CRHR2
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CRHR2
Corticotropin-releasing hormone receptor 2 (CRHR2) is a protein, also known by the IUPHAR-recommended name CRF2, that is encoded by the CRHR2 gene and occurs on the surfaces of some mammalian cells. CRF2 receptors are type 2 G protein-coupled receptors for corticotropin-releasing hormone (CRH) that are resident in the plasma membranes of hormone-sensitive cells. CRH, a peptide of 41 amino acids synthesized in the hypothalamus, is the principal neuroregulator of the hypothalamic-pituitary-adrenal axis, signaling via guanine nucleotide-binding proteins (G proteins) and downstream effectors such as adenylate cyclase. The CRF2 receptor is a multi-pass membrane protein with a transmembrane domain composed of seven helices arranged in a V-shape. CRF2 receptors are activated by two structurally similar peptides, urocortin II, and urocortin III, as well as CRH. Properties The human CRHR2 gene contains 12 exons. Three major functional isoforms, alpha (411 amino acids), beta (438 amino aci ...
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Corticotropin-releasing Hormone Receptor
Corticotropin-releasing hormone receptors (CRHRs), also known as corticotropin-releasing factor receptors (CRFRs), are a family of G protein-coupled receptors that bind corticotropin-releasing hormone (CRH). There are two main subtypes in this receptor family, designated as type 1 and type 2, each encoded by a distinct gene—CRHR1 and CRHR2, respectively. These receptors play a central role in regulating the hypothalamic-pituitary-adrenal (HPA) axis, a complex system that controls the release of stress-related hormones such as cortisol. The CRHR-mediated stress response is crucial for maintaining homeostasis, or physiological equilibrium. However, dysregulation of this system has been linked to several mental health disorders, including anxiety, depression, and post-traumatic stress disorder (PTSD). Corticotropin-releasing hormone receptors are classified into two subtypes: CRHR1 and CRHR2. CRHR1 is primarily involved in initiating the stress response, whereas CRHR2 appear ...
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Urocortin III
Urocortin III, a 38–41 amino acid peptide, is a member of the CRF (corticotropin-releasing factor), also known as CRH (corticotropin-releasing hormone) family of peptides, with a long evolutionary lineage. Separate chromosomes harboring two exons each are home to the genes encoding UCN, UCN2, and UCN3. A gene on human chromosome 10p15 at location 5.40 Mb encodes the urocortin, UCN III, which has been discovered more recently. A 161 amino acid precursor is produced when the UCN III gene is translated. Mature UCN III with 38 or 41 amino acids would be produced by proteolytic cleavage between arginine- or threonine-lysine residues. Human plasma contains both the 38 and 41 amino acid forms of UCN III, although the 38 amino acid form is more prevalent, according to findings from high-performance liquid chromatography. Each urocortin peptide has a distinct expression location and function, yet they all share conserved structural similarity. Urocortins' structures, as determined by ...
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Protein
Proteins are large biomolecules and macromolecules that comprise one or more long chains of amino acid residue (biochemistry), residues. Proteins perform a vast array of functions within organisms, including Enzyme catalysis, catalysing metabolic reactions, DNA replication, Cell signaling, responding to stimuli, providing Cytoskeleton, structure to cells and Fibrous protein, organisms, and Intracellular transport, transporting molecules from one location to another. Proteins differ from one another primarily in their sequence of amino acids, which is dictated by the Nucleic acid sequence, nucleotide sequence of their genes, and which usually results in protein folding into a specific Protein structure, 3D structure that determines its activity. A linear chain of amino acid residues is called a polypeptide. A protein contains at least one long polypeptide. Short polypeptides, containing less than 20–30 residues, are rarely considered to be proteins and are commonly called pep ...
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IUPHAR
The International Union of Basic and Clinical Pharmacology (IUPHAR) is a voluntary, non-profit association representing the interests of scientists in pharmacology-related fields to facilitate ''Better Medicines through Global Education and Research'' around the world. History Established in 1959 as a section of the International Union of Physiological Sciences, IUPHAR became an independent organization in 1966 and is a member of the International Council for Science (ICSU). The first World Congress of Pharmacology was held in Stockholm, Sweden in 1961 and subsequently held every three years. After 1990 the World Congresses were moved to a four-year interval. These meetings present the latest pharmacological research, technology, and methodology, and provide a forum for international collaboration and exchange of ideas. A General Assembly, consisting of delegates from all the member societies, is convened during the congresses so member societies have an opportunity to elect t ...
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Corticotropin-releasing Hormone
Corticotropin-releasing hormone (CRH) (also known as corticotropin-releasing factor (CRF) or corticoliberin; corticotropin may also be spelled corticotrophin) is a peptide hormone involved in stress responses. It is a releasing hormone that belongs to corticotropin-releasing factor family. In humans, it is encoded by the ''CRH'' gene. Its main function is the stimulation of the pituitary synthesis of adrenocorticotropic hormone (ACTH), as part of the hypothalamic–pituitary–adrenal axis (HPA axis). Corticotropin-releasing hormone (CRH) is a 41-amino acid peptide derived from a 196-amino acid preprohormone. CRH is secreted by the paraventricular nucleus (PVN) of the hypothalamus in response to stress. Increased CRH production has been observed to be associated with Alzheimer's disease and major depression, and autosomal recessive hypothalamic corticotropin deficiency has multiple and potentially fatal metabolic consequences including hypoglycemia. In addition to being ...
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G Protein
G proteins, also known as guanine nucleotide-binding proteins, are a Protein family, family of proteins that act as molecular switches inside cells, and are involved in transmitting signals from a variety of stimuli outside a cell (biology), cell to its interior. Their activity is regulated by factors that control their ability to bind to and hydrolyze guanosine triphosphate (GTP) to guanosine diphosphate (GDP). When they are bound to GTP, they are 'on', and, when they are bound to GDP, they are 'off'. G proteins belong to the larger group of enzymes called GTPases. There are two classes of G proteins. The first function as monomeric small GTPases (small G-proteins), while the second function as heterotrimeric G protein protein complex, complexes. The latter class of complexes is made up of ''G alpha subunit, alpha'' (Gα), ''beta'' (Gβ) and ''gamma'' (Gγ) protein subunit, subunits. In addition, the beta and gamma subunits can form a stable Protein dimer, dimeric complex re ...
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Adenylate Cyclase
Adenylate cyclase (EC 4.6.1.1, also commonly known as adenyl cyclase and adenylyl cyclase, abbreviated AC) is an enzyme with systematic name ATP diphosphate-lyase (cyclizing; 3′,5′-cyclic-AMP-forming). It catalyzes the following reaction: :ATP = 3′,5′-cyclic AMP + diphosphate It has key regulatory roles in essentially all cells. It is the most polyphyletic known enzyme: six distinct classes have been described, all catalyzing the same reaction but representing unrelated gene families with no known sequence or structural homology. The best known class of adenylyl cyclases is class III or AC-III (Roman numerals are used for classes). AC-III occurs widely in eukaryotes and has important roles in many human tissues. All classes of adenylyl cyclase catalyse the conversion of adenosine triphosphate (ATP) to 3',5'-cyclic AMP (cAMP) and pyrophosphate. Magnesium ions are generally required and appear to be closely involved in the enzymatic mechanism. The cAMP produced by ...
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Urocortin II
Urocortin 2 (Ucn2) is an endogenous peptide in the corticotrophin-releasing factor (CRF) family. Urocortin II is a 38-amino acid peptide that is a member of the CRF family of peptides. Unlike Urocortin I, Urocortin II is highly selective for the CRF2 receptor and does not show affinity for the CRF binding protein. Function Urocortin (UCN) II, also known as stresscopin-related peptide, is a 38 amino acid member of the mammalian corticotropin-releasing hormone (CRH) peptide family, which also includes CRH, UCN I, and UCN III. CRH mainly binds to type 1 CRH receptors (CRH1), while UCN II and III bind primarily to type 2 CRH receptors, and UCN I binds to both (CRH2). Each of these hormones has distinctive distribution patterns in the central nervous system and the periphery, suggesting each peptide may have distinct behavioral and physiological effects, although all have been associated with anxiety. In general, agonism of CRH1 receptors is posited to be anxiogenic and agonism of ...
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Exon
An exon is any part of a gene that will form a part of the final mature RNA produced by that gene after introns have been removed by RNA splicing. The term ''exon'' refers to both the DNA sequence within a gene and to the corresponding sequence in RNA transcripts. In RNA splicing, introns are removed and exons are covalently joined to one another as part of generating the mature RNA. Just as the entire set of genes for a species constitutes the genome, the entire set of exons constitutes the exome. History The term ''exon'' is a shortening of the phrase ''expressed region'' and was coined by American biochemist Walter Gilbert in 1978: "The notion of the cistron... must be replaced by that of a transcription unit containing regions which will be lost from the mature messengerwhich I suggest we call introns (for intragenic regions)alternating with regions which will be expressedexons." This definition was originally made for protein-coding transcripts that are spliced before b ...
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Corticotropin-releasing Hormone Receptor 1
Corticotropin-releasing hormone receptor 1 (CRHR1) is a protein, also known as CRF1, with the latter (CRF1) now being the IUPHAR-recommended name. In humans, CRF1 is encoded by the ''CRHR1'' gene at region 17q21.31, beside micrototubule-associated protein tau MAPT. Structure The human CRHR1 gene contains 14 exons over 20 kb of DNA, and its full gene product is a peptide composed of 444 amino acids. Excision of exon 6 yields in the mRNA for the primary functional CRF1, which is a peptide composed of 415 amino acids, arranged in seven hydrophobic alpha-helices. The CRHR1 gene is alternatively spliced into a series of variants. These variants are generated through deletion of one of the 14 exons, which in some cases causes a frame-shift in the open reading frame, and encode corresponding isoforms of CRF1. Though these isoforms have not been identified in native tissues, the mutations of the splice variants of mRNA suggest the existence of alternate CRF receptors, with difference ...
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Endoplasmic Reticulum
The endoplasmic reticulum (ER) is a part of a transportation system of the eukaryote, eukaryotic cell, and has many other important functions such as protein folding. The word endoplasmic means "within the cytoplasm", and reticulum is Latin for "little net". It is a type of organelle made up of two subunits – rough endoplasmic reticulum (RER), and smooth endoplasmic reticulum (SER). The endoplasmic reticulum is found in most eukaryotic cells and forms an interconnected network of flattened, membrane-enclosed sacs known as cisternae (in the RER), and tubular structures in the SER. The membranes of the ER are continuous with the outer nuclear membrane. The endoplasmic reticulum is not found in red blood cells, or spermatozoa. There are two types of ER that share many of the same proteins and engage in certain common activities such as the synthesis of certain lipids and cholesterol. Different types of Cell (biology), cells contain different ratios of the two types of ER dependin ...
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