PMID- 11554555 OWN - NLM STAT- MEDLINE DCOM- 20020219 LR - 20191210 IS - 1389-4501 (Print) IS - 1389-4501 (Linking) VI - 2 IP - 3 DP - 2001 Sep TI - Structure-function relationships of the NMDA receptor antagonist conantokin peptides. PG - 313-22 AB - The three members of the conantokin peptide family identified to date are conantokin(con)-G, -T and -R. Their defining attributes include a high relative content of gamma-carboxyglutamic acid (Gla), N-terminal sequence identity, as well as considerable overall sequence homology, and antagonism of the N-methyl-D-aspartate receptor (NMDAR). As promising templates for the design of neuroprotective agents, a thorough evaluation of structure-function relationships in these peptides will be invaluable in aiding rational drug modeling. To this end, a comprehensive assessment of the contributions of individual residues to conantokin structure and function is required. The current review summarizes recent efforts in this area, and also includes the effects of peptide length, as well as structural-stabilization and -destabilization on the structural and inhibitory profiles of an extensive panel ofconantokin derivatives. FAU - Prorok, M AU - Prorok M AD - Department of Chemistry and Biochemistry, and the W.M.Keck Center for Transgene Research, University of Notre Dame, Indiana 46556, USA. FAU - Castellino, F J AU - Castellino FJ LA - eng PT - Journal Article PT - Review PL - United Arab Emirates TA - Curr Drug Targets JT - Current drug targets JID - 100960531 RN - 0 (Conotoxins) RN - 0 (Excitatory Amino Acid Antagonists) RN - 0 (Intercellular Signaling Peptides and Proteins) RN - 0 (Mollusk Venoms) RN - 0 (Peptides) RN - 0 (Receptors, N-Methyl-D-Aspartate) RN - 0 (conantokin R) RN - 127476-26-0 (conantokin-T) RN - 93438-65-4 (conotoxin GV) SB - IM MH - Amino Acid Sequence MH - Animals MH - Conotoxins/chemistry/*pharmacology MH - Excitatory Amino Acid Antagonists/chemistry/*pharmacology MH - Humans MH - Intercellular Signaling Peptides and Proteins MH - Molecular Sequence Data MH - Mollusk Venoms/chemistry/*pharmacology MH - Peptides/chemistry/*pharmacology MH - Receptors, N-Methyl-D-Aspartate/*antagonists & inhibitors MH - Structure-Activity Relationship RF - 43 EDAT- 2001/09/14 10:00 MHDA- 2002/02/20 10:01 CRDT- 2001/09/14 10:00 PHST- 2001/09/14 10:00 [pubmed] PHST- 2002/02/20 10:01 [medline] PHST- 2001/09/14 10:00 [entrez] AID - 10.2174/1389450013348542 [doi] PST - ppublish SO - Curr Drug Targets. 2001 Sep;2(3):313-22. doi: 10.2174/1389450013348542.