MCHR1

MCHR1

A gene on chromosome 22q13.2 that encodes a G protein-coupled receptor and integral plasma membrane protein which binds melanin-concentrating hormone. MCHR1 can inhibit cAMP accumulation and stimulate intracellular calcium accumulation, and is probably involved in the neuronal regulation of food consumption.
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Examples of these upregulated genes include LALBA [6] (lactalbumin, alpha-), which encodes a principal milk protein that enables lactose production; CCKAR (cholecystokinin A receptor), which encodes a major physiological mediator of pancreatic enzyme secretion and smooth muscle contraction of the gallbladder and stomach; HCRTR2 [hypocretin (orexin) receptor 2], which encodes a protein involved in stimulation of food intake; MCHR1 (melanin-concentrating hormone receptor 1), which encodes a protein involved in neuronal regulation of food consumption; and DMP1 (dentin matrix acidic phosphoprotein 1), which encodes an extracellular matrix protein crucial for proper mineralization of bone and dentin (see Table 2 in the online Data Supplement).
6] Human genes: LALBA, lactalbumin, alpha-; CCKAR, cholecystokinin A receptor; HCRTR2, hypocretin (orexin) receptor 2; MCHR1, melanin-concentrating hormone receptor 1; DMP1, dentin matrix acidic phosphoprotein 1; AES, amino terminal enhancer of split; CEACAM1, carcinoembryonic antigen-related cell adhesion molecule 1 (biliary glycoprotein); SFTPB, surfactant protein B; FREM2, FRAS1 related extracellular matrix protein 2.
Our goal here was to screen our in-house synthesized compounds to discover potent and selective inhibitors of human MCHR1 and MCHR2 receptors.
Currently, we have two Phase 2b trials underway in chronic insomnia with NG2-73, and we recently announced positive first-in-human results for our MCHR1 antagonist, NGD 4715, targeted to treat obesity.
MCHR1 represents a new biological target for treating obesity and is the subject of research programs at many major pharmaceutical companies.
While the MCHR1 mechanism has been an area of high interest in the pharmaceutical community, we believe most in the industry have encountered significant obstacles to advancing drug candidates into human studies.