[HTML][HTML] Induction of osteoarthritis in the rat by surgical tear of the meniscus: inhibition of joint damage by a matrix metalloproteinase inhibitor

MJ Janusz, AM Bendele, KK Brown, YO Taiwo… - Osteoarthritis and …, 2002 - Elsevier
Objective Characterize a model of osteoarthritis (OA) induced by a surgically transecting the
medial collateral ligament and meniscus. Evaluate the effectiveness of a matrix …

Moderation of iodoacetate-induced experimental osteoarthritis in rats by matrix metalloproteinase inhibitors

MJ Janusz, EB Hookfin, SA Heitmeyer… - Osteoarthritis and …, 2001 - Elsevier
Objective To determine the effect of matrix metalloproteinase (MMP) inhibitors in mono-iodoacetate-induced
arthritis in rats. Design The ability of compounds to inhibit MMPs in vitro was …

Development of orally bioavailable bicyclic pyrazolones as inhibitors of tumor necrosis factor-α production

…, K Juergens, YO Taiwo, MJ Janusz - Journal of medicinal …, 2004 - ACS Publications
2-Aryl-3-pyrimidinyl based tumor necrosis factor-α (TNF-α) inhibitors, which contain a novel
bicyclic pyrazolone core, are described. Many showed low-nanomolar activity against …

Matrix metalloproteinases are involved in C-terminal and interglobular domain processing of cartilage aggrecan in late stage cartilage degradation

CB Little, CE Hughes, CL Curtis, MJ Janusz, R Bohne… - Matrix Biology, 2002 - Elsevier
Monoclonal antibody (MAb) technology was used to examine aggrecan metabolites and the
role of aggrecanases and matrix metalloproteinases (MMPs) in proteolysis of the …

Design and synthesis of piperazine-based matrix metalloproteinase inhibitors

…, F Gu, ME Dowty, GE Mieling, MJ Janusz… - Journal of medicinal …, 2000 - ACS Publications
A new generation of cyclic matrix metalloproteinase (MMP) inhibitors derived from dl-piperazinecarboxylic
acid has been described. The design involves: incorporation of hydroxamic …

[HTML][HTML] P38 MAP kinase inhibitors as potential therapeutics for the treatment of joint degeneration and pain associated with osteoarthritis

…, L Hsieh, M Buchalova, YO Taiwo, MJ Janusz - Journal of …, 2008 - Springer
Background Evaluate the potential role of p38 inhibitors for the treatment of osteoarthritis
using an animal model of joint degeneration (iodoacetate-induced arthritis) and a pain model (…

Design, synthesis, and biological evaluation of potent thiazine-and thiazepine-based matrix metalloproteinase inhibitors

…, F Gu, LE Williams, BA Hynd, MJ Janusz… - Journal of medicinal …, 1999 - ACS Publications
The synthesis and enzyme inhibition data for a series of thiazine- and thiazepine-based
matrix metalloproteinase (MMP) inhibitors are described. The thiazine- and thiazepine-based …

Development of new hydroxamate matrix metalloproteinase inhibitors derived from functionalized 4-aminoprolines

…, B De, NG Almstead, S Pikul, MJ Janusz… - Journal of medicinal …, 2000 - ACS Publications
A series of hydroxamates was prepared from an aminoproline scaffold and tested for efficacy
as matrix metalloproteinase (MMP) inhibitors. Detailed SAR for the series is reported for …

The development of 2-benzimidazole substituted pyrimidine based inhibitors of lymphocyte specific kinase (Lck)

…, RL Walter, MJ Mekel, A Evdokimov, MJ Janusz - Bioorganic & medicinal …, 2006 - Elsevier
This communication details the synthesis, biological activity, and binding mode of a novel
class of 2-benzimidazole substituted pyrimidines. The most potent analogs disclosed showed …

Inhibition of Human Neutrophil Elastase. 4. Design, Synthesis, X-ray Crystallographic Analysis, and Structure−Activity Relationships for a Series of P2-Modified, Orally …

…, CM Hare, RV Hoffman, MJ Janusz… - Journal of medicinal …, 1998 - ACS Publications
A series of P 2 -modified, orally active peptidic inhibitors of human neutrophil elastase (HNE)
are reported. These pentafluoroethyl ketone-based inhibitors were designed using …