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Combinatorial Synthesis of Omega-Conotoxin MVIIC Analogues and Their Binding With N- And P/Q-type Calcium Channels

Combinatorial Synthesis of Omega-Conotoxin MVIIC Analogues and Their Binding With N- And P/Q-type Calcium Channels

T Sasaki, K Kobayashi, T Kohno, K Sato

FEBS Lett. 2000 Jan 21;466(1):125-9.

PMID: 10648826

Abstract:

Omega-conotoxin MVIIC (MVIIC) blocks P/Q-type calcium channels with high affinity and N-type calcium channels with low affinity, while the highly homologous omega-conotoxin MVIIA blocks only N-type calcium channels. We wished to obtain MVIIC analogues more selective for P/Q-type calcium channels than MVIIC to elucidate structural differences among the channels, which discriminate the omega-conotoxins. To prepare a number of MVIIC analogues efficiently, we developed a combinatorial method which includes a random air oxidation step. Forty-seven analogues were prepared in six runs and some of them exhibited higher selectivity for P/Q-type calcium channels than MVIIC in binding assays.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP147794238	ω-Conotoxin MVIIC		147794-23-8	Price

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