Tyrosine kinases are implicated in tumorigenesis and progression, and have emerged as major targets for drug discovery. Tyrosine kinase inhibitors (TKIs) inhibit corresponding kinases from phosphorylating tyrosine residues of their substrates and then block the activation of downstream signaling pathways. Ove...
Rewcastle et al., " Tyrosine Kinase Inhibitors. 3. Structure-Activity Relationships for Inhibition of Protein Tyrosine Kinases by Nuclear-Substituted Derivatives of 2,2′-Dithiobis (1-methyl-N-phenyl-1H-indole-3-carboxamide), " J. Med. Chem., 37:2033-2042, 1994....
TYROSINE KINASE INHIBITORS 来自 百度文库 喜欢 0 阅读量: 12 申请(专利)号: NO20020001820 申请日期: 2002-04-18 公开/公告号: NO20021820A 公开/公告日期: 2002-05-23 申请(专利权)人: MERCK & CO INC 发明人: PECKHAM JENNIFER P.,HOFFMAN WILLIAM F.,ARRINGTON KENNETH L.,FRALEY MARK E....
Tyrosine kinase inhibitors are small molecules that compete with the adenosine triphosphate-binding site of the catalytic domain of a tyrosine kinase. Occupation of this site inhibits autophosphorylation and activation of the tyrosine kinase, and prevents further activation of intracellular signaling pathways...
新型酪氨酸激酶抑制剂 Novel Tyrosine Kinase Inhibitors本发明提供调节酪氨酸激酶活性的式(I)的化合物,或其立体异构体,互变异构体,盐,水合物或前药,包含所述化合物的组合物和其使用方法. The present invention provides a compound to modulate the activity of tyrosine of formula (I) kinase, or a ...
Imatinib, one of the first tyrosine kinase inhibitors (TKIs) to be approved, revolutionized the treatment of chronic myelogenous leukaemia, and other TKIs with different spectra of kinase inhibition are used to treat renal cell carcinoma, non-small-cell lung cancer and colon cancer. Studies also ...
Generally, there are two classes of protein tyrosine kinase inhibitors. One type binds to the ATP binding site and the other type binds to the substrate binding site of the enzyme (Fabbro et al., 2002). An in vitro study involving the determination of inhibition of p40 protein-tyrosine kinas...
The clinical benefit of tyrosine kinase inhibitors (TKIs)-based systemic therapy for advanced hepatocellular carcinoma (HCC) is limited due to drug resistance. Here, we uncover that lipid metabolism reprogramming mediated by unconventional prefoldin RPB5 interactor (URI) endows HCC with resistance to TK...
Prior treatment with the tyrosine kinase inhibitors dasatinib and nilotinib allows stem cell transplantation (SCT) in a less advanced disease phase and doe... Schleuning et al., “Prior treatment with the tyrosine kinase inhibitors dasatinib and nilotinib allows stem cell transplantation (SCT) in a...
Human epidermal growth factor receptor 3 (HER3) Epidermal growth factor receptor-tyrosine kinase inhibitors (EGFR-TKI) Resistance Antibody Antibody-drug conjugate (ADC) Non-small cell lung cancer (NSCLC) Sorry, something went wrong. Please try again and make sure cookies are enabledCited...