Determination of the melanocortin-4 receptor structure identifies Ca2+ as a cofactor for ligand binding
The melanocortin-4 receptor (MC4R) is involved in energy homeostasis and is an important
drug target for syndromic obesity. We report the structure of the antagonist SHU9119-bound …
drug target for syndromic obesity. We report the structure of the antagonist SHU9119-bound …
The melanocortin-3 receptor is a pharmacological target for the regulation of anorexia
…, J Maldonado, P Pan, K Fowler, SY Williams… - Science translational …, 2021 - science.org
Ablation of hypothalamic AgRP (Agouti-related protein) neurons is known to lead to fatal
anorexia, whereas their activation stimulates voracious feeding and suppresses other …
anorexia, whereas their activation stimulates voracious feeding and suppresses other …
Development of an assay for high-throughput energy expenditure monitoring in the zebrafish
BJ Renquist, C Zhang, SY Williams, RD Cone - Zebrafish, 2013 - liebertpub.com
Energy homeostasis is maintained by balancing energy intake and expenditure. Many signals
regulating energy intake are conserved between the human and teleost. However, before …
regulating energy intake are conserved between the human and teleost. However, before …
High throughput Danio rerio energy expenditure assay
SY Williams, BJ Renquist - JoVE (Journal of Visualized Experiments), 2016 - jove.com
Zebrafish are an important model organism with inherent advantages that have the potential
to make zebrafish a widely applied model for the study of energy homeostasis and obesity. …
to make zebrafish a widely applied model for the study of energy homeostasis and obesity. …
Obesity‐associated mutant melanocortin‐4 receptors with normal Gαs coupling frequently exhibit other discoverable pharmacological and biochemical defects
T Gillyard, K Fowler, SY Williams… - Journal of …, 2019 - Wiley Online Library
Mutations in the melanocortin‐4 receptor (MC4R) are the most common cause of early
syndromic obesity known. Most of these mutations result in a loss of protein expression, α‐…
syndromic obesity known. Most of these mutations result in a loss of protein expression, α‐…
Development of a high throughput screen for allosteric modulators of melanocortin-4 receptor signaling using a real time cAMP assay
J Pantel, SY Williams, D Mi, J Sebag, JD Corbin… - European journal of …, 2011 - Elsevier
… Author links open overlay panel Jacques Pantel a b , Savannah Y. Williams a , Dehui Mi b c
, Julien … Zhang, JP Kane, MJ Malloy, CR Pullinger, Y. Bromberg, LA Pennacchio, R. Dent, R. …
, Julien … Zhang, JP Kane, MJ Malloy, CR Pullinger, Y. Bromberg, LA Pennacchio, R. Dent, R. …
Structure-based design of melanocortin 4 receptor ligands based on the SHU-9119-hMC4R cocrystal structure
…, LE Gimenez, SY Williams, Y Jing, Y Wu… - Journal of medicinal …, 2020 - ACS Publications
The melanocortin receptors (MC1R–MC5R) belong to class A G-protein-coupled receptors (GPCRs)
and are known to have receptor-specific roles in normal and diseased states. …
and are known to have receptor-specific roles in normal and diseased states. …
Demonstration of a Common DPhe7 to DNal(2′)7 Peptide Ligand Antagonist Switch for Melanocortin-3 and Melanocortin-4 Receptors Identifies the Systematic …
LE Gimenez, TA Noblin, SY Williams… - Journal of Medicinal …, 2022 - ACS Publications
Melanocortin peptides containing a 3-(2-naphthyl)-d-alanine residue in position 7 (DNal(2′)
7 ), reported as melanocortin-3 receptor (MC3R) subtype-specific agonists in two separate …
7 ), reported as melanocortin-3 receptor (MC3R) subtype-specific agonists in two separate …
Global drivers of change across tropical savannah ecosystems and insights into their management and conservation
… All tropical savannahs are experiencing extensive … to savannahs. Here, using a recently
published ecosystem intactness metric, we assess the current condition of tropical savannahs …
published ecosystem intactness metric, we assess the current condition of tropical savannahs …
Inhibition of the melanocortin-3 receptor (MC3R) causes generalized sensitization to anorectic agents
NS Dahir, Y Gui, Y Wu, PR Sweeney, SY Williams… - bioRxiv, 2023 - biorxiv.org
The melanocortin-3 receptor (MC3R) acts presynaptically to regulate GABA release from
agouti-related protein (AgRP) nerve terminals and thus may be a negative regulator of multiple …
agouti-related protein (AgRP) nerve terminals and thus may be a negative regulator of multiple …