Mechanisms of Clinical Resistance to Small Molecule Tyrosine Kinase Inhibitors Targeting Oncogenic Tyrosine Kinases

2005 ◽  
Vol 5 (2) ◽  
pp. 101-112 ◽  
Author(s):  
Heiko van der Kuip ◽  
Lara Wohlbold ◽  
Carsten Oetzel ◽  
Matthias Schwab ◽  
Walter E Aulitzky
Keyword(s):  
Tyrosine Kinase ◽  
Tyrosine Kinase Inhibitors ◽  
Small Molecule ◽  
Tyrosine Kinases ◽  
Kinase Inhibitors ◽  
Clinical Resistance

Research progress in quinazoline derivatives as multi-target tyrosine kinase inhibitors

2018 ◽  
Vol 24 (1) ◽  
pp. 1-10 ◽  
Author(s):  
Hao Jin ◽  
Hu-Guang Dan ◽  
Guo-Wu Rao
Keyword(s):  
Tyrosine Kinase ◽  
Tyrosine Kinase Inhibitors ◽  
Small Molecule ◽  
Tyrosine Kinases ◽  
Kinase Inhibitors ◽  
Growth Factor Receptor ◽  
Synthetic Methods ◽  
Research Progress ◽  
Quinazoline Derivatives ◽  
Antitumor Bioactivity

Abstract Receptor tyrosine kinases (RTKs), such as epidermal growth factor receptor (EGFR), are involved in multiple human tumors. Therefore, RTKs are attractive targets for various antitumor strategies. Two classes of tyrosine kinase antagonists were applied in the clinic for monoclonal antibodies and small-molecule tyrosine kinase inhibitors. A well-studied class of small-molecule inhibitors is represented by 4-anilinoquinazolines, exemplified by gefitinib and erlotinib as mono-targeted EGFR inhibitors, which were approved for the treatment of non-small-cell lung cancer. Mono-target drugs may result in drug resistance and the innovation of multi-target drugs has grown up to be an active field. Recent advances in research on antitumor bioactivity of 4-anilino(or phenoxy)quinazoline derivatives with multiple targets are reviewed in this paper. At the same time, synthetic methods of quinazolines were introduced from the point of building the ring skeleton and based on the types of reaction.

Small molecule tyrosine kinase inhibitors and pancreatic cancer—Trials and troubles

2019 ◽  
Vol 56 ◽  
pp. 149-167 ◽  
Author(s):  
Bhaskar Venkata Kameswara Subrahmanya Lakkakula ◽  
Batoul Farran ◽  
Saikrishna Lakkakula ◽  
Sujatha Peela ◽  
Nagendra Sastry Yarla ◽  
...  
Keyword(s):  
Pancreatic Cancer ◽  
Tyrosine Kinase ◽  
Tyrosine Kinase Inhibitors ◽  
Small Molecule ◽  
Kinase Inhibitors ◽  
Cancer Trials

PXR-mediated P-glycoprotein induction by small molecule tyrosine kinase inhibitors

2013 ◽  
Vol 48 (4-5) ◽  
pp. 644-649 ◽  
Author(s):  
S. Harmsen ◽  
I. Meijerman ◽  
R.F. Maas-Bakker ◽  
J.H. Beijnen ◽  
J.H.M. Schellens
Keyword(s):  
Tyrosine Kinase ◽  
Tyrosine Kinase Inhibitors ◽  
Small Molecule ◽  
Kinase Inhibitors ◽  
P Glycoprotein

scholarly journals Small Molecule Tyrosine Kinase Inhibitors for the Treatment of Intestinal Inflammation

2011 ◽  
Vol 140 (5) ◽  
pp. S-516
Author(s):  
Maninder Sidhu ◽  
Carmen Alonso ◽  
Bayasi Guleng ◽  
SunYoung Chang ◽  
MyDoanh Chau ◽  
...  
Keyword(s):  
Tyrosine Kinase ◽  
Tyrosine Kinase Inhibitors ◽  
Small Molecule ◽  
Kinase Inhibitors ◽  
Intestinal Inflammation
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