discovery of PRN1008, a Novel, Reversible Covalent BTK Inhibitor in Clinical Development for Rheumatoid Arthritis
Ronald J. Hill¹, Patrick Smith², Janakan Krishnarajah³, J. Michael Bradshaw¹, Mohammad Masjedizadeh¹, Angelina Bisconte¹, Dane Karr¹, Timothy D. Owens¹, Ken Brameld¹, Jens Oliver Funk¹, David M. Goldstein¹, Philip A. Nunn¹ and Steven G. Gourlay¹, ¹Principia Biopharma, South San Francisco, CA, ²d3 Medicine, Parsippany, NJ, ³Linear Research Pty Ltd, Perth, Australia
Background/Purpose: There is strong pre-clinical validation for Bruton’s Tyrosine Kinase (BTK) as a therapeutic target for autoimmune diseases based on multiple animal models. Principia discovered…
Abstract Number: 1484 • 2014 ACR/ARHP Annual Meeting
Discovery of ARN-4079 – a Potent, Orally Available Dual Target Inhibitor of Janus Kinase 3 (JAK3) and Interleukin-2 Inducible T-Cell Kinase (ITK) for Rheumatoid Arthritis
Hariprasad Vankayalapati¹, Venkatakrishnareddy Yerramreddy¹, Philip Bendele², Alison Bendele³, Rueban Jacob Anicattu Issac⁴, Ram Sudheer Adluri⁵, Philip LoGrasso⁶ and Joel M. Kremer⁷, ¹Early Discovery and Medicinal Chemistry, Arrien Pharmaceuticals, Salt Lake City, UT, ²Principal Investigator CIA models, Bolder BioPATH, Inc., Boulder, CO, ³Pathologist, Bolder BioPATH Inc., Boulder, CO, ⁴Biology, GVK Biosciences Private Limited., Hyderabad, India, ⁵GVK Biosciences Private Limited., Hyderabad, India, ⁶Molecular Therapeutics, The Scripps Research Institute, Jupiter, FL, ⁷Medicine, Albany Medical College and the Center for Rheumatology, Albany, NY
Background/Purpose: The Non-receptor tyrosine kinases, JAK3 and ITK are key regulators of cytokine pathways and are important clinically validated targets, which offer the potential for…
Abstract Number: 1495 • 2014 ACR/ARHP Annual Meeting
Preclinical and Clinical Phase I Profile of MK-8457, a Selective Spleen Tyrosine Kinase and Zeta-Chain-Associated Protein Kinase 70 Inhibitor, Developed for the Treatment of Rheumatoid Arthritis
Gene Marcantonio¹, Alan Bass², Gretchen Baltus³, Judith Boice¹, Hongmin Chen⁴, Michael Crackower⁵, Jeroen Elassaiss-Schaap⁶, Michael Ellis⁷, Tomoko Freshwater⁸, Francois Gervais⁹, Jane Guo¹⁰, Sammy Kim⁹, Lily Moy⁵, Alan Northrup⁷, Jie Zhang-Hoover⁴, Mathew Maddess¹¹, Richard Miller¹², Marcella Ruddy⁵, Stella Vincent¹³, Haoling Weng¹ and Hani Houshyar¹⁴, ¹Merck & Co., Whitehouse Station, NJ, ²Safety Assessment, Merck & Co., Boston, MA, ³Immunomodulatory Regulators, Merck & Co., Boston, MA, ⁴Pharmacology, Merck & Co., Boston, MA, ⁵Merck & Co., Boston, MA, ⁶Clinical PK-PD, Merck & Co., Oss, Netherlands, ⁷Medicinal Chemistry, Merck & Co., Boston, MA, ⁸PPDM Early Stage, Merck & Co., Rahway, NJ, ⁹Cell Pathways and Proteins, Merck & Co., Boston, MA, ¹⁰Immunology, Merck & Co., Boston, MA, ¹¹Discovery Process Chemistry, Merck & Co., Boston, MA, ¹²Biochemistry & Biophysics, Merck & Co., Boston, MA, ¹³PPDM Preclinical ADME, Merck & Co., Boston, MA, ¹⁴33 Avenue Louis Pasteur, Merck & Co., Boston, MA
Background/Purpose: Spleen tyrosine kinase (SYK) is a potential target for treatment of several diseases including rheumatoid arthritis. SYK is a member of the Zeta-chain-associated protein…
Abstract Number: 329 • 2014 ACR/ARHP Annual Meeting
A Novel, Small Molecule Cyclin-Dependent Kinase 4/6 Inhibitor As the New Option for Treatment of Rheumatoid Arthritis
Hiroshi Takahashi¹, Tsuyoshi Mizuno¹, Toshimichi Nakamura¹, Yuri Sakai¹, Yumiko Muroga¹, Kyohei Horie¹, Naoki Hase¹, Hitoshi Kohsaka² and Tsuyoshi Kimura¹, ¹Teijin Pharma Limited, Hino,Tokyo, Japan, ²Department of Rheumatology, Graduate School of Medical and Dental Sciences,, Tokyo Medical and Dental University (TMDU), Tokyo, Japan
Background/Purpose The pathogenesis of rheumatoid arthritis (RA) is characterized by infiltration of immune cells to the synovial tissues and their hyperplasia. Therapeutic strategies to inhibit…
Abstract Number: 1150 • 2013 ACR/ARHP Annual Meeting
Differential Regulation Of IL-10 and Dusp1 Production By Kinases In The p38 MAPK Pathway
Deepa Hammaker¹, Katharyn Topolewski² and G. S. Firestein³, ¹MC 0656, UCSD School of Medicine, La Jolla, CA, ²UCSD School of Medicine, La Jolla, CA, ³Div of Rheumatology, UCSD School of Medicine, La Jolla, CA
Background/Purpose: MAPK kinases MKK3 and MKK6 regulate p38 function in inflammatory diseases like rheumatoid arthritis (RA). Targeting MKK3 or MKK6 might be superior to traditional…

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