Analogues of human calcitonin. V. Influence of basic amino acids in positions 11, 17 and 24 on hypocalcaemic activity in the rat.
The influence of positions 11 and 24 on hypocalcaemic potency and duration of action was examined. These positions are respectively occupied by threonine and glutamine in HCT, but by the basic amino acids lysine and arginine in SCT. Replacement of threonine by lysine trebled the hypocalcaemic potency of HCT and slightly prolonged its duration of action. Substitution of arginine for glutamine reduced the activity to about one tenth. The simultaneous introduction of both basic amino acids yielded an analogue intermediate in activity between those obtained by the single substitutions. The analogue [Bmp1, Va18, Lys11, Arg24]-HCT displayed the same effects as [Lys11]-HCT.
D000595:Amino Acid Sequence; D000818:Animals; D001665:Binding Sites; D002116:Calcitonin / Q000031:analogs & derivatives* / Q000494:pharmacology; D002118:Calcium / Q000097:blood*; D004305:Dose-Response Relationship, Drug; D051381:Rats; D013329:Structure-Activity Relationship
D002116:Calcitonin; D002118:Calcium