scholarly journals Fmoc Solid-Phase Peptide Synthesis of Human alfa-Calcitonin Gene-Related Peptide and Two Fluorescent Analogs

2015 ◽  
Author(s):  
M. Fuente-Moreno ◽  
A. Oddo ◽  
M. Sheykhzade ◽  
D.S. Pickering ◽  
P.R. Hansen
Keyword(s):  
Peptide Synthesis ◽  
Solid Phase ◽  
Solid Phase Peptide Synthesis ◽  
Calcitonin Gene Related Peptide ◽  
Related Peptide ◽  
Calcitonin Gene

scholarly journals Fluorescent Analogues of Human α-Calcitonin Gene-Related Peptide with Potent Vasodilator Activity

2020 ◽  
Vol 21 (4) ◽  
pp. 1343 ◽  
Author(s):  
Jing Zhu ◽  
Mahdieh Dagina Pedersen ◽  
Laraib Sabbah Ahmed ◽  
Bahareh Abdolalizadeh ◽  
Anne-Sofie Grell ◽  
...  
Keyword(s):  
Solid Phase ◽  
Solid Phase Peptide Synthesis ◽  
Calcitonin Gene Related Peptide ◽  
Receptor Internalization ◽  
Cgrp Receptor ◽  
Nociceptive Transmission ◽  
Related Peptide ◽  
Calcitonin Gene ◽  
Potent Vasodilator ◽  
Fluorescent Analogues

Human α-calcitonin gene-related peptide (h-α-CGRP) is a highly potent vasodilator peptide that belongs to the family of calcitonin peptides. There are two forms of CGRP receptors in humans and rodents: α-CGRP receptor predominately found in the cardiovascular system and β-CGRP receptor predominating in the gastrointestinal tract. The CGRP receptors are primarily localized to C and Aδ sensory fibers, where they are involved in nociceptive transmission and migraine pathophysiology. These fibers are found both peripherally and centrally, with extensive perivascular location. The CGRP receptors belong to the class B G-protein-coupled receptors, and they are primarily associated to signaling via Gα proteins. The objectives of the present work were: (i) synthesis of three single-labelled fluorescent analogues of h-α-CGRP by 9-fluorenylmethyloxycarbonyl (Fmoc)-based solid-phase peptide synthesis, and (ii) testing of their biological activity in isolated human, mouse, and rat arteries by using a small-vessel myograph setup. The three analogues were labelled with 5(6)-carboxyfluorescein via the spacer 6-aminohexanoic acid at the chain of Lys24 or Lys35. Circular dichroism (CD) experiments were performed to obtain information on the secondary structure of these fluorescently labelled peptides. The CD spectra indicated that the folding of all three analogues was similar to that of native α-CGRP. The three fluorescent analogues of α-CGRP were successfully prepared with a purity of >95%. In comparison to α-CGRP, the three analogues exhibited similar efficacy, but different potency in producing a vasodilator effect. The analogue labelled at the N-terminus proved to be the most readily synthesized, but it was found to possess the lowest vasodilator potency. The analogues labelled at Lys35 or Lys24 exhibited an acceptable reduction in potency (i.e., 3–5 times and 5–10 times less potent, respectively), and thus they have potential for use in further investigations of receptor internalization and neuronal reuptake.

Stimulation of calcitonin gene-related peptide synthesis and release

2004 ◽  
Vol 22 (9) ◽  
pp. 1819-1829 ◽  
Author(s):  
Pan-Yue Deng ◽  
Feng Ye ◽  
Wei-Jun Cai ◽  
Gui-Shan Tan ◽  
Chang-Ping Hu ◽  
...  
Keyword(s):  
Peptide Synthesis ◽  
Calcitonin Gene Related Peptide ◽  
Related Peptide ◽  
Calcitonin Gene ◽  
Stimulation Of

Biphasic effects of orchidectomy on calcitonin gene-related peptide synthesis and release

Neuroreport ◽  
2001 ◽  
Vol 12 (16) ◽  
pp. 3497-3502 ◽  
Author(s):  
Chao Sun ◽  
Mingzhe Chen ◽  
Jieming Mao ◽  
Xian Wang
Keyword(s):  
Peptide Synthesis ◽  
Calcitonin Gene Related Peptide ◽  
Related Peptide ◽  
Calcitonin Gene

Monoklonale Antikörper gegen CGRP oder den CGRP-Rezeptor in der Migräneprophylaxe

2020 ◽  
Vol 39 (07/08) ◽  
pp. 490-494
Author(s):  
Borries Kukowski
Keyword(s):  
Monoklonale Antikörper ◽  
Calcitonin Gene Related Peptide ◽  
Related Peptide ◽  
Calcitonin Gene

ZUSAMMENFASSUNGDie Charakterisierung von calcitonin gene-related peptide (CGRP) als Schlüsselmolekül in der Pathophysiologie der Migräne hat nicht nur unser Verständnis der Erkrankung, sondern auch die Entwicklung neuer Therapien vorangetrieben. Seit kurzem steht mit den monoklonalen Antikörpern gegen CGRP oder den CGRP-Rezeptor eine spezifische und hoch selektive Option für die medikamentöse Prophylaxe der episodischen und chronischen Migräne zur Verfügung, die in zahlreichen klinischen Studien ihre Überlegenheit gegenüber Placebo belegt hat. Hier werden Erfahrungen aus dem praktischen Behandlungsalltag zur kurz- und mittelfristigen Wirksamkeit und Verträglichkeit mitgeteilt und weitere Aspekte wie Therapiewechsel bei Non-Response, Verlauf nach Therapieende und die Frage des Wirkungsortes unter Einbeziehung bereits publizierter Daten angesprochen.

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