Clinical perspectives for irreversible tyrosine kinase inhibitors in cancer
- PMID: 22885287
- DOI: 10.1016/j.bcp.2012.07.031
Clinical perspectives for irreversible tyrosine kinase inhibitors in cancer
Abstract
Irreversible inhibitors provide potent and selective inhibition of tyrosine kinase enzymes. Use of such inhibitors has proved promising in overcoming the tumor resistance encountered with reversible tyrosine kinase inhibitors. Irreversible inhibitors inactivate their protein target through covalent interaction with a nucleophilic cysteine residue within the nucleotide binding pocket of the kinase domain. Different irreversible tyrosin kinase inhibitors directed against epidermal growth factor receptor (EGFR), Bruton's tyrosine kinase (BTK), vascular endothelial growth factor receptor (VEGFR) and fibroblast growth factor receptor tyrosine kinase (FGFR) have been developed and some of them have been employed clinically as anticancer agents. This review focuses on recent preclinical and clinical progress with currently available irreversible tyrosine kinase inhibitors. The chemical structures of the candidates, structure-activity relationships, biological activities and results of current clinical investigations are described.
Copyright © 2012 Elsevier Inc. All rights reserved.
Similar articles
-
The development of Bruton's tyrosine kinase (BTK) inhibitors from 2012 to 2017: A mini-review.Eur J Med Chem. 2018 May 10;151:315-326. doi: 10.1016/j.ejmech.2018.03.062. Epub 2018 Mar 23. Eur J Med Chem. 2018. PMID: 29631132 Review.
-
Role of tyrosine kinase inhibitors in cancer therapy.J Pharmacol Exp Ther. 2005 Dec;315(3):971-9. doi: 10.1124/jpet.105.084145. Epub 2005 Jul 7. J Pharmacol Exp Ther. 2005. PMID: 16002463 Review.
-
[Tyrosine kinase inhibitors in tumor therapy--part 2. Current position and perspectives].Dtsch Med Wochenschr. 2005 Jun 10;130(23):1438-42. doi: 10.1055/s-2005-870836. Dtsch Med Wochenschr. 2005. PMID: 15929020 Review. German. No abstract available.
-
Acquired resistance to tyrosine kinase inhibitors during cancer therapy.Curr Opin Genet Dev. 2008 Feb;18(1):73-9. doi: 10.1016/j.gde.2008.01.004. Epub 2008 Mar 5. Curr Opin Genet Dev. 2008. PMID: 18325754 Review.
-
Bruton's tyrosine kinase as a drug discovery target.Drug News Perspect. 2008 Sep;21(7):357-62. doi: 10.1358/dnp.2008.21.7.1255308. Drug News Perspect. 2008. PMID: 19259548 Review.
Cited by
-
An insight into the therapeutic potential of quinazoline derivatives as anticancer agents.Medchemcomm. 2017 Apr 7;8(5):871-885. doi: 10.1039/c7md00097a. eCollection 2017 May 1. Medchemcomm. 2017. PMID: 30108803 Free PMC article. Review.
-
Targeted Therapy for Hepatocellular Carcinoma: Old and New Opportunities.Cancers (Basel). 2022 Aug 20;14(16):4028. doi: 10.3390/cancers14164028. Cancers (Basel). 2022. PMID: 36011021 Free PMC article. Review.
-
L718Q mutant EGFR escapes covalent inhibition by stabilizing a non-reactive conformation of the lung cancer drug osimertinib.Chem Sci. 2018 Feb 12;9(10):2740-2749. doi: 10.1039/c7sc04761d. eCollection 2018 Mar 14. Chem Sci. 2018. PMID: 29732058 Free PMC article.
-
Discovery of novel quinazoline derivatives bearing semicarbazone moiety as potent EGFR kinase inhibitors.Comput Struct Biotechnol J. 2018 Oct 30;16:462-478. doi: 10.1016/j.csbj.2018.10.016. eCollection 2018. Comput Struct Biotechnol J. 2018. PMID: 30455856 Free PMC article.
-
Human epidermal growth factor receptor targeted inhibitors for the treatment of ovarian cancer.Cancer Biol Med. 2018 Nov;15(4):375-388. doi: 10.20892/j.issn.2095-3941.2018.0062. Cancer Biol Med. 2018. PMID: 30766749 Free PMC article.
Publication types
MeSH terms
Substances
LinkOut - more resources
Full Text Sources
Other Literature Sources
Research Materials
Miscellaneous
