A series of competitive, reversible cathepsin S (CatS) inhibitors was investigated. An earlier disclosure detailed the discovery of the 4-(2-keto-1-benzimidazolinyl)-piperidin-1-yl moiety as an effective replacement for the 4-arylpiperazin-1-yl group found in our screening hit. Continued investigation into replacements for the 4-aryl piperazine resulted in the identification of potentially useful CatS inhibitors with enzymatic and cellular activity similar to that of JNJ 10329670 as disclosed in a previous publication.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1016/j.bmcl.2006.01.038 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Development of a reporter feline herpesvirus-1 for antiviral screening assays.
Vet Res
December 2024
Shenzhen Key Laboratory of Viral Vectors for Biomedicine, Shenzhen-Hong Kong Institute of Brain Science, Shenzhen Institute of Advanced Technology, Chinese Academy of Sciences, Shenzhen, 518055, China.
Feline herpesvirus type 1 (FHV-1), a member of the Herpesviridae family, is one of the most important pathogens that causes upper respiratory tract disease in felines. Following infection, FHV-1 can spread retrogradely to the trigeminal ganglia, establishing a life-long latency. Although vaccines are available for routine feline vaccination, FHV-1 is still an agent that poses a serious threat to feline health.
View Article and Find Full Text PDFThe renin-angiotensin-aldosterone system in kidney diseases of cats and dogs.
Vet J
December 2024
Department of Small Animal Medicine and Surgery, University of Georgia, College of Veterinary Medicine, Athens 30601, USA.
The renin-angiotensin-aldosterone system (RAAS) has a well-established key pathophysiologic role in kidney diseases, and pharmacotherapy targeting this system is a mainstay of treatment of affected human beings, cats, and dogs. Several studies have evaluated the circulating RAAS in animals with spontaneous or experimentally induced kidney diseases. Evidence supporting the activation of this system has been demonstrated in some - but not all - studies and individuals, and the interindividual variability in circulating RAAS markers is high.
View Article and Find Full Text PDFFrequency and progression of azotemia during acute and chronic treatment of congestive heart failure in cats.
J Vet Intern Med
December 2024
Department of Veterinary Clinical Sciences, College of Veterinary Medicine, Iowa State University, Ames, Iowa, USA.
Background: Azotemia is common in cats with congestive heart failure (CHF) and might be exacerbated by diuretic therapy.
Hypothesis/objectives: Determine frequency, risk factors, and survival impact of progressive azotemia in cats treated for CHF.
Animals: One hundred and sixteen client-owned cats with kidney function testing performed at least twice during acute or chronic CHF treatment.
Salivary peptidomic profiling of chronic gingivostomatitis in cats by matrix-assisted laser desorption/ionization-time-of-flight mass spectrometry and nanoscale liquid chromatography-tandem mass spectrometry.
J Vet Intern Med
December 2024
Department of Pathology, Faculty of Veterinary Science, Chulalongkorn University, Bangkok, Thailand.
Background: Chronic gingivostomatitis in cats (FCGS) is a moderately to severely painful condition, potentially caused by inadequate immune response to oral antigenic stimulation. Salivary peptidome analysis can identify inflammatory protein mediators and pathways involved in oral mucosal immune activation and may indicate potential therapeutic options for FCGS.
Objective: Evaluate the diversity and abundance of salivary peptides in cats with FCGS using matrix-assisted laser desorption/ionization-time-of-flight mass spectrometry (MALDI-TOF MS) and nanoscale liquid chromatography-tandem mass spectrometry (nano LC-MS/MS).
Synthesis of α-fluorocinnamate derivatives as novel cathepsin S inhibitors with in vitro antiproliferative activity against pancreatic cancer cells.
Bioorg Med Chem
December 2024
Department of Chemistry, University of Milan, Via Golgi 19, 20133 Milano, Italy.
Cathepsins, key members of the papain-like family of cysteine proteases, are crucial for proteolysis processes within human cells, including osteolysis, immunomodulation and apoptosis. Recent research has highlighted the significant role of cathepsins, particularly the L, S, K, and B subtypes, in pancreatic cancer. This has driven the development of novel cathepsin inhibitors as potential treatments to inhibit tumor progression, migration and invasion.
View Article and Find Full Text PDFWant AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!