protein-kinase inhibitor ; PKIs WKPD
Definition: A protein kinase inhibitor is a type of enzyme inhibitor that blocks the action of one or more protein kinases. Protein kinases are enzymes that add a phosphate (PO4) group to a protein, and can modulate its function.
Protein-kinase inhibitors are generally small molecules that show competitive inhibition with respect to ATP.
Examples
tyrosine kinase inhibitors (TKIs )
References
Bogoyevitch MA. Therapeutic promise of JNK (...)
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protein kinase inhibitors
29 August 2005 -
crizotinib
10 June 2010Pfizer drug crizotinibPF-02341066 or 1066, PF-02341066, Xalkori Wikipedia
Molecular target: ALK
Definition: Crizotinib is an ALK inhibitor , ROS1 inhibitor and MET inhibitor .
Crizotinib is undergoing clinical trials testing its safety and efficacy in anaplastic large cell lymphoma, neuroblastoma, advanced non-small cell lung carcinoma (NSCLC ).
Crizotinib is an oral ALK (anaplastic lymphoma kinase) inhibitor under study in patients with advanced NSCLC carrying the echinoderm (...) -
artemisinins
31 May 2006Combinations of an artemisinin with other antimalarial drugs are now recommended treatments for Plasmodium falciparum malaria in most endemic areas.
Several individual molecules have been proposed as targets for artemisinins, in addition to the idea that artemisinins might have many targets at the same time.
Artemisinins could inhibit the parasite-encoded sarco-endoplasmic reticulum Ca(2+)-ATPase (SERCA) PfATP6. A polymorphism in the gene encoding PfATP6 is associated with in vitro (...) -
cisplatin
12 March 2006Cisplatin, a platinating agent commonly used to treat several cancers, is associated with nephrotoxicity, neurotoxicity, and ototoxicity, which has hindered its utility.
Cisplatin is similar to the bifunctional alkylating agents. It covalently binds to DNA and disrupts DNA function. After cisplatin enters the cells, the chloride ligands are replaced by water molecules. This reaction results in the formation of positively charged platinum complexes that react with the nucleophilic sites on (...) -
5-FU
12 March 20045-fluoro-2’-deoxyuridine, 5-fluorouracil, fluorouracil
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cyanamide
20 October 2003Microscopical synopsis
pseudo-Lafora bodies in liver (#6307616#) -
disulfiram
20 October 2003Microscopical synopsis
pseudo-Lafora bodies in liver (#6307616#) -
sunitinib
2 June 2009Definition: Sunitinib (marketed as Sutent, and previously known as SU11248) is an oral, small-molecule, multi-targeted receptor tyrosine kinase (RTKs) inhibitor (multiRTKs inhibitors).
Sunitinib was approved by the FDA for the treatment of renal cell carcinoma (RCC) and imatinib-resistant gastrointestinal stromal tumor (GIST) on January 26, 2006.
The concept was of a ATP analogue that would compete with ATP for binding to the catalytic site of receptor tyrosine kinases. This concept led (...) -
ACEIs
22 November 2004angiotensin-converting enzyme inhibitors
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methotrexate
28 November 2005MTX