Under the conditions of the assays, dasatinib was able to overcome imatinib resistance resulting from BCR-ABL kinase domain mutations, activation of alternate signaling pathways involving the SRC family kinases (LYN, HCK), and multi-drug resistance gene overexpression. How should this medicine be ...
To understand the structural basis of promiscuous inhibitor binding, we determined the co-crystal structure of the receptor tyrosine kinase DDR1 with the type I inhibitors dasatinib and VX-680. Surprisingly, we find that DDR1 binds these type I inhibitors in an inactive conformation typically ...
Sprycel®, also known as dasatinib, is a protein-tyrosine kinase inhibitor generally used to treat two types of leukemia — chronic myeloid leukemia (CML) and acute lymphoblastic leukemia (ALL). This medication stops the spread of leukemia cancer cells by slowing down their growth rate. Usually...
Ultimately, one goal would be to use MRD as an early readout in clinical trials, which could potentially greatly shorten clinical trials (an example would be the 1-year BCR-ABL level endpoint in the registration trials of dasatinib and nilotinib in CML). However, beyond this, there are ...
Van Etten said, pointing out that "the devil is always in the details." For instance, the 4% rate of progression seen with imatinib in this trial is quite different from the 1.5% that was reported with the drug in the IRIS trial. Another approach in the treatment of CML is the ...
BRAF mutations are found to frequently occur in many cancers, and many kinase inhibitors are in clinical trials specifically targeting B-RAF kinase. Currently there is only one FDA-approved small molecule drug which targets many other oncogenes besides BRAF: ...
Cancer-associated fibroblasts (CAFs) are a major component of the tumor stroma and actively participate in tumor development, invasion, metas- tasis, drug resistance, and other biological behaviors. CAFs are a highly heterogeneous group of cells, a reflection of the diversity of their origin, ...
The high frequency of primary KIT and PDGFRA mutations in these tumors makes them sensitive to kinase inhibitors such as imatinib, and this drug is FDA- approved for use in both the adjuvant and advanced disease settings. Accurate assessment of the risk of disease recurrence is essential in ...
The drug is used in the treatment of bladder, colorectal and pancreatic cancers, head and neck sarcoma, and lung-, hepatic and esophageal carcinoma [273]. Spergualin (C17H37N7O4, Mw. 403.53 Da), produced by Brevibacillus laterosporus BMG162-aF2, re- pressed fibrosarcoma cells (M5076) ...
9 RegisterLog in Sign up with one click: Facebook Twitter Google Share on Facebook EFN (redirected fromEphrin) AcronymDefinition EFNÉcole Française de Naples(French: French School of Naples) EFNEscuela Francesa de Negocios(Spanish: French School of Business; Uruguay) ...