Ontology highlight
ABSTRACT:
SUBMITTER: Han TS
PROVIDER: S-EPMC4074532 | biostudies-literature | 2009 Mar
REPOSITORIES: biostudies-literature
Han Tiffany S TS Zhang Min-Min MM Walewska Aleksandra A Gruszczynski Pawel P Robertson Charles R CR Cheatham Thomas E TE Yoshikami Doju D Olivera Baldomero M BM Bulaj Grzegorz G
ChemMedChem 20090301 3
Disulfide bridges that stabilize the native conformation of conotoxins pose a challenge in the synthesis of smaller conotoxin analogues. Herein we describe the synthesis of a minimized analogue of the analgesic mu-conotoxin KIIIA that blocks two sodium channel subtypes, the neuronal Na(V)1.2 and skeletal muscle Na(V)1.4. Three disulfide-deficient analogues of KIIIA were initially synthesized in which the native disulfide bridge formed between either C1-C9, C2-C15, or C4-C16 was removed. Deletion ...[more]