Corticotropin

A new human/rat CRH analogue has been synthesized using the Fmoc/tBu solid-phase synthetic protocol. The sequence ofthe new peptide differs from the original in two positions, 12 and 15, at which the native amino acids L-phenylalanine 12 and L-leucine 15 have been replaced by the nonprotein amino acids D-phenylalanine and a-aminoisobutyric acid (Aib), respectively. The high resolution three-dimensional solution structure of [D-Phe12, Aib15]CRH has been determined by 688 dis-tance constraints (656 meaningful NOE and 32 H-bonds distance limits) and 21 angle constraints. ...

11p tumor12 22-04-2013 34 3   Download

Anovel photoactivatable analog of antisauvagine-30 (aSvg-30), a specific antagonist for corticotropin-releasing factor (CRF) receptor, type 2 (CRF2), has been synthesized and characterized. TheN-terminal amino-acidD-Phe in aSvg-30 [D-Phe11,His12]Svg(11)40) was replacedbyaphenyldiazirine, the 4-(1-azi-2,2,2-trifluoroethyl)benzoyl (ATB) residue.

7p tumor12 22-04-2013 32 3   Download

The corticotropin releasing factor receptor 1 (CRFR1) belongs to the superfamily of G-protein coupled receptors. Though CRF is involved in the aetiology of several stress-relateddisorders, includingdepressionandanxiety, detailsof CRFR1 regulation such as internalization remain unchar-acterized. In the present study, agonist-induced internal-ization of CRFR1 in HEK293 cells was visualized by confocal microcopy and quantified using the radioligand 125 I-labelled sauvagine.

0p awards 05-04-2013 32 3   Download

In our continued studies on corticotropin releasing factor receptor (CRFR1) signaling in the skin, we tested functional activity of CRFR1a, e, f, g and h isoforms after transfection to COS cells.Both membrane-bound and soluble variants are translatedin vivointofinal proteinproducts that undergo further post-translational modifications.

10p dell39 03-04-2013 41 3   Download