A series of structurally novel aminothiazole based small molecule inhibitors of Itk were prepared to elucidate their structure-activity relationships (SARs), selectivity and cell activity in inhibiting IL-2 secretion in a Jurkat T-cell assay. Compound 2 is identified as a potent and selective Itk inhibitor which inhibits anti-TCR antibody induced IL-2 production in mice in vivo.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1016/j.bmcl.2006.01.115 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
High-intensity focused ultrasound: an innovative approach for micro-manipulation of demineralized dentine.
J Transl Med
January 2025
Dental School, The University of Western Australia, 17 Monash Avenue, Nedlands, WA, 6009, Australia.
Background: Treatment of deep carious lesions poses significant challenges in dentistry, as complete lesion removal risks compromising pulp vitality, while selective removal often reduces the longevity of restorations. Herein, we propose a minimally invasive approach using High-Intensity Focused Ultrasound (HIFU) for microscale removal of carious dentine. Concurrently, HIFU's antimicrobial effects against associated cariogenic biofilms and the corresponding thermal and biological impacts on surrounding tissues were investigated.
View Article and Find Full Text PDFCompound 38, a novel potent and selective antagonist of adenosine A receptor, enhances arousal in mice.
Acta Pharmacol Sin
January 2025
Department of Pharmacology, School of Basic Medical Sciences, State Key Laboratory of Medical Neurobiology and MOE Frontiers Center for Brain Science, Institutes of Brain Science, Joint International Research Laboratory of Sleep, Fudan University, Shanghai, 200032, China.
Adenosine A receptor (AR) plays a pivotal role in the regulation of sleep-wake behaviors. We previously reported an AR selective antagonist compound 38 with an IC value of 29.0 nM.
View Article and Find Full Text PDFPan-inhibition of super-enhancer-driven oncogenic transcription by next-generation synthetic ecteinascidins yields potent anti-cancer activity.
Nat Commun
January 2025
IGBMC, Institut de Génétique et de Biologie Moléculaire et Cellulaire Illkirch Cedex, C.U. Equipe Labélisée Ligue contre le Cancer, Strasbourg, France.
The plasticity of cancer cells facilitates their ability to adopt heterogeneous differentiation states, posing a significant challenge to therapeutic interventions. Specific gene expression programs, driven in part by super-enhancers (SEs), underlie cancer cell states. Here we successfully inhibit SE-driven transcription in phenotypically distinct metastatic melanoma cells using next-generation synthetic ecteinascidins.
View Article and Find Full Text PDFTargeting the Hippo and Rap1 signaling pathways: the anti-proliferative effects of curcumin in colorectal cancer cell lines.
Med Oncol
January 2025
Department of Medical Surgical Nursing, College of Nursing, Princess Nourah bint Abdulrahman University, P.O. Box 84428, 11671, Riyadh, Saudi Arabia.
CRC has the third-highest cancer incidence and death. Many human cancers, including colorectal cancer, are connected to abnormal signaling pathway gene expression. Many human malignancies include Hippo and Rap1 signaling.
View Article and Find Full Text PDFOligosaccharide-assisted resolution of holothurian fucosylated chondroitin sulfate for fine structure and P-selectin inhibition.
Carbohydr Polym
March 2025
School of Chemistry and Materials Science, South-Central Minzu University, Wuhan 430074, China; School of Pharmaceutical Sciences, South-Central Minzu University, Wuhan 430074, China. Electronic address:
Fucosylated chondroitin sulfate (FCS) from Holothuria mexicana (FCS) was selected for investigation because of its intriguing branch features. Selective β-eliminative depolymerization and the bottom-up assembly were performed to unravel that FCS consisted of a {D-GlcA-β1,3-D-GalNAc} backbone and branches of alternating Fuc (55 %) and D-GalNAc-α1,2-L-Fuc (45 %), the highest proportion of disaccharide branch reported to date. In branches, sulfation could occur at every free -OH site except O-3 of GalNAc, being the most complex and various structure features of natural FCS.
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!