نتایج جستجو برای: kinase inhibitors
تعداد نتایج: 385681 فیلتر نتایج به سال:
kaolin-so3h as a new solid acid is prepared via reaction of kaolin and chlorosulfonic acid. this natural based catalyst is very inexpensive and easy available. imidazoles are an important class of heterocycles being the core fragment of different natural products and biological systems such as anti-allergic, anti-inflammatory, analgesic, antifungal, antimycotic, antibiotic, antiulcerative, anti...
Publicly available kinase inhibitors provide a large source of information for structure-activity relationship analysis and kinase drug design. In this study, publicly available inhibitors of the human kinome were collected and analog series formed by kinase inhibitors systematically identified. Then, alternative scaffold concepts were applied to assess diversity and promiscuity of kinase inhib...
objective(s):several investigations have revealed that caspase-14 is responsible for the epidermal differentiation and cornification, as well as the regulation of moisturizing effect. however, the precise regulation mechanism is still not clear. this study was aimed to investigate the expression of caspase-14 in filaggrin-deficient normal human epidermal keratinocytes (nheks) and to explore the...
Background: The transformation of epidermal growth factor receptor (EGFR)-mutant lung adenocarcinoma (LUAD) into small cell cancer (SCLC) accounts for 3–14% the resistance mechanism to EGFR tyrosine kinase inhibitors (TKIs). At present, there is no relevant research explore dynamic expression EGFR-mutant proteins and genomic evolution in transformed SCLC/neuroendocrine carcinoma (NEC).
Novel inhibitors that target the Eph family of transmembrane tyrosine kinase receptors have been optimized and characterized. Some compounds show remarkable receptor selectivity affinity for inhibit growth colon cancer cells where these are expressed active. More information can be found in Research Article by G. Tosato, H. Schwalbe co-workers (DOI: 10.1002/chem.202203967).
Src is a non-receptor tyrosine kinase (TK) whose involvement in cancer, including glioblastoma (GBM), has been extensively demonstrated. In this context, we started from our in-house library of pyrazolo[3,4-d]pyrimidines that are active as and/or Bcr-Abl TK inhibitors and performed lead optimization study to discover new generation derivative suitable for targeting. We synthesized 19 compounds,...
An ultrasensitive electrochemical assay for T4 polynucleotide kinase (T4 PNK) activity and inhibition was developed based on magnetic Fe 3 O 4 @TiO 2 core–shell nanoparticles gold hybrid probe (Fe -dsDNA-AuNPs) modified electrode (MGE). -dsDNA-AuNPs formed via DNA hybridization between phosphorylated S1 complementary S2 assembled AuNPs. [Ru(NH ) 6 ] 3+ used as an electrochemically active indica...
People’s lives and health are gravely threatened by non-small-cell lung cancer (NSCLC). Mutations in epidermal growth factor receptor (EGFR), a transmembrane tyrosine kinase, considered one of the causes NSCLC. Tyrosine kinase inhibitors (TKIs) typically used to treat patients with EGFR mutations. In this study, Gefitinib, member first generation TKIs, was an single-point mutation (single mutan...
Kinases are principal components of signal transduction pathways and the focus of intense basic and drug discovery research. Irreversible inhibitors that covalently modify non-catalytic cysteines in kinase active sites have emerged as valuable probes and approved drugs. Many protein classes, however, have functional cysteines, and therefore understanding the proteome-wide selectivity of covalen...
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