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Neuropeptide Y Receptor
Neuropeptide Y receptors are a family of receptors belonging to class A G-protein coupled receptors and they are activated by the closely related peptide hormones neuropeptide Y, peptide YY and pancreatic polypeptide. These receptors are involved in the control of a diverse set of behavioral processes including appetite, circadian rhythm, and anxiety. Activated neuropeptide receptors release the Gi subunit from the heterotrimeric G protein complex. The Gi subunit in turn inhibits the production of the second messenger cAMP from ATP. Only the crystal structure of Y1 in complex with two antagonist is available. Types There are five known mammalian neuropeptide Y receptors designated Y1 through Y5. Four neuropeptide Y receptors each encoded by a different gene have been identified in humans, all of which may represent therapeutic targets for obesity and other disorders. * Y1 - * Y2 - * Y4 - * Y5 - Antagonists *BIBP-3226 *Lu AA-33810 *BIIE-0246 *UR-AK49 UR-AK49 ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Neuropeptide Y Receptor Y1
Neuropeptide Y receptor type 1 is a protein that in humans is encoded by the ''NPY1R'' gene. Selective ligands Agonists * Neuropeptide Y (endogenous agonist, non subtype selective) * Peptide YY Antagonists ;Peptide * BVD-10 (selective NPY1 antagonist, CAS# 262418-00-8) * GR-231,118 (mixed NPY1 antagonist / NPY4 agonist, CAS# 158859-98-4) ;Non-peptide * BIBO-3304 (CAS# 191868-14-1) * BIBP-3226 (CAS# 159013-54-4) * PD-160,170 (CAS# 181468-88-2) Available Structures 5ZBH(Neuropeptide Y1 bound to antagonist BMS-193835) 5ZBQ(Neuropeptide Y1 bound to antagonist UR-MK299) See also * Neuropeptide Y receptor Neuropeptide Y receptors are a family of receptors belonging to class A G-protein coupled receptors and they are activated by the closely related peptide hormones neuropeptide Y, peptide YY and pancreatic polypeptide. These receptors are invo ... References Further reading * * * * * * * * * * * * * * External links * * G protein-cou ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Heterotrimeric G Protein
Heterotrimeric G protein, also sometimes referred to as the ''"large" G proteins'' (as opposed to the subclass of smaller, monomeric small GTPases) are membrane-associated G proteins that form a heterotrimeric complex. The biggest non-structural difference between heterotrimeric and monomeric G protein is that heterotrimeric proteins bind to their cell-surface receptors, called G protein-coupled receptors, directly. These G proteins are made up of ''alpha'' (α), ''beta'' (β) and ''gamma'' (γ) subunits. The alpha subunit is attached to either a GTP or GDP, which serves as an on-off switch for the activation of G-protein. When ligands bind a GPCR, the GPCR acquires GEF ( guanine nucleotide exchange factor) ability, which activates the G-protein by exchanging the GDP on the ''alpha'' subunit to GTP. The binding of GTP to the ''alpha'' subunit results in a structural change and its dissociation from the rest of the G-protein. Generally, the ''alpha'' subunit binds membrane-boun ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
BIIE-0246
BIIE-0246 is a drug used in scientific research which acts as a potent and selective antagonist for the Neuropeptide Y receptor Y2. It was one of the first non-peptide Y2-selective antagonists developed, and remains among the most widely used tools for studying this receptor. It has been used to demonstrate a role for the Y2 subtype as a presynaptic autoreceptor limiting further neuropeptide Y release, as well as modulating dopamine and acetylcholine release. It has also been shown to produce several behavioural effects in animals, including reducing alcohol consumption in addicted rats and anxiolytic effects, although while selective Y2 agonists are expected to be useful as anorectic An anorectic or anorexic is a drug which reduces appetite, resulting in lower food consumption, leading to weight loss. By contrast, an appetite stimulant is referred to as orexigenic. The term is (from the Greek ''ἀν-'' (an-) = "without" ...s, BIIE-0246 did not appear to increase appetit ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Lu AA-33810
Lu AA-33810 is a drug developed by Lundbeck, which acts as a potent and highly selective antagonist for the Neuropeptide Y receptor Y5, with a Ki of 1.5nM and around 3300x selectivity over the related Y1, Y2 and Y4 receptors. In animal studies it produced anorectic, antidepressant and anxiolytic effects, and further research is now being conducted into its possible medical application in the treatment of eating disorder An eating disorder is a mental disorder defined by abnormal eating behaviors that negatively affect a person's physical or mental health. Only one eating disorder can be diagnosed at a given time. Types of eating disorders include binge eating ...s. References Neuropeptide Y antagonists Experimental drugs {{nervous-system-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
BIBP-3226
BIBP-3226 is a drug used in scientific research which acts as a potent and selective antagonist for both the Neuropeptide Y receptor Y1 and also the neuropeptide FF receptor. It was the first non-peptide antagonist developed for the Y1 receptor and has been widely used to help determine its functions in the body. Activation of Y1 is thought to be involved in functions such as regulation of appetite and anxiety, and BIBP-3226 has anxiogenic and anorectic effects, as well as blocking the Y1-mediated corticotropin releasing hormone release. It has also been used as a lead compound A lead compound (, i.e. a "leading" compound, not to be confused with various compounds of the metallic element lead) in drug discovery is a chemical compound that has pharmacological or biological activity likely to be therapeutically useful, but ... to develop a number of newer more potent Y1 antagonists. References Neuropeptide Y antagonists {{nervous-system-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Neuropeptide Y Receptor Y5
Neuropeptide Y receptor type 5 is a protein that in humans is encoded by the ''NPY5R'' gene. Selective ligands Agonists * Neuropeptide Y (endogenous agonist, non subtype selective) * BWX-46 (selective NPY5 agonist, CAS# 172997-92-1) * Peptide YY Antagonists * CGP-71683 (CAS# 192322-50-2) * FMS-586 * L-152,804 (CAS# 6508-43-6) * Lu AA-33810 * MK-0557 * NTNCB (CAS# 486453-65-0) * Velneperit Velneperit (S-2367) is a drug developed by Shionogi, which acts as a potent and selective antagonist An antagonist is a character in a story who is presented as the chief foe of the protagonist. Etymology The English word antagonist comes f ... (S-2367) See also * Neuropeptide Y receptor References Further reading * * * * * * * * * External links * G protein-coupled receptors {{transmembranereceptor-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Pancreatic Polypeptide Receptor 1
Pancreatic polypeptide receptor 1, also known as Neuropeptide Y receptor type 4, is a protein that in humans is encoded by the ''PPYR1'' gene. Selective Ligands Agonists * Pancreatic polypeptide * Neuropeptide Y (endogenous agonist, non subtype selective) * Peptide YY * GR-231,118 (mixed NPY1 antagonist / NPY4 agonist, CAS# 158859-98-4) Antagonists * UR-AK49 See also * Neuropeptide Y receptor Neuropeptide Y receptors are a family of receptors belonging to class A G-protein coupled receptors and they are activated by the closely related peptide hormones neuropeptide Y, peptide YY and pancreatic polypeptide. These receptors are invo ... References External links * Further reading * * * * * * * * * * * * * * * * G protein-coupled receptors {{transmembranereceptor-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Neuropeptide Y Receptor Y2
Neuropeptide Y receptor type 2 (Y2R) is a member of the neuropeptide Y receptor family of G-protein coupled receptors, that in humans is encoded by the ''NPY2R'' gene. Selective ligands Agonists * Neuropeptide Y (endogenous agonist, non subtype selective) * Neuropeptide Y fragment 13-36 (NPY2 selective agonist) * Peptide YY * Peptide YY 3-36 fragment Antagonists * BIIE-0246 (CAS# 246146-55-4) * JNJ 5207787 (CAS# 683746-68-1) * SF 11 (CAS# 443292-81-7) See also * Neuropeptide Y receptor Neuropeptide Y receptors are a family of receptors belonging to class A G-protein coupled receptors and they are activated by the closely related peptide hormones neuropeptide Y, peptide YY and pancreatic polypeptide. These receptors are invo ... References External links * Further reading * * * * * * * * * * * * * * * G protein-coupled receptors {{transmembranereceptor-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Neuropeptide Y Receptor Y1
Neuropeptide Y receptor type 1 is a protein that in humans is encoded by the ''NPY1R'' gene. Selective ligands Agonists * Neuropeptide Y (endogenous agonist, non subtype selective) * Peptide YY Antagonists ;Peptide * BVD-10 (selective NPY1 antagonist, CAS# 262418-00-8) * GR-231,118 (mixed NPY1 antagonist / NPY4 agonist, CAS# 158859-98-4) ;Non-peptide * BIBO-3304 (CAS# 191868-14-1) * BIBP-3226 (CAS# 159013-54-4) * PD-160,170 (CAS# 181468-88-2) Available Structures 5ZBH(Neuropeptide Y1 bound to antagonist BMS-193835) 5ZBQ(Neuropeptide Y1 bound to antagonist UR-MK299) See also * Neuropeptide Y receptor Neuropeptide Y receptors are a family of receptors belonging to class A G-protein coupled receptors and they are activated by the closely related peptide hormones neuropeptide Y, peptide YY and pancreatic polypeptide. These receptors are invo ... References Further reading * * * * * * * * * * * * * * External links * * G protein-cou ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Adenosine Triphosphate
Adenosine triphosphate (ATP) is an organic compound that provides energy to drive many processes in living cells, such as muscle contraction, nerve impulse propagation, condensate dissolution, and chemical synthesis. Found in all known forms of life, ATP is often referred to as the "molecular unit of currency" of intracellular energy transfer. When consumed in metabolic processes, it converts either to adenosine diphosphate (ADP) or to adenosine monophosphate (AMP). Other processes regenerate ATP. The human body recycles its own body weight equivalent in ATP each day. It is also a precursor to DNA and RNA, and is used as a coenzyme. From the perspective of biochemistry, ATP is classified as a nucleoside triphosphate, which indicates that it consists of three components: a nitrogenous base ( adenine), the sugar ribose, and the triphosphate. Structure ATP consists of an adenine attached by the 9-nitrogen atom to the 1′ carbon atom of a sugar ( ribose), which in ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Cyclic Adenosine Monophosphate
Cyclic adenosine monophosphate (cAMP, cyclic AMP, or 3',5'-cyclic adenosine monophosphate) is a second messenger important in many biological processes. cAMP is a derivative of adenosine triphosphate (ATP) and used for intracellular signal transduction in many different organisms, conveying the cAMP-dependent pathway. History Earl Sutherland of Vanderbilt University won a Nobel Prize in Physiology or Medicine in 1971 "for his discoveries concerning the mechanisms of the action of hormones", especially epinephrine, via second messengers (such as cyclic adenosine monophosphate, cyclic AMP). Synthesis Cyclic AMP is synthesized from ATP by adenylate cyclase located on the inner side of the plasma membrane and anchored at various locations in the interior of the cell. Adenylate cyclase is ''activated'' by a range of signaling molecules through the activation of adenylate cyclase stimulatory G ( Gs)-protein-coupled receptors. Adenylate cyclase is ''inhibited'' by agonists of adenylate ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Second Messenger
Second messengers are intracellular signaling molecules released by the cell in response to exposure to extracellular signaling molecules—the first messengers. (Intercellular signals, a non-local form or cell signaling, encompassing both first messengers and second messengers, are classified as autocrine, juxtacrine, paracrine, and endocrine depending on the range of the signal.) Second messengers trigger physiological changes at cellular level such as proliferation, differentiation, migration, survival, apoptosis and depolarization. They are one of the triggers of intracellular signal transduction cascades. Examples of second messenger molecules include cyclic AMP, cyclic GMP, inositol triphosphate, diacylglycerol, and calcium. First messengers are extracellular factors, often hormones or neurotransmitters, such as epinephrine, growth hormone, and serotonin. Because peptide hormones and neurotransmitters typically are biochemically hydrophilic molecules, these first ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
