Role of the guanidine group in the N-terminal fragment of PTH(1-11).
A series of PTH hybrids containing a diamine [NH(2)(CH(2))(n)NH(2); n = 4, 5, 6] in the C-terminal position was synthesized based on the H-Aib-Val-Aib-Glu-Ile-Gln-Leu-Nle-His-Gln-Har-NH(2) (Har = homoarginine) template. The compounds were pharmacologically characterized at PTH1R receptors for agonist activity.
Caporale
Andrea
A
Department of Chemical Sciences, Institute of Biomolecular Chemistry, CNR, University of Padova, via Marzolo 1, 35131, Padua, Italy. caporaleandrea74@gmail.com
Woznica
Iwona
I
Schievano
Elisabetta
E
Mammi
Stefano
S
Peggion
Evaristo
E
D000595:Amino Acid Sequence; D000596:Amino Acids / Q000737:chemistry; D000621:Aminoisobutyric Acids / Q000737:chemistry; D002460:Cell Line; D002942:Circular Dichroism; D003959:Diamines / Q000737:chemistry*; D004305:Dose-Response Relationship, Drug; D015195:Drug Design; D017930:Genes, Reporter; D019791:Guanidine / Q000737:chemistry*; D006709:Homoarginine / Q000031:analogs & derivatives* / Q000737:chemistry; D006801:Humans; D018716:Molecular Mimicry; D008970:Molecular Weight; D009646:Norleucine / Q000737:chemistry; D009842:Oligopeptides / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D010281:Parathyroid Hormone / Q000819:agonists / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D010446:Peptide Fragments / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D044168:Receptor, Parathyroid Hormone, Type 1 / Q000819:agonists / Q000235:genetics; D013329:Structure-Activity Relationship
D000596:Amino Acids; D000621:Aminoisobutyric Acids; D003959:Diamines; D009842:Oligopeptides; D010281:Parathyroid Hormone; D010446:Peptide Fragments; D044168:Receptor, Parathyroid Hormone, Type 1; C454802:parathyroid hormone (1-11); D006709:Homoarginine; D009646:Norleucine; D019791:Guanidine