A5111632271- Synthesis and biological activity
- Cancer Mechanisms and Therapy
- Cytokine Signaling Pathways and Interactions
- Cell death mechanisms and regulation
- Melanoma and MAPK Pathways
- Synthesis and Characterization of Heterocyclic Compounds
- Machine Learning in Materials Science
- Synthesis and Reactions of Organic Compounds
- RNA Interference and Gene Delivery
- Quinazolinone synthesis and applications
- Synthesis of Tetrazole Derivatives
- Medical Imaging Techniques and Applications
- Analytical Chemistry and Chromatography
- Chemical Synthesis and Analysis
- Eicosanoids and Hypertension Pharmacology
- Pesticide Residue Analysis and Safety
- S100 Proteins and Annexins
- Digital Radiography and Breast Imaging
- Cholesterol and Lipid Metabolism
- Forensic Fingerprint Detection Methods
- NMR spectroscopy and applications
- Multicomponent Synthesis of Heterocycles
- Historical Medical Research and Treatments
- Cell Image Analysis Techniques
- Fungal and yeast genetics research
Faculty of 1000 (United States)
2023
Burlington College
2023
RELX Group (United States)
2023
Scripps Research Institute
2009-2019
Scripps (United States)
2011
Scripps Institution of Oceanography
2011
Translational Research Institute
2009
University of Florida
2003
Modular Genetics (United States)
1998
SMART Reading
1998
AbstractTumor cells can grow in an anchorage-independent manner. This is mediated part through survival signals that bypass normal growth restraints controlled by integrin cell surface receptors. Focal adhesion kinase (FAK) a cytoplasmic protein-tyrosine associates with integrins and modulates various cellular processes including growth, survival, migration. As increased FAK expression tyrosine phosphorylation are associated tumor progression, inhibitors of being tested for anti-tumor...
Dasatinib was approved in 2006 for the treatment of imatinib-resistant chronic myelogenous leukemia and functions primarily through inhibition BCR-ABL Src kinase. is extensively metabolized humans by CYP3A4. In this study, we report that bioactivation dasatinib CYP3A4 proceeds a reactive intermediate leads to inactivation with <i>K</i><sub>I</sub> = 6.3 μM <i>k</i><sub>inact</sub> 0.034 min<sup>–1</sup>. The major mechanism hydroxylation at <i>para</i>-position 2-chloro-6-methylphenyl ring...
The thiazolidinediones (TZD) typified by rosiglitazone are the only approved therapeutics targeting PPARγ for treatment of type-2 diabetes (T2DM). Unfortunately, despite robust insulin sensitizing properties, they accompanied a number severe side effects including congestive heart failure, edema, weight gain, and osteoporosis. We recently identified antagonists that bind reversibly with high affinity but do not induce transactivation receptor, yet act as sensitizers in mouse models...
Both JNK and LRRK2 are associated with Parkinson's disease (PD). Here we report a reasonably selective potent kinase inhibitor (compound 6) that bound to both (a dual inhibitor). A bidentate-binding strategy simultaneously utilized the ATP hinge binding unique protein surface site outside of pocket was applied design identification this kind inhibitor. Compound 6 JNK3 modest an enzyme IC50 value 12 nM 99 (LRRK2-G2019S), respectively. also exhibited good cell potency, inhibited...
The design and synthesis of a potent series c-jun N-terminal kinase (JNK2) inhibitors is described. development optimization the 2,4-diaminopyrimidines was carried out from an earlier in-house inhibitor program. Through scaffold 2, several cell compounds with good in vivo profiles were discovered.
ADVERTISEMENT RETURN TO ISSUEPREVAddition/CorrectionNEXTORIGINAL ARTICLEThis notice is a correctionCorrection to Discovery of Novel Class Exquisitely Selective Mesenchymal-Epithelial Transition Factor (c-MET) Protein Kinase Inhibitors and Identification the Clinical Candidate 2-(4-(1-(Quinolin-6-ylmethyl)-1H-[1,2,3]triazolo[4,5-b]pyrazin-6-yl)-1H-pyrazol-1-yl)ethanol (PF-04217903) for Treatment CancerJ. Jean Cui*, Michele McTigue, Mitchell Nambu, Michelle Tran-Dubé, Mason Pairish, Hong Shen,...
Despite a massive industry endeavor to develop RORγ-modulators for autoimmune disorders, there has been no indication of efforts target the close family member RORα similar indications. This may be due misconception that is redundant RORγ, or inherent difficulty in cultivating tractable starting points RORα. RORα-selective modulators would useful tools interrogate biology this understudied orphan nuclear receptor.The goal research effort was identify and optimize synthetic ligands from known...