The article examines drug interactions that affect tyrosine kinase inhibitor (TKI) metabolism. It lists medicines indicated for the treatment of a variety of malignancies due to their ability to interfere with cell communication and growth. The effects of cytochrome P450 3A4 (CYP3A) inhibitors and ...
Identification of novel tyrosine kinase inhibitors for drug resistant T315I mutant BCR-ABL: a virtual screening and molecular dynamics simulations study Hemanth Naick Banavath1*, Om Prakash Sharma2*, Muthuvel Suresh Kumar2 & R. Baskaran1 1Department of Biochemistry & Molecular biology, School of ...
Nature Reviews Drug Discovery volume 9, pages 956–970 (2010)Cite this article 3764 Accesses 7 Altmetric Metrics details Key Points Receptor and non-receptor tyrosine kinases are involved in multiple proliferative signalling pathways. Imatinib, one of the first tyrosine kinase inhibitors (TKIs) to ...
It has opened the way to the development of additional tyrosine kinase inhibitors (TKIs), including sunitinib, nilotinib, dasatinib and sorafenib, all indicated for the treatment of various haematological malignancies and solid tumours. TKIs are prescribed for prolonged periods and are often taken by ...
Spleen tyrosine kinase (SYK) plays a crucial role in the coordination of immune recognition receptors and orchestrates multiple downstream signaling pathways in various hematopoietic cells. In addition to its well-known function in transducing Fcγ receptor-and B cell receptor-mediated events, SYK signa...
different humanmalignancies. Moreover, PTKs are considered therapeutic targets in cancer [54,55]. AlthoughTyrosine kinase inhibitors(TKIs) therapy has led to increasing lifespans for many patients with blood and solid cancers, drug resistance andcancer relapsecontinue to be a major limit. Autophagic ...
Figure 7. Some Bcr-Abl and dual Src and Bcr-Abl tyrosine kinase inhibitors, including several that have advanced to clinical testing. AMN-107,139 a second-generation analog of STI-571, is a more potent inhibitor of Bcr-Abl kinase (IC50<30 nM) as well as being active against se...
A major challenge to improving the benefits of targeted therapies is understanding the molecular mechanisms of acquired resistance to tyrosine kinase inhibitors (TKIs). Enormous efforts have been made to identify activating mutations, particularly those involved in cancer initiation and drug resistance. ...
However, despite the dramatic initial responses to treatment in some cases, NSCLC eventually becomes resistant to EGFR-tyrosine kinase inhibitors (TKIs). Mechanisms of resistance include EGFR secondary mutations that interfere with drug binding. Besides, molecular cross-talk and redundancy between EGFR ...
Tyrosine kinase inhibitors (TKIs) are oral targeted agents that have become the standard guideline-recommended treatment for patients withBCR-ABL1positive or Ph-positive CML.3The aim of oral TKI treatment is to obtain optimal hematologic, cytogenetic, and molecular responses ([MRs] typically mea...