Eckert, William A 3rd Wiener, John J M Cai, Hui Ameriks, Michael K Zhu, Jian Ngo, Karen Nguyen, Steven Fung-Leung, Wai-Ping Thurmond, Robin L Grice, Cheryl
...
Published in
European journal of pharmacology
Cathepsin S (CatS) is a cysteine protease found in lysosomes of hematopoietic and microglial cells and in secreted form in the extracellular space. While CatS has been shown to contribute significantly to neuropathic pain, the precise mechanisms remain unclear. In this report, we describe JNJ-39641160, a novel non-covalent, potent, selective and or...
Lemke, Carina Cianni, Lorenzo Feldmann, Christian Gilberg, Erik Yin, Jiafei Dos Reis Rocho, Fernanda de Vita, Daniela Bartz, Ulrike Bajorath, Jürgen Montanari, Carlos A
...
Published in
Bioorganic & medicinal chemistry letters
A library of cathepsin S inhibitors of the dipeptide nitrile chemotype, bearing a bioisosteric sulfonamide moiety, was synthesized. Kinetic investigations were performed at four human cysteine proteases, i.e. cathepsins S, B, K and L. Compound 12 with a terminal 3-biphenyl sulfonamide substituent was the most potent (Ki = 4.02 nM; selectivity ratio...
Lai, Chao-Han Chang, Jang-Yang Wang, Kuan-Chieh Lee, Fang-Tzu Wu, Hua-Lin Cheng, Tsung-Lin
Published in
European journal of vascular and endovascular surgery : the official journal of the European Society for Vascular Surgery
Evidence suggests that cathepsin S (CTSS), a potent mammalian elastase, participates in abdominal aortic aneurysm (AAA) formation. This study examines the hypothesis that pharmacological inhibition of CTSS with an α-ketoamide based compound 6r might suppress AAA in mice. Experimental study of the CaCl2 induced AAA model in B6 mice and angiotensin I...
Ahmad, Sabahuddin Bhagwati, Sudha Kumar, Sushil Banerjee, Dibyendu Siddiqi, Mohammad Imran
Published in
Journal of molecular graphics & modelling
Cathepsin S (CatS) is one of the cysteinyl cathepsins widely studied for its clinical significance and found to be a promising therapeutic target for several diseases; to name a few is arthritis, allergic inflammation, cancer, diabetes, obesity, and cystic fibrosis. Elevated CatS level is a contributing factor for related disorders, and therefore a...
Vlachogiannis, Nikolaos I. Gatsiou, Aikaterini Silvestris, Domenico Alessandro Stamatelopoulos, Kimon Tektonidou, Maria G. Gallo, Angela Sfikakis, Petros P. Stellos, Konstantinos
Published in
Journal of Autoimmunity
• The RNA editing enzyme ADAR1 is increased in rheumatoid arthritis. • ADAR1-induced Alu A-to-I RNA editing is increased in active RA and decreases after treatment only in responding patients. • Association of increased A-to-I RNA editing with pro-inflammatory gene expression suggests a role in chronic inflammation. • Interrupting the pro-inflammat...
Montague-Cardoso, Karli Pitcher, Thomas Chisolm, Kim Salera, Giorgia Lindstrom, Erik Hewitt, Ellen Solito, Egle Malcangio, Marzia
Published in
Brain, behavior, and immunity
Chemotherapy-induced neuropathic pain is a dose-limiting side effect of many cancer therapies due to their propensity to accumulate in peripheral nerves, which is facilitated by the permeability of the blood-nerve barrier. Preclinically, the chemotherapy agent vincristine (VCR) activates endothelial cells in the murine peripheral nervous system and...
Campden, Rhiannon I Zhang, Yifei
Published in
Archives of biochemistry and biophysics
Lysosomal cysteine cathepsins are a family of proteases that are involved in a myriad of cellular processes from proteolytic degradation in the lysosome to bone resorption. These proteins mature following the cleavage of a pro-domain in the lysosome to become either exo- or endo-peptidases. The cathepsins B, C, L, S and Z have been implicated in NL...
Hargreaves, Patrick Daoudlarian, Douglas Theron, Michel Kolb, Fabrice A. Manchester Young, Marianne Reis, Bernhard Tiaden, Andre Bannert, Bettina Kyburz, Diego Manigold, Tobias
...
Published in
Arthritis Research & Therapy
ObjectivePrimary Sjögren syndrome (pSS) is characterized by T and B cell infiltration of exocrine glands. The cysteine protease cathepsin S (CatS) is crucially involved in MHCII processing and T cell stimulation, and elevated levels have been found in patients with RA, psoriasis and pSS. However, little is known about the functional characteristics...
Lee, Byung-Chul Kang, Insung Lee, Seung-Eun Lee, Jin Young Shin, Nari Kim, Jae-Jun Choi, Soon Won Kang, Kyung-Sun
Published in
BMB Reports
Social requirements are needed for living in an aging society and individual longevity. Among them, improved health and medical cares, appropriate for an aging society are strongly demanded. Human cord blood-derived plasma (hUCP) has recently emerged for its unique anti-aging effects. In this study, we investigated brain rejuvenation, particularly ...
Janga, Srikanth R Shah, Mihir Ju, Yaping Meng, Zhen Edman, Maria C Hamm-Alvarez, Sarah F
Published in
Biomarkers : biochemical indicators of exposure, response, and susceptibility to chemicals
Cathepsin S (CTSS) activity is elevated in Sjögren's Syndrome (SS) patient tears. To evaluate longitudinal expression of tear and tissue CTSS activity relative to other disease indicators in Non-Obese Diabetic (NOD) mice. CTSS activity was measured in tears and lacrimal glands (LG) from male 1-6 month (M) NOD and 1 and 6 M BALB/c mice. Lymphocytic ...
