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A small-molecule inhibitor of the NLRP3 inflammasome for the treatment of inflammatory diseases
TLDR
MCC950 treatment rescued neonatal lethality in a mouse model of CAPS and was active in ex vivo samples from individuals with Muckle–Wells syndrome, and is a potential therapeutic for NLRP3-associated syndromes, and a tool for further study of theNLRP3 inflammasome in human health and disease. Expand
C5a2 can modulate ERK1/2 signaling in macrophages via heteromer formation with C5a1 and β‐arrestin recruitment
TLDR
An improved understanding of C5a2 modulation of signaling in acute inflammation could be of benefit in the development of ligands for conditions such as sepsis. Expand
Discovery of functionally selective C5aR2 ligands: novel modulators of C5a signalling
TLDR
Two ligands were identified as functionally selective C5aR2 ligands, exhibiting selective recruitment of β‐arrestin 2 via C5 aR2, partial inhibition of C5A‐induced ERK1/2 activation and lipopolysaccharide‐stimulated interleukin‐6 release from human monocyte‐derived macrophages. Expand
chi-Conopeptide pharmacophore development: toward a novel class of norepinephrine transporter inhibitor (Xen2174) for pain.
TLDR
A pharmacophore model for the allosteric binding of 3 to NET is proposed and it is shown that 3 interacts with NET predominantly through amino acids in the first loop, forming a tight inverse turn presenting amino acids Tyr7, Lys8, and Leu9 in an orientation allowing for high affinity interaction with NET. Expand
C5a, but not C5a‐des Arg, induces upregulation of heteromer formation between complement C5a receptors C5aR and C5L2
TLDR
Investigation of receptor localization in transfected HEK293 cells and human monocyte‐derived macrophages suggested that C5aR‐C5L2 can form heteromers in a process enhanced by C5A, but not by C 5a‐des Arg, which may be of benefit in understanding the regulation of C5 a in acute inflammation. Expand
Conopressin-T from Conus tulipa Reveals an Antagonist Switch in Vasopressin-like Peptides*
TLDR
NMR structures of both conopressin-T and L7P analogue revealed a marked difference in the orientation of the exocyclic tripeptide that may serve as templates for the design of novel ligands with enhanced affinity for the V1a receptor. Expand
Allosteric α1-Adrenoreceptor Antagonism by the Conopeptide ρ-TIA*
TLDR
The unique allosteric antagonism of ρ-TIA resulting from its interaction with receptor residues that constitute a binding site that is distinct from that of the classical competitive α1-adrenoreceptor antagonists may allow the development of inhibitors that are highly subtype selective. Expand
Conopeptide-Derived κ-Opioid Agonists (Conorphins): Potent, Selective, and Metabolic Stable Dynorphin A Mimetics with Antinociceptive Properties.
TLDR
A conorphin agonist inhibited colonic nociceptors in a mouse tissue model of chronic visceral hypersensitivity, suggesting the potential of KOR agonists for the treatment of chronic abdominal pain. Expand
Allosteric alpha1-adrenoceptor antagonism by the conopeptide rho-TIA
TLDR
The unique allosteric antagonism of rho-TIA resulting from its interaction with receptor residues that constitute a binding site that is distinct from that of the classical competitive alpha1-adrenoreceptor antagonists may allow the development of inhibitors that are highly subtype selective. Expand
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