title: Antisense homology box-derived peptides represent a new class of endothelin receptor inhibitors.
abstract: Several peptides encoded by the sense and corresponding antisense DNA have been found to recognize and bind to each other. We developed software to search for sense-antisense regions within proteins taking into account the degeneracy of the genetic code, i.e., one amino acid can have several "antisense" counterparts. Using this approach, we searched endothelin receptor type A for intramolecular regions related in sense-antisense fashion. After locating these regions (termed "antisense homology boxes"), several corresponding peptides were synthesized. The four new ET(A) receptor fragment peptides ETR-P1 ("CALSVDRYRAVASW"), ETR-P3 ("QGIGPLITAIEI"), ETR-P4 ("IADNAERYSANLSSHV") and ETR-P6 ("LNRRNGSLRIALSEHLKNRREVA") reported here can inhibit ET-1 activity.
authors.affiliation: Choju Medical Institute, Fukushimura Hospital, Toyohashi, Japan.
authors.forename: L
authors.initials: L
authors.lastname: Baranyi
authors.forename: W
authors.initials: W
authors.lastname: Campbell
authors.forename: K
authors.initials: K
authors.lastname: Ohshima
authors.forename: S
authors.initials: S
authors.lastname: Fujimoto
authors.forename: M
authors.initials: M
authors.lastname: Boros
authors.forename: J
authors.initials: J
authors.lastname: Kaszaki
authors.forename: H
authors.initials: H
authors.lastname: Okada
mesh_terms: D016475:3T3 Cells; D000595:Amino Acid Sequence; D000818:Animals; D002118:Calcium / Q000378:metabolism; D002417:Cattle; D016373:DNA, Antisense / Q000235:genetics*; D004285:Dogs; D065128:Endothelin Receptor Antagonists; D019332:Endothelin-1 / Q000097:blood / Q000378:metabolism; D006801:Humans; D066298:In Vitro Techniques; D017136:Ion Transport / Q000187:drug effects; D008297:Male; D051379:Mice; D008969:Molecular Sequence Data; D009126:Muscle Relaxation / Q000187:drug effects; D010449:Peptide Mapping; D010455:Peptides / Q000235:genetics* / Q000378:metabolism / Q000494:pharmacology*; D051381:Rats; D017208:Rats, Wistar; D044022:Receptor, Endothelin A; D017466:Receptors, Endothelin / Q000235:genetics / Q000378:metabolism; D017386:Sequence Homology, Amino Acid; D012984:Software
chemical_list: D016373:DNA, Antisense; D065128:Endothelin Receptor Antagonists; D019332:Endothelin-1; D010455:Peptides; D044022:Receptor, Endothelin A; D017466:Receptors, Endothelin; D002118:Calcium