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Combinatorial synthesis of ω‐conotoxin MVIIC analogues and their binding with N‐ and P/Q‐type calcium channels
Author(s) -
Sasaki Toru,
Kobayashi Kuniko,
Kohno Toshiyuki,
Sato Kazuki
Publication year - 2000
Publication title -
febs letters
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.593
H-Index - 257
eISSN - 1873-3468
pISSN - 0014-5793
DOI - 10.1016/s0014-5793(99)01772-x
Subject(s) - conotoxin , chemistry , calcium , biochemistry , peptide , organic chemistry
ω‐Conotoxin MVIIC (MVIIC) blocks P/Q‐type calcium channels with high affinity and N‐type calcium channels with low affinity, while the highly homologous ω‐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 ω‐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.