Receptor, Melanocortin, Type 3
Arthritis, Gouty
Receptors, Melanocortin
Receptor, Melanocortin, Type 4
alpha-MSH
Receptor, Melanocortin, Type 1
Receptor, Melanocortin, Type 2
Receptors, Corticotropin
Melanocyte-Stimulating Hormones
Agouti-Related Protein
Agouti Signaling Protein
gamma-MSH
beta-MSH
Sebaceous Gland Diseases
Hypothalamus
Arcuate Nucleus
Peptides, Cyclic
Adrenocorticotropic Hormone
Leptin
Neuropeptide Y
Cosyntropin
Long term orexigenic effect of a novel melanocortin 4 receptor selective antagonist. (1/383)
1. We designed and synthesized several novel cyclic MSH analogues and tested their affinities for cells expressing the MC1, MC3, MC4 and MC5 receptors. 2. One of the substances HS028 (cyclic [AcCys11, dichloro-D-phenylalanine14, Cys18, Asp-NH2(22)]-beta-MSH11-22) showed high affinity (Ki of 0.95nM) and high (80 fold) MC4 receptor selectivity over the MC3 receptor. HS028 thus shows both higher affinity and higher selectivity for the MC4 receptor compared to the earlier first described MC4 receptor selective substance HS014. 3. HS028 antagonised a alpha-MSH induced increase in cyclic AMP production in transfected cells expressing the MC3 and MC4 receptors, whereas it seemed to be a partial agonist for the MC1 and MC5 receptors. 4. Chronic intracerebroventricularly (i.c.v.) administration of HS028 by osmotic minipumps significantly increased both food intake and body weight in a dose dependent manner without tachyphylaxis for a period of 7 days. 5. This is the first report demonstrating that an MC4 receptor antagonist can increase food intake and body weight during chronic administration providing further evidence that the MC4 receptor is an important mediator of long term weight homeostasis. (+info)Identification and functional analysis of novel human melanocortin-4 receptor variants. (2/383)
Inactivation of the melanocortin-4 receptor (MC4-R) by gene-targeting results in mice that develop maturity-onset obesity, hyperinsulinemia, and hyperglycemia. These phenotypes resemble common forms of human obesity, which are late-onset and frequently accompanied by NIDDM. It is not clear whether sequence variation of the MC4-R gene contributes to obesity in humans. Therefore, we examined the human MC4-R gene polymorphism in 190 individuals ascertained on obesity status. Three allelic variants were identified, including two novel ones, Thr112Met and Ile137Thr. To analyze possible functional alterations, the variants were cloned and expressed in vitro and compared with the wild-type receptor. One of the novel variants, Ile137Thr, identified in an extremely obese proband (BMI 57), was found to be severely impaired in ligand binding and signaling, raising the possibility that it may contribute to development of obesity. Furthermore, our results also suggest that sequence polymorphism in the MC4-R coding region is unlikely to be a common cause of obesity in the population studied, given the low frequency of functionally significant mutations. (+info)Testing of human homologues of murine obesity genes as candidate regions in Finnish obese sib pairs. (3/383)
The human homologues of recently discovered murine obesity genes provide relevant candidates to study the genetic component of obesity in humans. We analysed the human counterparts to murine obesity genes ob, db, agouti, tub, melanocortin 4-receptor (MC4-R) and mitochondrial uncoupling proteins 2 and 3 (UCP2 and UCP3), as well as two other chromosomal regions reported to be linked to obesity-related phenotypes in restricted populations. We found no significant evidence for linkage to any analysed loci in our total study material of 105 affected sib pairs collected from the genetically homogenous population of Finland. However, several markers on 14 cM chromosomal region flanking the MC4-R gene showed sharing of alleles identical-by-descent (IBD) more frequently than expected. A selected subset of non-diabetic obese sib pairs strengthened the P values down to 0.003 in this particular region. The smallest P value (P = 0.001) was obtained with a marker D18S487 in a subgroup containing only sib pairs with one lean and one obese parent. We therefore screened seven obese subjects included in our sib pair material for sequence changes in their MC4-R gene, but no mutations of apparent causal relationship were found. In conclusion, we could not find evidence for significant contribution of the chromosomal loci corresponding to the murine single gene obesity genes for human morbid obesity, but additional studies are still needed to clarify whether DNA alterations within or adjacent to the MC4-R gene play some role. (+info)Contribution of melanocortin receptor exoloops to Agouti-related protein binding. (4/383)
Agouti-related protein (AGRP) is an endogenous antagonist of melanocortin action that functions in the hypothalamic control of feeding behavior. Although previous studies have shown that AGRP binds three of the five known subtypes of melanocortin receptor, the receptor domains participating in binding and the molecular interactions involved are presently unknown. The present studies were designed to examine the contribution of extracytoplasmic domains of the melanocortin-4 receptor (MC4R) to AGRP binding by making chimerical receptor constructs of the human melanocortin-1 receptor (MC1R; a receptor that is not inhibited by AGRP) and the human MC4R (a receptor that is potently inhibited by AGRP). Substitutions of the extracytoplasmic NH2 terminus and the first extracytoplasmic loop (exoloop) of the MC4R with homologous domains of the MC1R had no effect on AGRP (87-132) binding affinity or inhibitory activity (the ability to inhibit melanocortin-stimulated cAMP generation). In contrast, cassette substitutions of exoloops 2 and 3 of the MC4R with the homologous exoloops of the MC1R resulted in a substantial loss of AGRP binding affinity and inhibitory activity. Conversely, the exchange of exoloops 2 and 3 of the MC1R with the homologous exoloops of the MC4R was found to confer AGRP binding and inhibitory activity to the basic structure of the MC1R. Importantly, these substitutions did not affect the ability of the alpha-melanocyte stimulating hormone analogue [Nle4,D-Phe7] melanocyte stimulating hormone to bind or activate the chimeric receptors. These data indicate that exoloops 2 and 3 of the melanocortin receptors are important for AGRP binding. (+info)Altered energy balance causes selective changes in melanocortin-4(MC4-R), but not melanocortin-3 (MC3-R), receptors in specific hypothalamic regions: further evidence that activation of MC4-R is a physiological inhibitor of feeding. (5/383)
We have examined the effects of underfeeding and obesity on the density of hypothalamic melanocortin MC3 and MC4 receptors (MC3-R and MC4-R, respectively), which may mediate the hypophagic effects of alpha-melanocyte-stimulating hormone (MSH) in the rat. MC3-R and MC4-R were measured by quantitative autoradiography in brain sections using 125I-labeled Nle4-D-Phe7-alpha-MSH (125I-NDP-MSH) and discriminated by masking MC3-R with excess unlabelled gamma2-MSH. High densities of MC4-R occurred in the ventromedial (VMH) and arcuate (ARC) nuclei, median eminence (ME), and medial habenular nucleus (MHb), with lower densities in the dorsomedial hypothalamus (DMH) and forebrain regions. MC3-R were confined to the VMH, ARC, and MHb. After 10-days of food restriction (14% weight loss), density of MC4-R was significantly increased by 20-65% in the VMH, ARC, ME, and DMH, with no changes elsewhere. Similarly, obese (fa/fa) Zucker rats showed 43-98% increases in MC4-R in the same regions. By contrast, rats with diet-induced obesity (18% heavier than controls) showed significantly decreased binding to MC4-R, especially in the VMH, ARC, and ME. MC3-R showed no significant alterations in any model. We suggest that increased density of MC4-R with food restriction and in obese Zucker rats reflects receptor upregulation secondary to decreased release of alpha-MSH, consistent with increased hunger in these models. Conversely, downregulation of MC4-R in diet-induced obesity may indicate increased alpha-MSH secretion in an attempt to limit overeating. This alpha-MSH/MC4-R system may be inhibited by leptin and/or insulin. MC3-R are not apparently involved in regulating feeding. (+info)Conformation of the core sequence in melanocortin peptides directs selectivity for the melanocortin MC3 and MC4 receptors. (6/383)
Melanocortin peptides regulate a variety of physiological processes. Five melanocortin receptors (MC-R) have been cloned and the MC3R and MC4R are the main brain MC receptors. The aim of this study was to identify structural requirements in both ligand and receptor that determine gamma-melanocyte-stimulating hormone (MSH) selectivity for the MC3R versus the MC4R. Substitution of Asp10 in [Nle4]Lys-gamma2-MSH for Gly10 from [Nle4]alpha-MSH, increased both activity and affinity for the MC4R while the MC3R remained unaffected. Analysis of chimeric MC3R/MC4Rs and mutant MC4Rs showed that Tyr268 of the MC4R mainly determined the low affinity for [Nle4]Lys-gamma2-MSH. The data demonstrate that Asp10 determines selectivity for the MC3R, however, not through direct side chain interactions, but probably by influencing how the melanocortin core sequence is presented to the receptor-binding pocket. This is supported by mutagenesis of Tyr268 to Ile in the MC4R which increased affinity and activity for [Nle4]Lys-gamma2-MSH, but decreased affinity for two peptides with constrained cyclic structure of the melanocortin core sequence, MT-II and [D-Tyr4]MT-II, that also displayed lower affinity for the MC3R. This study provides a general concept for peptide receptor selectivity, in which the major determinant for a selective receptor interaction is the conformational presentation of the core sequence in related peptides to the receptor-binding pocket. (+info)Anatomy of an endogenous antagonist: relationship between Agouti-related protein and proopiomelanocortin in brain. (7/383)
Agouti-related protein (AGRP) is a recently discovered orexigenic neuropeptide that inhibits the binding and action of alpha-melanocyte-stimulating hormone derived from proopiomelanocortin (POMC) at the melanocortin 3 receptor (MC3R) and melanocortin 4 receptor (MC4R) and has been proposed to function primarily as an endogenous melanocortin antagonist. To better understand the interplay between the AGRP and melanocortin signaling systems, we compared their nerve fiber distributions with each other by immunohistochemistry and their perikarya distribution with MC3R and MC4R by double in situ hybridization. Although deriving from distinct cell groups, AGRP and melanocortin terminals project to identical brain areas. Both AGRP and melanocortin neurons selectively express the MC3R, which provides a neuroanatomical basis for a dual-input circuit with biological amplification and feedback inhibition. These studies highlight a broader complexity in POMC-mediated behavior in the brain. (+info)Type I beta-turn conformation is important for biological activity of the melanocyte-stimulating hormone analogues. (8/383)
In order to define which structure of alpha-melanocyte-stimulating hormone (MSH) analogues plays a critical role for ligand-receptor interaction and selectivity, we analysed receptor-binding and cAMP-generating activity in Chinese hamster ovary cell lines stably transfected with rMC3R and hMC4R, as well as the NMR structures of chemically synthesized alpha-MSH analogues. Compared with [Ahx4]alpha-MSH, the linear MTII designated as alpha-MSH-ND revealed a preference for the MC4R, whereas its IC50 and EC50 values were comparable to those of MTII reported previously. Truncation of Ahx4 and Asp5 of alpha-MSH-ND remarkably decreased the receptor-binding and cAMP-generating activity. Meanwhile, maximum cAMP-generating activity was observed at a higher concentration (10(-5) M) of alpha-MSH-ND(6-10), and MC4R preference was changed into MC3R preference. In contrast, [Gln6]alpha-MSH-ND(6-10) lost its cAMP-generating activity almost completely, even though it bound to both receptors. Whereas the solution conformation of alpha-MSH-ND revealed a stable type I beta-turn structure, [Gln6]alpha-MSH-ND(6-10) revealed a tight gamma-turn composed of Gln6-D-Phe7-Arg8. Replacement of the His6 residue of alpha-MSH-ND by Gln, Asn, Arg or Lys decreased not only the receptor binding, but also the cAMP-generating activity in both the MC3R and the MC4R. The structure of [Gln6]alpha-MSH-ND exhibited a stable type I' beta-turn comprising Asp5, Gln6, D-Phe7 and Arg8. [Lys6]alpha-MSH-ND showed a greatly reduced binding affinity and cAMP-generating activity with the loss of MC4R selectivity. In NMR studies, [Lys6]alpha-MSH-ND also demonstrated a gamma-turn conformation around Lys6-DPhe7-Arg8. From the above results, we conclude that a type I beta-turn conformation comprising the residues Asp5-His6-(D-Phe7)-Arg8 was important for receptor binding and activation, as well as the selectivity of MSH analogues. (+info)A melanocortin receptor (MCR) is a type of G protein-coupled receptor that binds melanocortin peptides. The melanocortin system plays crucial roles in various biological processes such as pigmentation, energy homeostasis, sexual function, and inflammation.
The melanocortin receptor type 3 (MC3R) is one of the five subtypes of MCRs (MC1R to MC5R). It is widely expressed in the central nervous system, including the hypothalamus, and is involved in the regulation of energy balance, feeding behavior, and body weight.
The endogenous ligands for MC3R include α-melanocyte stimulating hormone (α-MSH) and adrenocorticotropic hormone (ACTH), which are derived from the precursor protein proopiomelanocortin (POMC). Activation of MC3R by these ligands leads to a decrease in food intake and an increase in energy expenditure, contributing to weight loss. However, the exact mechanisms through which MC3R modulates these physiological functions are not yet fully understood.
Gouty arthritis is a type of inflammatory arthritis that occurs due to the buildup of uric acid crystals in the joints. Uric acid is a waste product that is formed when the body breaks down purines, which are substances found naturally in the body and in certain foods such as organ meats, anchovies, sardines, and beer.
In people with gouty arthritis, uric acid levels in the blood become elevated, leading to the formation of sharp, needle-like crystals that can accumulate in the joints, causing pain, inflammation, and swelling. The symptoms of gouty arthritis typically occur suddenly and may include:
* Intense pain in the affected joint, often occurring at night
* Redness, warmth, and swelling in the affected area
* Stiffness and limited mobility in the affected joint
The most commonly affected joint is the big toe, but gouty arthritis can also occur in other joints such as the ankles, knees, wrists, and fingers. Over time, repeated episodes of gouty arthritis can lead to joint damage and chronic pain. Treatment typically involves medications to reduce inflammation and manage pain, as well as lifestyle changes to lower uric acid levels in the body.
Melanocortin receptors (MCRs) are a group of G protein-coupled receptors that bind melanocortin peptides, which include α-, β-, and γ-melanocyte stimulating hormones (MSH) and adrenocorticotropic hormone (ACTH). These receptors are involved in a variety of physiological processes, including pigmentation, energy homeostasis, sexual function, and inflammation. There are five subtypes of melanocortin receptors (MCR1-5) that are expressed in different tissues and have distinct functions.
MCR1 is primarily expressed in melanocytes and plays a crucial role in skin and hair pigmentation. Activation of MCR1 by α-MSH leads to the production and distribution of eumelanin, which results in darker skin and hair.
MCR2 is widely expressed in the central nervous system (CNS) and peripheral tissues, including the adrenal gland, testis, and ovary. It is involved in various functions such as sexual function, feeding behavior, and energy homeostasis.
MCR3 is primarily expressed in the adrenal gland and plays a critical role in the regulation of steroid hormone production and release. Activation of MCR3 by ACTH leads to the synthesis and secretion of cortisol and other steroid hormones.
MCR4 is widely expressed in the CNS, peripheral tissues, and immune cells. It is involved in various functions such as energy homeostasis, feeding behavior, sexual function, and inflammation.
MCR5 is primarily expressed in the testis and plays a role in spermatogenesis and fertility.
Overall, melanocortin receptors are important regulators of various physiological processes, and dysregulation of these receptors has been implicated in several diseases, including obesity, metabolic disorders, and skin disorders.
A melanocortin receptor (MCR) is a type of G protein-coupled receptor that binds melanocortin peptides. The melanocortin system plays crucial roles in various biological processes such as pigmentation, energy homeostasis, sexual function, and inflammation.
The melanocortin receptor 4 (MC4R) is one of the five subtypes of MCRs, which is widely expressed in the central nervous system, including the hypothalamus, and some peripheral tissues. MC4R is a key component in the regulation of energy balance, appetite, and body weight. Activation of MC4R by melanocortin peptides, such as α-melanocyte stimulating hormone (α-MSH), leads to decreased food intake and increased energy expenditure, while antagonism or deficiency of MC4R results in obesity.
In summary, the medical definition of 'Receptor, Melanocortin, Type 4' is a G protein-coupled receptor that binds melanocortin peptides and plays a critical role in regulating energy balance, appetite, and body weight.
Alpha-MSH (α-MSH) stands for alpha-melanocyte stimulating hormone. It is a peptide hormone that is produced in the pituitary gland and other tissues in the body. Alpha-MSH plays a role in various physiological processes, including:
1. Melanin production: Alpha-MSH stimulates melanin production in the skin, which leads to skin tanning.
2. Appetite regulation: Alpha-MSH acts as a appetite suppressant by signaling to the brain that the stomach is full.
3. Inflammation and immune response: Alpha-MSH has anti-inflammatory effects and helps regulate the immune response.
4. Energy balance and metabolism: Alpha-MSH helps regulate energy balance and metabolism by signaling to the brain to increase or decrease food intake and energy expenditure.
Alpha-MSH exerts its effects by binding to melanocortin receptors, specifically MC1R, MC3R, MC4R, and MC5R. Dysregulation of alpha-MSH signaling has been implicated in various medical conditions, including obesity, anorexia nervosa, and certain skin disorders.
A melanocortin receptor (MCR) is a type of G protein-coupled receptor that binds melanocortin peptides. The melanocortin-1 receptor (MC1R) is one of five known subtypes of MCRs (MC1R-MC5R).
The MC1R is primarily expressed in melanocytes, which are pigment-producing cells located in the skin, hair follicles, and eyes. This receptor plays a crucial role in determining the type of melanin that is produced in response to environmental stimuli such as UV radiation.
Activation of the MC1R by its endogenous ligands, including α-melanocyte-stimulating hormone (α-MSH) and adrenocorticotropic hormone (ACTH), leads to the activation of adenylate cyclase and an increase in intracellular cAMP levels. This results in the activation of protein kinase A and the phosphorylation of key transcription factors, which ultimately promote the expression of genes involved in melanin synthesis.
Mutations in the MC1R gene have been associated with various pigmentation disorders, including red hair color, fair skin, and an increased risk of developing skin cancer. Additionally, polymorphisms in the MC1R gene have been linked to an increased risk of developing other diseases such as obesity and type 2 diabetes.
A melanocortin type 2 receptor (MC2R) is a G protein-coupled receptor that binds melanocortin peptides such as adrenocorticotropic hormone (ACTH). It is primarily expressed in the adrenal gland, specifically in the zona fasciculata of the cortex. Upon activation by ACTH, MC2R stimulates the production and release of steroid hormones, particularly cortisol, through the cAMP signaling pathway. Dysfunction in this receptor can lead to various endocrine disorders such as congenital adrenal hyperplasia and Cushing's disease.
Corticotropin receptors are a type of cell surface receptor that bind to the hormone corticotropin (also known as adrenocorticotropic hormone or ACTH). These receptors are found in various tissues throughout the body, including the adrenal glands.
There are two main types of corticotropin receptors, known as melanocortin receptor 1 (MC1R) and melanocortin receptor 2 (MC2R). MC2R is the primary receptor for corticotropin in the adrenal glands. When corticotropin binds to this receptor, it stimulates the production and release of steroid hormones, such as cortisol, which help regulate metabolism, immune response, and stress response.
Abnormalities in corticotropin receptors have been implicated in several medical conditions, including certain endocrine disorders and skin pigmentation disorders.
Melanocyte-stimulating hormones (MSH) are a group of peptide hormones that originate from the precursor protein proopiomelanocortin (POMC). They play crucial roles in various physiological processes, including pigmentation, energy balance, and appetite regulation.
There are several types of MSH, but the most well-known ones include α-MSH, β-MSH, and γ-MSH. These hormones bind to melanocortin receptors (MCRs), which are found in various tissues throughout the body. The binding of MSH to MCRs triggers a series of intracellular signaling events that ultimately lead to changes in cell behavior.
In the context of skin physiology, α-MSH and β-MSH bind to melanocortin 1 receptor (MC1R) on melanocytes, which are the cells responsible for producing pigment (melanin). This binding stimulates the production and release of eumelanin, a type of melanin that is brown or black in color. As a result, increased levels of MSH can lead to darkening of the skin, also known as hyperpigmentation.
Apart from their role in pigmentation, MSH hormones have been implicated in several other physiological processes. For instance, α-MSH has been shown to suppress appetite and promote weight loss by binding to melanocortin 4 receptor (MC4R) in the hypothalamus, a region of the brain that regulates energy balance. Additionally, MSH hormones have been implicated in inflammation, immune response, and sexual function.
Overall, melanocyte-stimulating hormones are a diverse group of peptide hormones that play important roles in various physiological processes, including pigmentation, energy balance, and appetite regulation.
Agouti-related protein (AGRP) is a neuropeptide that functions as an endogenous antagonist of melanocortin receptors, specifically MC3R and MC4R. It is expressed in the hypothalamus and plays a crucial role in regulating energy balance, body weight, and glucose homeostasis. AGRP increases food intake and decreases energy expenditure by inhibiting melanocortin signaling in the hypothalamus. Dysregulation of AGRP has been implicated in various metabolic disorders, including obesity and type 2 diabetes.
Agouti signaling protein (ASP) is a protein that in humans is encoded by the ASIP gene. It is a paracrine signaling molecule that regulates melanin synthesis in the hair follicle and plays a critical role in determining coat color in mammals. ASP binds to and antagonizes the melanocortin-1 receptor (MC1R), which is a G protein-coupled receptor found on the surface of melanocytes, the cells that produce melanin.
When ASP binds to MC1R, it inhibits the activation of adenylyl cyclase and reduces the intracellular levels of cAMP, which in turn leads to a decrease in eumelanin (black or brown) production and an increase in pheomelanin (yellow or red) production. This switch in melanin synthesis results in a banded coat pattern, as seen in the agouti mouse and some other mammals.
In addition to its role in coat color determination, ASP has been implicated in various physiological processes, including energy homeostasis, appetite regulation, and inflammation. Dysregulation of ASP function has been associated with obesity, metabolic disorders, and certain types of cancer.
Gamma-MSH (Gamma-Melanocyte Stimulating Hormone) is a type of melanocyte stimulating hormone that is produced in the human body. It is a tripeptide, consisting of four amino acids (His-Phe-Arg-Trp), and is a cleavage product of the proopiomelanocortin (POMC) peptide.
Gamma-MSH plays a role in regulating pigmentation in the skin by stimulating melanin production in melanocytes, which are specialized cells found in the skin. It also has been shown to have potential effects on appetite regulation and energy balance, as well as anti-inflammatory and neuroprotective properties. However, its precise physiological roles and therapeutic potentials remain an area of ongoing research.
I'm sorry for any confusion, but "hair color" is not a term that has a medical definition in the same way that a term like "myocardial infarction" (heart attack) does. Hair color can be described in various ways, such as being a natural hair color (like blonde, brunette, red, or black) or describing a change in hair color due to factors like aging (gray or white hairs) or hair dye usage.
However, it's worth noting that changes in hair color can sometimes be associated with certain medical conditions. For example, premature graying of the hair before the age of 30 can be a feature of certain genetic disorders or vitamin B12 deficiency. Similarly, some skin conditions like alopecia areata or vitiligo can cause patchy changes in hair color. But these associations don't provide a medical definition for 'hair color'.
Beta-MSH (beta-melanocyte-stimulating hormone) is a neuropeptide that is a cleavage product of the proopiomelanocortin (POMC) protein. It plays a role in regulating melanin production in the skin and has been found to have appetite suppressant effects, making it a target for obesity research. Beta-MSH acts as an agonist at melanocortin receptors MC3R and MC4R, which are involved in energy balance and feeding behavior.
Sebaceous gland diseases refer to conditions that affect the sebaceous glands, which are small glands in the skin that produce an oily substance called sebum. Sebum helps keep the skin and hair moisturized. Sebaceous gland diseases can cause a variety of symptoms, including skin inflammation, redness, pain, and the formation of bumps or cysts.
Some common types of sebaceous gland diseases include:
1. Acne: A common skin condition that occurs when the hair follicles become plugged with oil and dead skin cells, leading to whiteheads, blackheads, or pimples.
2. Seborrheic dermatitis: A skin condition that causes red, itchy, and flaky skin, often on the scalp, face, or chest.
3. Rosacea: A chronic skin condition that causes redness, pimples, and visible blood vessels on the face.
4. Sebaceous hyperplasia: A benign growth of the sebaceous glands that appears as a small, yellowish bump on the skin.
5. Sebaceous adenitis: A rare inflammatory disease that affects the sebaceous glands, causing hair loss and scaly skin.
6. Sebaceous carcinoma: A rare and aggressive form of skin cancer that develops in the sebaceous glands.
Treatment for sebaceous gland diseases depends on the specific condition and its severity. Treatments may include topical or oral medications, light therapy, or surgical removal of affected tissue. It is important to consult a healthcare provider for an accurate diagnosis and treatment plan.
The medical definition of "eating" refers to the process of consuming and ingesting food or nutrients into the body. This process typically involves several steps, including:
1. Food preparation: This may involve cleaning, chopping, cooking, or combining ingredients to make them ready for consumption.
2. Ingestion: The act of taking food or nutrients into the mouth and swallowing it.
3. Digestion: Once food is ingested, it travels down the esophagus and enters the stomach, where it is broken down by enzymes and acids to facilitate absorption of nutrients.
4. Absorption: Nutrients are absorbed through the walls of the small intestine and transported to cells throughout the body for use as energy or building blocks for growth and repair.
5. Elimination: Undigested food and waste products are eliminated from the body through the large intestine (colon) and rectum.
Eating is an essential function that provides the body with the nutrients it needs to maintain health, grow, and repair itself. Disorders of eating, such as anorexia nervosa or bulimia nervosa, can have serious consequences for physical and mental health.
The hypothalamus is a small, vital region of the brain that lies just below the thalamus and forms part of the limbic system. It plays a crucial role in many important functions including:
1. Regulation of body temperature, hunger, thirst, fatigue, sleep, and circadian rhythms.
2. Production and regulation of hormones through its connection with the pituitary gland (the hypophysis). It controls the release of various hormones by producing releasing and inhibiting factors that regulate the anterior pituitary's function.
3. Emotional responses, behavior, and memory formation through its connections with the limbic system structures like the amygdala and hippocampus.
4. Autonomic nervous system regulation, which controls involuntary physiological functions such as heart rate, blood pressure, and digestion.
5. Regulation of the immune system by interacting with the autonomic nervous system.
Damage to the hypothalamus can lead to various disorders like diabetes insipidus, growth hormone deficiency, altered temperature regulation, sleep disturbances, and emotional or behavioral changes.
The arcuate nucleus is a part of the hypothalamus in the brain. It is involved in the regulation of various physiological functions, including appetite, satiety, and reproductive hormones. The arcuate nucleus contains two main types of neurons: those that produce neuropeptide Y and agouti-related protein, which stimulate feeding and reduce energy expenditure; and those that produce pro-opiomelanocortin and cocaine-and-amphetamine-regulated transcript, which suppress appetite and increase energy expenditure. These neurons communicate with other parts of the brain to help maintain energy balance and reproductive function.
Cyclic peptides are a type of peptides in which the N-terminus and C-terminus of the peptide chain are linked to form a circular structure. This is in contrast to linear peptides, which have a straight peptide backbone with a free N-terminus and C-terminus. The cyclization of peptides can occur through various mechanisms, including the formation of an amide bond between the N-terminal amino group and the C-terminal carboxylic acid group (head-to-tail cyclization), or through the formation of a bond between side chain functional groups.
Cyclic peptides have unique structural and chemical properties that make them valuable in medical and therapeutic applications. For example, they are more resistant to degradation by enzymes compared to linear peptides, which can increase their stability and half-life in the body. Additionally, the cyclic structure allows for greater conformational rigidity, which can enhance their binding affinity and specificity to target molecules.
Cyclic peptides have been explored as potential therapeutics for a variety of diseases, including cancer, infectious diseases, and neurological disorders. They have also been used as tools in basic research to study protein-protein interactions and cell signaling pathways.
Pigmentation, in a medical context, refers to the coloring of the skin, hair, or eyes due to the presence of pigment-producing cells called melanocytes. These cells produce a pigment called melanin, which determines the color of our skin, hair, and eyes.
There are two main types of melanin: eumelanin and pheomelanin. Eumelanin is responsible for brown or black coloration, while pheomelanin produces a red or yellow hue. The amount and type of melanin produced by melanocytes can vary from person to person, leading to differences in skin color and hair color.
Changes in pigmentation can occur due to various factors such as genetics, exposure to sunlight, hormonal changes, inflammation, or certain medical conditions. For example, hyperpigmentation refers to an excess production of melanin that results in darkened patches on the skin, while hypopigmentation is a condition where there is a decreased production of melanin leading to lighter or white patches on the skin.
Adrenocorticotropic Hormone (ACTH) is a hormone produced and released by the anterior pituitary gland, a small endocrine gland located at the base of the brain. ACTH plays a crucial role in the regulation of the body's stress response and has significant effects on various physiological processes.
The primary function of ACTH is to stimulate the adrenal glands, which are triangular-shaped glands situated on top of the kidneys. The adrenal glands consist of two parts: the outer cortex and the inner medulla. ACTH specifically targets the adrenal cortex, where it binds to specific receptors and initiates a series of biochemical reactions leading to the production and release of steroid hormones, primarily cortisol (a glucocorticoid) and aldosterone (a mineralocorticoid).
Cortisol is involved in various metabolic processes, such as regulating blood sugar levels, modulating the immune response, and helping the body respond to stress. Aldosterone plays a vital role in maintaining electrolyte and fluid balance by promoting sodium reabsorption and potassium excretion in the kidneys.
ACTH release is controlled by the hypothalamus, another part of the brain, which produces corticotropin-releasing hormone (CRH). CRH stimulates the anterior pituitary gland to secrete ACTH, which in turn triggers cortisol production in the adrenal glands. This complex feedback system helps maintain homeostasis and ensures that appropriate amounts of cortisol are released in response to various physiological and psychological stressors.
Disorders related to ACTH can lead to hormonal imbalances, resulting in conditions such as Cushing's syndrome (excessive cortisol production) or Addison's disease (insufficient cortisol production). Proper diagnosis and management of these disorders typically involve assessing the function of the hypothalamic-pituitary-adrenal axis and addressing any underlying issues affecting ACTH secretion.
Skin pigmentation is the coloration of the skin that is primarily determined by two types of melanin pigments, eumelanin and pheomelanin. These pigments are produced by melanocytes, which are specialized cells located in the epidermis. Eumelanin is responsible for brown or black coloration, while pheomelanin produces a red or yellow hue.
The amount and distribution of melanin in the skin can vary depending on genetic factors, age, sun exposure, and various other influences. Increased production of melanin in response to UV radiation from the sun helps protect the skin from damage, leading to darkening or tanning of the skin. However, excessive sun exposure can also cause irregular pigmentation, such as sunspots or freckles.
Abnormalities in skin pigmentation can result from various medical conditions, including albinism (lack of melanin production), vitiligo (loss of melanocytes leading to white patches), and melasma (excessive pigmentation often caused by hormonal changes). These conditions may require medical treatment to manage or improve the pigmentation issues.
Leptin is a hormone primarily produced and released by adipocytes, which are the fat cells in our body. It plays a crucial role in regulating energy balance and appetite by sending signals to the brain when the body has had enough food. This helps control body weight by suppressing hunger and increasing energy expenditure. Leptin also influences various metabolic processes, including glucose homeostasis, neuroendocrine function, and immune response. Defects in leptin signaling can lead to obesity and other metabolic disorders.
Appetite regulation refers to the physiological and psychological processes that control and influence the desire to eat food. This complex system involves a variety of hormones, neurotransmitters, and neural pathways that work together to help maintain energy balance and regulate body weight. The hypothalamus in the brain plays a key role in appetite regulation by integrating signals from the digestive system, fat cells, and other organs to adjust feelings of hunger and fullness.
The hormones leptin and ghrelin are also important regulators of appetite. Leptin is released from fat cells and acts on the hypothalamus to suppress appetite and promote weight loss, while ghrelin is produced in the stomach and stimulates appetite and promotes weight gain. Other factors that can influence appetite regulation include stress, emotions, sleep patterns, and cultural influences.
Abnormalities in appetite regulation can contribute to the development of eating disorders such as anorexia nervosa, bulimia nervosa, and binge eating disorder, as well as obesity and other health problems. Understanding the mechanisms of appetite regulation is an important area of research for developing effective treatments for these conditions.
Neuropeptide Y (NPY) is a neurotransmitter and neuropeptide that is widely distributed in the central and peripheral nervous systems. It is a member of the pancreatic polypeptide family, which includes peptide YY and pancreatic polypeptide. NPY plays important roles in various physiological functions such as energy balance, feeding behavior, stress response, anxiety, memory, and cardiovascular regulation. It is involved in the modulation of neurotransmitter release, synaptic plasticity, and neural development. NPY is synthesized from a larger precursor protein called prepro-NPY, which is post-translationally processed to generate the mature NPY peptide. The NPY system has been implicated in various pathological conditions such as obesity, depression, anxiety disorders, hypertension, and drug addiction.
Cosyntropin is a synthetic form of adrenocorticotropic hormone (ACTH) that is used in medical testing to assess the function of the adrenal glands. ACTH is a hormone produced and released by the pituitary gland that stimulates the production and release of cortisol, a steroid hormone produced by the adrenal glands.
Cosyntropin is typically administered as an injection, and its effects on cortisol production are measured through blood tests taken at various time points after administration. This test, known as a cosyntropin stimulation test or ACTH stimulation test, can help diagnose conditions that affect the adrenal glands, such as Addison's disease or adrenal insufficiency.
It is important to note that while cosyntropin is a synthetic form of ACTH, it is not identical to the natural hormone and may have slightly different effects on the body. Therefore, it should only be used under the supervision of a healthcare professional.
Intraventricular injections are a type of medical procedure where medication is administered directly into the cerebral ventricles of the brain. The cerebral ventricles are fluid-filled spaces within the brain that contain cerebrospinal fluid (CSF). This procedure is typically used to deliver drugs that target conditions affecting the central nervous system, such as infections or tumors.
Intraventricular injections are usually performed using a thin, hollow needle that is inserted through a small hole drilled into the skull. The medication is then injected directly into the ventricles, allowing it to circulate throughout the CSF and reach the brain tissue more efficiently than other routes of administration.
This type of injection is typically reserved for situations where other methods of drug delivery are not effective or feasible. It carries a higher risk of complications, such as bleeding, infection, or damage to surrounding tissues, compared to other routes of administration. Therefore, it is usually performed by trained medical professionals in a controlled clinical setting.
Leptin receptors are cell surface receptors that bind to and respond to the hormone leptin. These receptors are found in various tissues throughout the body, including the hypothalamus in the brain, which plays a crucial role in regulating energy balance and appetite. Leptin is a hormone produced by adipose (fat) tissue that signals information about the size of fat stores to the brain. When leptin binds to its receptors, it activates signaling pathways that help regulate energy intake and expenditure, body weight, and glucose metabolism.
There are several subtypes of leptin receptors (LEPR), including LEPRa, LEPRb, LEPC, and LEPD. Among these, the LEPRb isoform is the most widely expressed and functionally important form. Mutations in the gene encoding the leptin receptor can lead to obesity, hyperphagia (excessive hunger), and impaired energy metabolism, highlighting the importance of this receptor in maintaining energy balance and overall health.
Melanocortin 4 receptor
Cat coat genetics
Melanocortin 1 receptor
Agouti-signaling protein
Red hair
Melanocortin 2 receptor accessory protein
Melanocyte
Nicotine
Raymond C. Stevens
Chromosome 21
Microphthalmia-associated transcription factor
Ocular albinism type 1
Proopiomelanocortin
Adipose tissue
Inverse agonist
MRAP2
Polyphagia
Ligand (biochemistry)
Dark skin
Melanocortin
Human skin color
Rhodopsin-like receptors
Melanocortin 3 receptor
List of MeSH codes (D12.776.543)
KCNA3
Common raccoon dog
Evolution
MRNA surveillance
Gyrfalcon
ACTH receptor
Mc4r<sup>m1Hubr</sup> (melanocortin 4 receptor; ENU induced mutation 1, Hubr) - Rat...
Melanocortin 4 receptor - Wikipedia
JCI - Motivational valence is determined by striatal melanocortin 4 receptors
Frontiers | The role of Neurochemicals, Stress Hormones and Immune System in the Positive Feedback Loops between Diabetes,...
Effect of vertical sleeve gastrectomy in melanocortin receptor 4-deficient rats.
Haplosufficiency of the melanocortin-4 receptor gene in individuals with deletions of 18q<...
Arthritic diseases: melanocortin type 3 receptor agonists as potential therapeutics : WestminsterResearch
RYTM - Rhythm Pharmaceuticals, Inc. Stock Price and Quote
Publications
Neuroscience - Publications - Albert Einstein College of Medicine
Insulin resistance and type 2 diabetes in children
Jeffrey E. Pessin - Publications - Albert Einstein College of Medicine
Melanocortin (MC) Receptors
Obesity Treatment & Management: Approach Considerations, Patient Screening, Assessment, and Expectations, Weight-Loss Goals
Michel BOUVIER - La recherche - Université de Montréal
Samreen, S.<...
Skill Checkup: Woman Gains Weight After Diet and Exercise
Association between the DNA methylations of POMC, MC4R, and HNF4A and metabolic profiles in the blood of children aged 7-9...
Items for Psychology in 2007 : Sussex Research Online
Role of the paraventricular nucleus of the hypothalamus in the sympathoexcitatory effects of leptin<...
Type V atherosclerotic lesion (Concept Id: C4703477) - MedGen - NCBI
PDF) The role of retinal photoreceptors in the regulation of circadian rhythms
Evolution of melanocortin receptors in teleost fish: the melanocortin type 1 receptor - Institut de Génomique Fonctionnelle de...
FDA Approvals, Highlights, and Summaries
Genome-Wide Association Studies of Estimated Fatty Acid Desaturase Activity in Serum and Adipose Tissue in Elderly Individuals:...
검색결과 - koreascholar
Mc1r (melanocortin 1 receptor) - Rat Genome Database
The Roles of Bacterial Products, Lipopolysaccharides and Bacteriocins, in Obesity and its Related Complications
Búsqueda | BVS Bolivia
Evo and Proud: Is eye color sex-linked?
Mc4r14
- Melanocortin 4 receptor (MC4R) is a melanocortin receptor that in humans is encoded by the MC4R gene. (wikipedia.org)
- It encodes the MC4R protein, a G protein-coupled receptor (GPCR) that binds α-melanocyte stimulating hormone (α-MSH). (wikipedia.org)
- Among the 16 genes, the analysis identified two for which rare mutations are known to cause monogenic obesity: MC4R and PCSK1 (proprotein convertase subtilisin/kexin type 1). (wikipedia.org)
- In humans, partial loss of melanocortin receptor-4 (MC4R) activity is the most common monogenic correlate of obesity regardless of lifestyle. (duke.edu)
- Following VSG, we analyzed body weight, food intake, glucose sensitivity, and macronutrient preference of wild-type and MC4R-deficient (Mc4r(+/-) and Mc4r(-/-)) rats compared with sham-operated controls. (duke.edu)
- The melanocortin-4 receptor (MC4R) is a seven, transmembrane G-protein-coupled receptor whose ligand, α-melanocyte-stimulating hormone (α-MSH), is a post-translational derivative of pro-opiomelanocortin (POMC). (psu.edu)
- 4 receptor (MC4R) agonist setmelanotide as a treatment option in rare obesity syndromes. (eurospe.org)
- 5 Mutations in leptin (LEP) and its receptor (LEPR), melanocortin 4 receptor (MC4R), pro-opiomelanocortin (POMC), prohormone convertase 1 (PCSK1), brain-derived neurotrophic factor (BDNF), neurotrophic tyrosine kinase receptor type 2 (NTRK2), and single-minded homolog 1 (SIM1) have all been shown to influence appetite and weight gain. (bariatrictimes.com)
- 7,8 MC4R is a receptor in this axis, and POMC encodes the precursor polypeptide that acts on this receptor, which must first be processed by PCSK1. (bariatrictimes.com)
- 5,9 BDNF, its receptor NTRK2, and SIM1 are known downstream targets of MC4R signaling, yet their exact actions are still being elucidated. (bariatrictimes.com)
- Patients with mutations in MC4R have undergone weight loss surgery, including Roux-en-Y gastric bypass, sleeve gastrectomy, and gastric banding. (bariatrictimes.com)
- 3 In patients with heterozygous MC4R mutations, reported results were comparable to wild type MC4R patients, with 60 percent excess weight loss reported following gastric bypass and 48 percent excess weight loss reported following gastric banding, although these results are from small cohorts. (bariatrictimes.com)
- PMID 22869321 ] Common polymorphism near the MC4R gene is associated with type 2 diabetes: data from a meta-analysis of 123,373 individuals. (snpedia.com)
- A well-studied example of this is melanocortin 4 receptor (MC4R), mutations in which are the most common cause of human monogenic obesity. (inforang.com)
Obesity15
- Obesity accelerated the age-related reduction of T-cell receptor (TCR) excision circle bearing peripheral lymphocytes, an index of recently generated T cells from thymus. (nih.gov)
- Furthermore, the obesity induced by melanocortin 4 receptor deficiency also constricted the T-cell repertoire diversity, recapitulating the thymic defects observed with diet-induced obesity. (nih.gov)
- In accordance with the above, MC4 receptor agonists have garnered interest as potential treatments for obesity and insulin resistance, while MC4 receptor antagonists have attracted interest as potential treatments for cachexia. (wikipedia.org)
- Soon after the introduction of atypical antipsychotics, which antagonize serotonin receptors and dopamine D 2 receptors (D 2 R), numerous case reports appeared showing that the use of these drugs were associated with increased obesity and the development of type 2 diabetes mellitus (T2DM) ( 5 ). (frontiersin.org)
- In patients with type 2 diabetes mellitus who are overweight or obese, antidiabetic medications that have additional actions to promote weight loss (such as glucagonlike peptide-1 [GLP-1] analogs or sodium-glucose-linked transporter-2 [SGLT-2] inhibitors) are suggested, in addition to the first-line agent for type 2 diabetes mellitus and obesity, metformin. (medscape.com)
- Recently, the FDA approved tirzepatide , glucose-dependent insulinotropic polypeptide (GIP) receptor and GLP-1 receptor agonist, for chronic weight maintenance in adults with obesity. (medscape.com)
- In this review, we will consider obesity with special attention to adipocyte types, microbiota, and microbial products, LPS and bacteriocins. (heraldopenaccess.us)
- Depression and obesity are strongly interrelated: The occurrence of one increases the risk of the other [4]. (heraldopenaccess.us)
- Obesity is a prominent risk factor for Non-insulin Dependent Diabetes Mellitus, (NIDDM), which is also called diabetes mellitus type II. (heraldopenaccess.us)
- The hyperphagia and resulting obesity manifesting in individuals with BBS are associated with impaired signaling in the central melanocortin pathway of the hypothalamus, which is a critical component in the control of energy intake and expenditure [ 11 , 12 ]. (biomedcentral.com)
- Investigation into the causes and pathogenesis of this pandemic have revealed several monogenic forms of obesity, including syndromic disorders, such as Prader Willi and Bardet Biedl syndromes and nonsyndromic disorders, which are largely confined to the leptin-melanocortin pathway. (bariatrictimes.com)
- Liver and adipose (fat) tissues in the rodents showed no evidence of fatty liver disease, a complication related to poor diet, obesity and type 2 diabetes. (sciencedaily.com)
- The familiar results of this stress are obesity, type 2 diabetes and cardiovascular complications. (sciencedaily.com)
- Mouse models of cell type-specific cilia dysgenesis have subsequently demonstrated that ciliary defects restricted to specific hypothalamic neurons are sufficient to induce obesity and hyperphagia. (inforang.com)
- A potential mechanism underlying hypothalamic neuron cilia-related obesity is impaired ciliary localization of G protein-coupled receptors involved in the regulation of appetite and energy metabolism. (inforang.com)
Protein-coupled receptors2
- The research program focuses on the molecular mechanisms controlling the function of the largest family of drug targets, the G protein-coupled receptors (GPCR). (umontreal.ca)
- Most tmACs are principally controlled by G protein coupled receptors via direct activation by heterotrimeric G proteins either by direct connection between tmACs and the G s subunit or subunits [1]. (bioinf.org)
Agonists5
- And agonists of the MC4 receptor such as melanotan II and PF-00446687, via activation of the central oxytocin system, have been found to promote pair bond formation in prairie voles and, due to these prosocial effects, have been suggested as possible treatments for social deficits in autism spectrum disorders and schizophrenia. (wikipedia.org)
- In obese patients with type 2 diabetes mellitus who require insulin therapy, at least one of the following is suggested: metformin, pramlintide, or GLP-1 agonists to mitigate associated weight gain due to insulin. (medscape.com)
- Glucagon-like peptide-1 (GLP-1) agonists have been shown to promote weight loss in patients with or without type 2 diabetes and are the Food and Drug Administration (FDA)-approved for chronic weight management . (medscape.com)
- Melanocortin-4 receptor agonists are approved for weight management in patients with rare genetic conditions (ie, proopiomelanocortin, proprotein convertase subtilisin/kexin type 1, and leptin receptor deficiencies). (medscape.com)
- cAMP microdomains were first appreciated in the 1970s from the groups of Keely Hayes Brunton and others when they identified that different tmAC activating hormones (e.g. β-adrenergic receptor and prostaglandin E1 agonists) all led to cAMP elevation but each induced unique cellular events in cardiomyocytes e.g. only β-adrenergic activation induced improved contractility and glycogen rate of metabolism [12]. (bioinf.org)
MC1R2
- Spontaneous alleles of a few key pigmentation loci are known to cause melanism in domestic or laboratory populations of mammals, but in natural populations, mutations at one gene, the melanocortin-1 receptor (Mc1r), have been implicated in the vast majority of cases, possibly due to its minimal pleiotropic effects. (gephebase.org)
- To date, the melanocortin 1 receptor (MC1R) is the only gene identified that explains substantial phenotypic variance in human pigmentation. (ncl.ac.uk)
Hypothalamus1
- 6,7 Leptin is a hormone secreted by adipose tissue which, when bound to its receptor in the arcuate nucleus of the hypothalamus, signals satiety through the melanocortin axis. (bariatrictimes.com)
Ionotropic Glutamate Receptors1
- Blockade of paraventricular melanocortin 3/4 receptors with SHU9119 or ionotropic glutamate receptors with kynurenate, alone or together, each partially reversed the effects of leptin, implicating increased activation of glutamate and melanocortin 3/4 receptors. (elsevierpure.com)
Gene6
- PMID 21736789 ] A variant near the melanocortin-4 receptor gene regulates postprandial lipid metabolism in a healthy Caucasian population. (snpedia.com)
- Evaluation of platelet reactivity during combined antiplatelet therapy in patients with stable coronary artery disease in relation to diabetes type 2 and the GPIIB/IIIA receptor gene polymorphism. (cdc.gov)
- A Bayesian analysis for investigating the association between rs13266634 polymorphism in SLC30A8 gene and type 2 diabetes. (cdc.gov)
- Glutathione S-transferases gene polymorphism influence on the age of diabetes type 2 onset. (cdc.gov)
- This gene provides instructions for making a protein called the melanocortin 1 receptor, which is involved in the pathway that produces melanin. (medlineplus.gov)
- Molecular defects of the ACTH receptor gene, consisting of point mutations, are described in approximately 25-40% of patients with FGD. (medscape.com)
Pathway2
- BBS genes are required for leptin receptor (LEPR) trafficking, a key component of the melanocortin pathway. (biomedcentral.com)
- Since the discovery of two leptin deficient children in 1997, investigations into these disorders have focused on the Leptin-Melanocortin pathway and its regulation of appetite and energy homeostasis. (bariatrictimes.com)
Paraventricular nucleus2
- Conversely, although blockade of neuropeptide Y Y1 receptors in the paraventricular nucleus increased LSNA, mean arterial pressure, and heart rate, these responses were prevented by intracerebroventricular or arcuate nucleus injections of leptin, suggesting that, at least in part, leptin also increases sympathetic nerve activity by suppression of tonic neuropeptide Y inhibitory inputs from the arcuate nucleus. (elsevierpure.com)
- Injection of the melanocortin 3/4 receptor agonist melanotan-II into the paraventricular nucleus increased LSNA, mean arterial pressure, and heart rate only after blockade of neuropeptide Y Y1 receptors. (elsevierpure.com)
Mutations2
- Mutations in the MC2 receptor accessory protein (MRAP) are responsible for another estimated 15-20% of cases of FGD. (medscape.com)
- these mutations may affect ACTH signal transduction, expression of the ACTH receptor, or differentiation of the adrenal cortex. (medscape.com)
Leptin receptor1
- Under normal conditions, leptin binds the leptin receptor on proopiomelanocortin (POMC) neurons, and POMC is then cleaved by the protein encoded by PCSK1 . (biomedcentral.com)
Agonist setmelanotide1
- The structures of the receptor in complex with the agonist setmelanotide and the antagonist SHU9119 have been determined. (wikipedia.org)
Insulin Resistance1
- Insulin resistance (IR) has been identified as a cardinal trigger of impaired glucose metabolism, T2D, and cardiovascular diseases [ 3 , 4 ]. (e-apem.org)
Antigen1
- Thus, Zfx restrains the stress response and couples antigen receptor signaling to B cell expansion and maintenance during development and peripheral homeostasis. (gsea-msigdb.org)
20203
- The selective 5-HT 2C receptor agonist lorcaserin was approved by the FDA in 2012 but was taken off the market in 2020 because of potential cancer risk. (medscape.com)
- Primary care diabetes 2020 9 15 (1): 4-9. (cdc.gov)
- Endokrynologia Polska 2020 71 (4): 334-342. (cdc.gov)
Diabetes mellitus5
- Type 2 diabetes mellitus (T2DM) and depression are significant public health and socioeconomic issues. (frontiersin.org)
- Angiotensin-converting enzyme (ACE) inhibitors, angiotensin receptor blockers (ARBs), and calcium channel blockers, rather than beta-adrenergic blockers, should be considered as first-line therapy for hypertension in patients with type 2 diabetes mellitus who are obese. (medscape.com)
- In recent decades, the world has seen expanding waistlines in expanding numbers, and with this, an increased prevalence of metabolic syndrome, a collection of risk factors predisposing toward cardiovascular disease (CVD) and type 2 diabetes mellitus (T2DM). (bariatrictimes.com)
- Association between PPARGC1A single nucleotide polymorphisms and increased risk of nonalcoholic fatty liver disease among Iranian patients with type 2 diabetes mellitus. (cdc.gov)
- Autoimmune thyroiditis in patients with type 1 diabetes mellitus: A long-term follow-up study. (cdc.gov)
Antagonist1
- Novel hybrid compounds, opioid agonist+melanocortin 4 receptor antagonist, as efficient analgesics in mouse neuropathic pain model. (physiciansweekly.com)
Lorcaserin1
- The BLOOM-DM study was a 1-year RCT in Type 2 diabetics taking metformin or SU, or both, comparing placebo with 10 mg lorcaserin daily (q.d.) versus lorcaserin 10 mg twice daily (b.i.d. (medscape.com)
Middle-aged1
- In middle-aged humans, progressive adiposity with or without type 2 diabetes also compromised thymic output. (nih.gov)
20192
- The MC4 receptor agonist bremelanotide (PT-141), sold under the brand name Vyleesi, was approved in the United States as a treatment for low sexual desire in women in 2019. (wikipedia.org)
- Turkish journal of medical sciences 2019 08 49 (4): 1089-1094. (cdc.gov)
Regulation2
- In mouse models, MC4 receptors have been found to be involved in feeding behaviour, the regulation of metabolism, sexual behaviour, and male erectile function. (wikipedia.org)
- GLP-1 is a physiologic regulator of appetite and calorie intake, and the GLP-1 receptor is present in several areas of the brain involved in appetite regulation. (medscape.com)
Selective5
- The non-selective melanocortin receptor agonist afamelanotide (NDP-α-MSH) has been found to induce brain-derived neurotrophic factor (BDNF) expression in the rodent brain via activation of the MC4 receptor and mediate "intense" neurogenesis and cognitive recovery in an animal model of Alzheimer's disease. (wikipedia.org)
- The effect of the selective human MC3 receptor agonist PG992 on high density human chondrocyte micromass cultures activated by IL-1beta. (westminster.ac.uk)
- Additionally, other selective 5-HT 2C receptors were withdrawn from the market as well owing to unwanted effects, such as higher risk for cardiac valvular abnormalities . (medscape.com)
- Here we describe a model system, SELective Expression and Controlled Transduction In Vivo (SELECTIV), that enables efficient and specific expression of transgenes by coupling adeno-associated virus (AAV) vectors with Cre-inducible overexpression of the multi-serotype AAV receptor, AAVR. (nature.com)
- Arena Pharmaceuticals, CA, USA), approved in June 2012 by the FDA but still under review by the EMA, is a selective agonist at the G-protein coupled 5HT 2c receptor. (medscape.com)
Neurons1
- In particular her research is focused on how different cell types in the brain (neurons, microglia, astrocytes and endothelial cells) coordinate and interact to regulate these processes. (exeter.ac.uk)
POMC1
- Activation of this receptor has previously been shown to decrease hunger and increase satiety, [ 89 ] the mechanism of which has been proposed to be by increasing pro-opiomelanocortin (POMC) expression with subsequent increased release of α-melanocyte stimulating hormone, which stimulates the anorexigenic melanocortin 4 receptor. (medscape.com)
Hormone3
- Therefore, identification of novel endogenous targets for drug development may have beneficial properties ACTH4-10, a heptapeptide fragment derived from the hormone adrenocorticotrophin (ACTH) modulates the inflammatory response in a corticosterone-independent manner, via agonism at melanocortin type 3 receptors (MC3-R) expressed on peritoneal macrophages. (westminster.ac.uk)
- Enables hormone binding activity and melanocortin receptor activity. (mcw.edu)
- tmACs provide an important link between hormonal (e.g. melanocortin revitalizing hormone) signals and intracellular processes. (bioinf.org)
Defect2
- One theory suggests that lipid over supply leads to defect in Insulin Receptor Substrate (IRS) through serine/threonine phosphorylation. (heraldopenaccess.us)
- In 1977, Spark and Etzkorn proposed an etiology involving a defect at the ACTH receptor or a postreceptor site. (medscape.com)
Intake1
- The his- Bariatric surgery reduces the size of the stomach, increases tory of dietary supplements is full of success stories in terms the feeling of fullness, and reduces the amount of food intake.8 of efficacy, but this success is matched by tragedy with regard Different types of bariatric surgery include the following: to safety. (eddoctor24h.com)
Precision Medicine1
- However, direct use of 5-HT 2C receptor positive allosteric modulators in precision medicine is currently being studied. (medscape.com)
Cancer1
- Antibodies directed against the soluble adenylyl cyclase (sAC) are highly specific markers for melanoma especially for lentigo maligna melanoma and are being described as "second generation" cancer diagnostics which are diagnostics that Kaempferol determine the 'state' of a cell and not just identify the cell type. (bioinf.org)
Genes2
- The development of transgenic mouse models that express genes of interest in specific cell types has transformed our understanding of basic biology and disease. (nature.com)
- The type and amount of melanin in hair is determined by many genes, although little is known about most of them. (medlineplus.gov)
Expression4
- Our approach exploits the absolute dependence of AAV transduction on the expression of its receptor 22 , AAVR (also named KIAA0319L). (nature.com)
- By directing AAV transduction through the regulated expression of its receptor, the approach provides precise control over which cells express the AAV-vectored transgene. (nature.com)
- We hypothesized that AAV transgene expression could be targeted to specific tissues or cell types by selectively overexpressing AAVR. (nature.com)
- T. J. Park, S. S. Choi, G. A. Gang, Y. Kim, High-Level Expression and Purification of the Second Transmembrane Domain of Wild-Type and Mutant Human Melanocortin-4 Receptor for Solid-State NMR Structural Studies, Protein Expression and Purification, Volume 62, (Issue 2), December 2008, Pages 139-145. (praiseworthyprize.org)
Genetic3
- Genome-wide trans-ancestry meta-analysis provides insight into the genetic architecture of type 2 diabetes susceptibility. (snpedia.com)
- Development and Standardization of an Improved Type 1 Diabetes Genetic Risk Score for Use in Newborn Screening and Incident Diagnosis. (cdc.gov)
- This type of genetic change is described as loss-of-function. (medlineplus.gov)
Lymphocytes1
- The development, homeostasis and function of B lymphocytes involve multiple rounds of B cell receptor (BCR)-controlled proliferation and prolonged maintenance. (gsea-msigdb.org)
Glucose1
- In addition, there is evidence that fatty acids interfere with very early stages of Glucose Transporter Type 4 (GLUT4) and hexokinase II activity [8]. (heraldopenaccess.us)
Increases1
- We demonstrate that transgenic AAVR overexpression greatly increases the efficiency of transduction of many diverse cell types, including muscle stem cells, which are normally refractory to AAV transduction. (nature.com)
Publication1
- Scholars@Duke publication: Effect of vertical sleeve gastrectomy in melanocortin receptor 4-deficient rats. (duke.edu)