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


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]

SUBMITTER: Rose TM 

PROVIDER: S-EPMC2535796 | biostudies-literature | 2006 Jun

REPOSITORIES: biostudies-literature

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

Rose Tyler M TM   Prestwich Glenn D GD  

Organic letters 20060601 12


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 mo  ...[more]

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