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 -
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 (...) -
amiodarone
24 February 2005Definition: Amiodarone is a potent antiarrhythmic agent.
Images
Amiodarone-induced change in thyroid
https://twitter.com/aakasharmand/status/727148670987149312
cirrhosis and amiodarone
https://twitter.com/CArnold_GI/status/735956508492615682
Liver injury
Amiodarone causes elevated liver enzymes in up to 30% of patients and steatohepatitis in 1–2% of patients.
The majority of cases display liver enzyme abnormalities within 24 h of intravenous infusion.
Even low oral dosing (200 (...) -
platinum
12 June 2005The accidental discovery of the anticancer properties of cisplatin and its clinical introduction in the 1970s represent a major landmark in the history of successful anticancer drugs.
Although carboplatin—a second-generation analogue that is safer but shows a similar spectrum of activity to cisplatin—was introduced in the 1980s, the pace of further improvements slowed for many years.
However, in the past several years interest in platinum drugs has increased.
Key developments include the (...) -
COX inhibitors
15 April 2005Types
COX-1 inhibitors
COX-2 inhibitors
References
Chan TA. Prostaglandins and the colon cancer connection. Trends Mol Med. 2006 Jun;12(6):240-4. PMID: #16650804#
Marcus AJ, Broekman MJ, Pinsky DJ. COX inhibitors and thromboregulation. N Engl J Med. 2002 Sep 26;347(13):1025-6. PMID: #12324561# -
ara-C
6 June 2005arabinofuranosylcytosine, cytosine arabinoside
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HIV integrase inhibitors
12 June 2005References
Ciuffi A, Bushman FD. Retroviral DNA integration: HIV and the role of LEDGF/p75. Trends Genet. 2006 Jul;22(7):388-95. PMID: #16730094#
Pommier Y, Johnson AA, Marchand C. Integrase inhibitors to treat HIV/AIDS. Nat Rev Drug Discov. 2005 Mar;4(3):236-48. PMID: #15729361# -
anaesthetics
9 May 2005References
Rudolph U, Antkowiak B. Molecular and neuronal substrates for general anaesthetics. Nat Rev Neurosci. 2004 Sep;5(9):709-20. PMID: #15322529# -
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 (...) -
Sulindac
31 May 2007Sulindac is a nonsteroidal anti-inflammatory drug.
It has been reported to be effective in suppressing tumor growth through the induction of p21WAF1/cip1 in human, animal models of colon cancer and colon cancer cells.
The efficiency of sulindac in the inhibition of cell proliferation (other than the induction of apoptosis) may be through the suppression of beta-catenin pathway in human breast and lung cancer cell (...)
