Literature DB >> 7054169

Haloenol lactones: enzyme-activated irreversible inactivators for serine proteases. Inactivation of alpha-chymotrypsin.

P K Chakravarty, G A Krafft, J A Katzenellenbogen.   

Abstract

Two haloenol lactones have been shown to inactivate alpha-chymotrypsin by an enzyme-mediated process. According to the postulated mechanism, acylation of the active site serine by the haloenol lactone reveals an alpha-haloketone, which alkylates the enzyme at the active site and renders the enzyme inactive. The inactivation has been shown to require enzymatic activation of the inhibitor to its reactive form to take place within the acyl-enzyme intermediate and to be irreversible.

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Year:  1982        PMID: 7054169

Source DB:  PubMed          Journal:  J Biol Chem        ISSN: 0021-9258            Impact factor:   5.157


  5 in total

1.  Haloenol lactones as inactivators and substrates of aldehyde dehydrogenase.

Authors:  N Mukerjee; M Dryjanski; W Dai; J A Katzenellenbogen; R Pietruszko
Journal:  J Protein Chem       Date:  1996-10

2.  Haloenol pyranones and morpholinones as antineoplastic agents of prostate cancer.

Authors:  Jason N Mock; John P Taliaferro; Xiao Lu; Sravan Kumar Patel; Brian S Cummings; Timothy E Long
Journal:  Bioorg Med Chem Lett       Date:  2012-05-17       Impact factor: 2.823

3.  Smooth muscle cell arachidonic acid release, migration, and proliferation are markedly attenuated in mice null for calcium-independent phospholipase A2beta.

Authors:  Sung Ho Moon; Christopher M Jenkins; David J Mancuso; John Turk; Richard W Gross
Journal:  J Biol Chem       Date:  2008-10-16       Impact factor: 5.157

4.  Mechanism-based inhibition of iPLA2β demonstrates a highly reactive cysteine residue (C651) that interacts with the active site: mass spectrometric elucidation of the mechanisms underlying inhibition.

Authors:  Christopher M Jenkins; Jingyue Yang; Richard W Gross
Journal:  Biochemistry       Date:  2013-06-10       Impact factor: 3.162

5.  Characterization of FKGK18 as inhibitor of group VIA Ca2+-independent phospholipase A2 (iPLA2β): candidate drug for preventing beta-cell apoptosis and diabetes.

Authors:  Tomader Ali; George Kokotos; Victoria Magrioti; Robert N Bone; James A Mobley; William Hancock; Sasanka Ramanadham
Journal:  PLoS One       Date:  2013-08-20       Impact factor: 3.240

  5 in total

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