title: Calreticulin transacetylase: a novel enzyme-mediated protein acetylation by acetoxy derivatives of 3-alkyl-4-methylcoumarins.
abstract: Our earlier investigations culminated in the discovery of a unique membrane-bound enzyme Calreticulin transacetylase (CRTAase) in mammalian cells catalyzing the transfer of acetyl group from polyphenolic acetates (PAs) to certain functional proteins viz. Glutathione S-transferase (GST), NADPH Cytochrome c reductase and Nitric oxide synthase (NOS) resulting in the modulation of their biological activities. In order to develop SAR study, herein, we studied the influence of alkyl group at C-3 position of acetoxy coumarins on the CRTAase activity. The alkylated acetoxy coumarins lead to inhibition of catalytic activity of GST, and ADP induced platelet aggregation by the way of activation of platelet Nitric oxide synthase (NOS). Furthermore, the increase in size of the coumarin C-3 alkyl group was found to decrease the CRTAase activity.
authors: Bioorganic Laboratory, Department of Chemistry, University of Delhi, Delhi 110 007, India.
authors: Sarah
authors: S
authors: Jalal
authors: Bioorganic Laboratory, Department of Chemistry, University of Delhi, Delhi 110 007, India.
authors: Karam
authors: K
authors: Chand
authors: Bioorganic Laboratory, Department of Chemistry, University of Delhi, Delhi 110 007, India.
authors: Abha
authors: A
authors: Kathuria
authors: Department of Biochemistry, VP Chest Institute, University of Delhi, Delhi 110 007, India.
authors: Prabhjot
authors: P
authors: Singh
authors: Department of Biochemistry, VP Chest Institute, University of Delhi, Delhi 110 007, India.
authors: Nivedita
authors: N
authors: Priya
authors: Department of Chemistry, University of Massachusetts Lowell, MA 01854, USA.
authors: Bhavna
authors: B
authors: Gupta
authors: Department of Biochemistry, VP Chest Institute, University of Delhi, Delhi 110 007, India.
authors: Hanumantharao G
authors: HG
authors: Raj
authors: Bioorganic Laboratory, Department of Chemistry, University of Delhi, Delhi 110 007, India. Electronic address: sk.sharma90@gmail.com.
authors: Sunil K
authors: SK
authors: Sharma
mesh_terms: D000107:Acetylation; D000123:Acetyltransferases / Q000378:metabolism*; D000244:Adenosine Diphosphate / Q000494:pharmacology; D000328:Adult; D001792:Blood Platelets / Q000201:enzymology; D003374:Coumarins / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D005982:Glutathione Transferase / Q000378:metabolism; D006801:Humans; D019001:Nitric Oxide Synthase / Q000037:antagonists & inhibitors / Q000378:metabolism; D010974:Platelet Aggregation / Q000187:drug effects; D010975:Platelet Aggregation Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology
chemical_list: D003374:Coumarins; D010975:Platelet Aggregation Inhibitors; D000244:Adenosine Diphosphate; D019001:Nitric Oxide Synthase; D000123:Acetyltransferases; C539012:calreticulin transacetylase, human; D005982:Glutathione Transferase