IndraLab

Statements


STAMBP activates MC4R. 29 / 29
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sparser
"In vitro , EC 50 for α-MSH activation of MC4R(I316S) and MC4R(I317T) are similar to the wild-type MC4R, however maximum receptor activity is reduced xref – xref ."

sparser
"Α-MSH binds and activates melanocortin 4 receptor (MC4R), resulting in an increase in cAMP, inducing the sensation of satiety."

sparser
"The mechanism of action of α-MSH-reactive IgG may include activation of MC4R by the immune complexes with α-MSH, which deregulates feeding behavior and emotions [ xref ]."

sparser
"ACTH (1–39) or α-MSH can activate MC1R, MC3R, MC4R, and MC5R ( xref ), but MC2R can only be activated by ACTH and not by α-MSH or other analogs ( xref )."

sparser
"This gut bacteria ClpB protein has been identified as a conformational antigen-mimetic of α-MSH that could activate the MC4R in the hypothalamus ultimately promoting the anorexigenic pathway [ xref ]."

sparser
"MC3R and MC4R in these neurons can be activated by α-MSH or inactivated by AgRP to exhibit negative or positive energy balance, respectively [ xref ]."

sparser
"Whereas events leading to MC4R activation by α-MSH are known, virtually nothing was known about how α-MSH action is terminated until recently, when a new processing enzyme was identified as the responsible enzyme for α-MSH inactivation ( xref and xref )."

reach
"Of interest, if synaptic plasticity is the primary means by which aMSH activates PVH MC4R neurons and causes satiety, then it would explain why alphaMSH and MC4R signaling is so necessary on the one hand, and why alphaMSH release by ARC POMC neurons is generally so insufficient on the other hand."

sparser
"The second salient feature of complete POMC deficiency that subsequently presents is the hyperphagia and severe obesity resulting from lack of MC4R activation by α-MSH."

sparser
"TTP2515 blocked AgRP inhibition of α-MSH-induced MC4-R activation; with TTP2515 α-MSH was able to activate the MC4-R even in the presence of AgRP ( xref )."

sparser
"Activation of the MC4R by α-MSH, or its synthetic analogues, generally leads to weight loss ( xref ), due to a reduction in caloric intake and an increase in energy expenditure."

sparser
"Furthermore, endogenous agonist α-MSH activates MC4R resulting in an increased intracellular cAMP level through Gαs signaling and inhibition of K + efflux through potassium channel Kir7.1, which have depolarizing effect."

sparser
"Homozygous or compound heterozygous loss-of-function mutations in POMC result in severe hyperphagia and obesity due to lack of MC4R activation by α-MSH in the hypothalamus and adrenal insufficiency due to defective ACTH synthesis in the pituitary ( xref ) Several studies in mice have investigated the interaction between glucocorticoids, the melanocortin system and insulin sensitivity."

sparser
"In summary, activation of the POMC-expressing neurons in the hypothalamic arcuate nucleus triggers the release of α-MSH, which activates MC4R at the paraventricular nucleus, leading to suppressed food intake and increased energy expenditure."

sparser
"The MC4R is activated principally by α-MSH, leading to neuronal depolarization and action potential firing, while AgRP acts as an antagonist or biased agonist promoting neuronal hyperpolarization (see below)."

sparser
"Α-MSH activates MC3-R and MC4-R equally but γ 2 -MSH has a higher affinity for MC3-R [1,2] ."

sparser
"On the other hand, α-MSH-induced MC4R activation stimulates the pertussis toxin (PTx)-sensitive GTPγS binding in a hypothalamic cell line (GT1-7 cells) suggesting that MC4R is also able to couple to G[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"

sparser
"ACTH can activate all five receptor subtypes; of the melanocortins, only ACTH activates MC2R; ACTH as well as α-MSH, β-MSH and γ-MSH activate MC1R, MC3R, MC4R and MC5R, although with varying affinities."

sparser
"Activation of the melanocortin 4 receptor (MC4R) by α-MSH is also thought to stimulate TRH gene transcription ( xref )."

sparser
"Activation of the MC4R protein by binding α-MSH results in decreased feeding and increased energy expenditure through thermogenesis, while deactivation of the MC4R protein by binding AgRP inhibits this process and therefore decreases satiety and energy expenditure [ xref ]."

sparser
"While α-MSH activates MC4R, AgRP competitively inhibits this receptor and NPY functionally antagonizes MC4R signaling."

sparser
"Here, α-MSH activates the MC4R, whereas these same receptors are inhibited by AGRP [ xref ]."

sparser
"Both mc1r and mc4r are activated by α-MSH and are involved in the control of the pigmentation and the modulation of food intake, respectively xref xref xref ."

sparser
"Α-MSH activates MC4R to increase cAMP in the neurons for sensation of satiety."

sparser
"Whether an α-MSH activation of MC4-R plays a role in the leptin-induced stimulation BAT thermogenesis remains controversial."

sparser
"Furthermore, α-MSH-induced MC4R activation has been shown to be neuroprotective, to improve memory and learning, induce neurite-like outgrowth, and affect reproduction xref xref xref xref xref xref ."

sparser
"This may involve a modulatory role of Igs on α-MSH-induced activation of the MC4-R (Lucas et al., xref ), although the exact mechanisms needs further investigation."

sparser
"The POMC derived α-melanocyte stimulating hormone (α-MSH) is an agonist and AgRP is an antagonist of the MC4R. When calories are replete, α-MSH activates MC4R to promote satiety, feeding suppression, and weight loss by energy expenditure."

reach
"However, a-MSH activates MC4R, reduces food intake, and increases energy expenditure."