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Synthesis and evaluation of fluorogenic substrates for phospholipase D and phospholipase C.

TitleSynthesis and evaluation of fluorogenic substrates for phospholipase D and phospholipase C.
Publication TypeJournal Article
Year of Publication2006
AuthorsRose, TM, Prestwich, GD
JournalOrg Lett
Volume8
Issue12
Pagination2575-8
Date Published2006 Jun 8
ISSN1523-7060
KeywordsBacillus cereus, Clostridium perfringens, Enzyme Activation, Fluorescent Dyes, Lysophosphatidylcholines, Phosphatidylcholines, Phospholipase D, Phosphoric Diester Hydrolases, Spider Venoms, Type C Phospholipases
Abstract

Fluorogenic analogues of phosphatidylcholine and lysophosphatidylcholine, DDPB and lysoDDPB, were synthesized by an enzyme-assisted strategy. The analogues were evaluated as substrates for phospholipases C and D and lysophospholipase D. DDPB was cleaved by bacterial and plant phospholipase D (PLD) enzymes and represents the first direct fluorogenic substrate for real-time measurement of PLD activity. Both fluorogenic substrates have potential in screening for PLD and PC-PLC inhibitors and for monitoring spatiotemporal changes in PLD activity in cells. [structure: see text]

DOI10.1021/ol060773d
Alternate JournalOrg. Lett.
PubMed ID16737317
PubMed Central IDPMC2535796
Grant ListHL 070231 / HL / NHLBI NIH HHS / United States
NS 29632 / NS / NINDS NIH HHS / United States
R01 NS029632-14 / NS / NINDS NIH HHS / United States
R01 NS029632-15 / NS / NINDS NIH HHS / United States