De novo design and synthesis of a mu-conotoxin KIIIA peptidomimetic

Ryan Brady, Minmin Zhang, Robert W Gable, Raymond Stanley Norton, Jonathan Bayldon Baell

Research output: Contribution to journalArticleOtherpeer-review

Abstract

mu-Conotoxin KIIIA blocks voltage-gated sodium channels and displays potent analgesic activity in mice models for pain. Structure-activity studies with KIIIA have shown that residues important for sodium channel activity are presented on an alpha-helix. Herein, we report the de novo design and synthesis of a three-residue (Lys7, Trp8, His12) peptidomimetic based on a novel diketopiperazine (DKP) carboxamide scaffold.
Original languageEnglish
Pages (from-to)4892 - 4895
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume23
Issue number17
DOIs
Publication statusPublished - 2013

Cite this

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abstract = "mu-Conotoxin KIIIA blocks voltage-gated sodium channels and displays potent analgesic activity in mice models for pain. Structure-activity studies with KIIIA have shown that residues important for sodium channel activity are presented on an alpha-helix. Herein, we report the de novo design and synthesis of a three-residue (Lys7, Trp8, His12) peptidomimetic based on a novel diketopiperazine (DKP) carboxamide scaffold.",
author = "Ryan Brady and Minmin Zhang and Gable, {Robert W} and Norton, {Raymond Stanley} and Baell, {Jonathan Bayldon}",
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De novo design and synthesis of a mu-conotoxin KIIIA peptidomimetic. / Brady, Ryan; Zhang, Minmin; Gable, Robert W; Norton, Raymond Stanley; Baell, Jonathan Bayldon.

In: Bioorganic and Medicinal Chemistry Letters, Vol. 23, No. 17, 2013, p. 4892 - 4895.

Research output: Contribution to journalArticleOtherpeer-review

TY - JOUR

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AU - Norton, Raymond Stanley

AU - Baell, Jonathan Bayldon

PY - 2013

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AB - mu-Conotoxin KIIIA blocks voltage-gated sodium channels and displays potent analgesic activity in mice models for pain. Structure-activity studies with KIIIA have shown that residues important for sodium channel activity are presented on an alpha-helix. Herein, we report the de novo design and synthesis of a three-residue (Lys7, Trp8, His12) peptidomimetic based on a novel diketopiperazine (DKP) carboxamide scaffold.

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DO - 10.1016/j.bmcl.2013.06.086

M3 - Article

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JF - Bioorganic and Medicinal Chemistry Letters

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