Orally Active MMP-1 Sparing α-Tetrahydropyranyl and α-Piperidinyl Sulfone Matrix Metalloproteinase (MMP) Inhibitors with Efficacy in Cancer, Arthritis, and Cardiovascular Disease

Daniel P. Becker, Thomas E. Barta, Louis J. Bedell, +24

Journal of Medicinal Chemistry

Spare Mmp-1PharmacotherapyPharmaceutical ChemistryInflammatory ArthritisTumor Biology +15

Synthesis and Structure−Activity Relationships of β- and α-Piperidine Sulfone Hydroxamic Acid Matrix Metalloproteinase Inhibitors with Oral Antitumor Efficacy

Daniel P. Becker, Clara I. Villamil, Thomas E. Barta, +15

Journal of Medicinal Chemistry

Pharmaceutical ScienceBreast OncologyImmunologyPharmacotherapyPharmaceutical Chemistry +21

Novel Autotaxin Inhibitors for the Treatment of Osteoarthritis Pain: Lead Optimization via Structure-Based Drug Design

Spencer B. Jones, Lance A. Pfeifer, Thomas J. Bleisch, +17

ACS Medicinal Chemistry Letters

Excellent PotencyPharmaceutical ScienceDrug TargetBioorganic ChemistryMolecular Pain +18

Development of a novel clinical biomarker assay to detect and quantify aggrecanase-generated aggrecan fragments in human synovial fluid, serum and urine

Craig Swearingen, John W. Carpenter, Robert W. Siegel, +13

Osteoarthritis and Cartilage

Biomarker (Medicine)EngineeringAutoimmune DiseaseAggrecanase-generated Aggrecan FragmentsMedicine +11

α-Amino-β-sulphone hydroxamates as potent MMP-13 inhibitors that spare MMP-1

Daniel P. Becker, Thomas E. Barta, Louis J. Bedell, +10

Bioorganic & Medicinal Chemistry Letters

Medicinal ChemistryMedicinePotent Mmp-13 InhibitorsPharmacotherapyAnti-cancer Agent +4

Intraarticular Matrix Metalloproteinases and Aggrecan Degradation Are Elevated After Articular Fracture

Justin M. Haller, Craig Swearingen, Deveree Partridge, +3

Clinical Orthopaedics and Related Research

Negatively charged residues interacting with the p4 pocket confer binding specificity to DRB1*0401

Susan L. Woulfe, Christine P. Bono, Michelle L. Zacheis, +5

Arthritis & Rheumatism

Pharmacological Characterization of a Potent Inhibitor of Autotaxin in Animal Models of Inflammatory Bowel Disease and Multiple Sclerosis

Kannan Thirunavukkarasu, Craig Swearingen, Guilherme Rocha, +6

Journal of Pharmacology and Experimental Therapeutics

Investigation of pre-existing reactivity to biotherapeutics can uncover potential immunogenic epitopes and predict immunogenicity risk

Nicoletta Bivi, Terry L. Moore, George H. Rodgers, +10

mAbs

ImmunologyImmunodominanceImmunotherapeuticsImmunotherapySerum Pre-existing Reactivity +18

A short-term pharmacodynamic model for monitoring aggrecanase activity: injection of monosodium iodoacetate (MIA) in rats and assessment of aggrecan neoepitope release in synovial fluid using novel ELISAs

Craig Swearingen, M.G. Chambers, Chaohua Lin, +11

Osteoarthritis and Cartilage

Monosodium IodoacetateAutoimmune DiseaseMedicineBioanalysisGlycobiology +6