Bradykinin receptors: Agonists, antagonists, expression, signaling, and adaptation to sustained stimulation

F Marceau, H Bachelard, J Bouthillier, JP Fortin… - International …, 2020 - Elsevier
Bradykinin-related peptides, the kinins, are blood-derived peptides that stimulate 2 G protein–
coupled receptors, the B 1 and B 2 receptors (B 1 R, B 2 R). The pharmacologic and …

G-protein coupled receptor resensitization-appreciating the balancing act of receptor function

ML Mohan, NT Vasudevan, MK Gupta… - Current molecular …, 2012 - ingentaconnect.com
G-protein coupled receptors (GPCRs) are seven transmembrane receptors that are pivotal
regulators of cellular responses including vision, cardiac contractility, olfaction, and platelet …

Junctophilin‐4 facilitates inflammatory signalling at plasma membrane‐endoplasmic reticulum junctions in sensory neurons

A Hogea, S Shah, F Jones, CM Carver… - The Journal of …, 2021 - Wiley Online Library
Key points Rat somatosensory neurons express a junctional protein, junctophilin‐4 (JPH4)
JPH4 is necessary for the formation of store operated Ca2+ entry (SOCE) complex at the …

In Vitro Pharmacological Profile of a New Small Molecule Bradykinin B2 Receptor Antagonist

A Lesage, C Gibson, F Marceau, HD Ambrosi… - Frontiers in …, 2020 - frontiersin.org
We here report the discovery and early characterization of Compound 3, a representative of
a novel class of small molecule bradykinin (BK) B2 receptor antagonists, and its superior …

Bifunctional ligands of the bradykinin B2 and B1 receptors: An exercise in peptide hormone plasticity

F Marceau, MT Bawolak, JP Fortin, G Morissette, C Roy… - Peptides, 2018 - Elsevier
Kinins are the small and fragile hydrophilic peptides related to bradykinin (BK) and derived
from circulating kininogens via the action of kallikreins. Kinins bind to the preformed and …

Bradykinin signaling regulates solute permeability and cellular junction organization in lymphatic endothelial cells

S Kempe, G Fois, C Brunner, TK Hoffmann… - …, 2020 - Wiley Online Library
Objective Determine the effect of bradykinin on solute permeability and cellular junctional
proteins in human dermis microvascular endothelial cells. Methods Cells were characterized …

Potent antiproliferative activity of bradykinin B2 receptor selective agonist FR-190997 and analogue structures thereof: A paradox resolved?

G Rassias, S Leonardi, D Rigopoulou… - European Journal of …, 2021 - Elsevier
Βradykinin stimulation of B2 receptor is known to activate the oncogenic ERK pathway and
overexpression of bradykinin receptors B1 and B2 has been reported to occur in glioma …

Comparing pathways of bradykinin formation in whole blood from healthy volunteers and patients with hereditary angioedema due to C1 inhibitor deficiency

X Charest-Morin, J Hébert, GÉ Rivard… - Frontiers in …, 2018 - frontiersin.org
Multiple pathways have been proposed to generate bradykinin (BK)-related peptides from
blood. We applied various forms of activation to fresh blood obtained from 10 healthy …

Vascular smooth muscle contractility assays for inflammatory and immunological mediators

F Marceau, D deBlois, E Petitclerc, L Levesque… - International …, 2010 - Elsevier
The blood vessels are one of the important target tissues for the mediators of inflammation
and allergy; further cytokines affect them in a number of ways. We review the use of the …

Prolonged signalling and trafficking of the bradykinin B2 receptor stimulated with the amphibian peptide maximakinin: insight into the endosomal inactivation of kinins

MT Bawolak, C Roy, L Gera, F Marceau - Pharmacological research, 2012 - Elsevier
Maximakinin, a 19-residue peptide from the amphibian Bombina maxima, incorporates the
full sequence of bradykinin (BK) at its C-terminus with a hydrophilic 10-residue N-terminal …