Title : Modifications of the pyroglutamic acid and histidine residues in thyrotropin-releasing hormone (TRH) yield analogs with selectivity for TRH receptor type 2 over type 1.

Pub. Date : 2007 Jan 1

PMID : 17035026






4 Functional Relationships(s)
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1 Modifications of the pyroglutamic acid and histidine residues in thyrotropin-releasing hormone (TRH) yield analogs with selectivity for TRH receptor type 2 over type 1. Pyrrolidonecarboxylic Acid thyrotropin releasing hormone Homo sapiens
2 Modifications of the pyroglutamic acid and histidine residues in thyrotropin-releasing hormone (TRH) yield analogs with selectivity for TRH receptor type 2 over type 1. Pyrrolidonecarboxylic Acid thyrotropin releasing hormone Homo sapiens
3 Modifications of the pyroglutamic acid and histidine residues in thyrotropin-releasing hormone (TRH) yield analogs with selectivity for TRH receptor type 2 over type 1. Pyrrolidonecarboxylic Acid thyrotropin releasing hormone Homo sapiens
4 For example, the most selective agonist of the series 13, in which pGlu is replaced with the pAad and histidine residue is substituted at the N-1 position with an isopropyl group, was found to activate TRH-R2 with a potency (EC(50)=1.9microM) but did not activate TRH-R1 (potency>100 microM); that is, exhibited >51-fold greater selectivity for TRH-R2 versus TRH-R1. Pyrrolidonecarboxylic Acid thyrotropin releasing hormone Homo sapiens