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Adenosine Receptor A2b
The adenosine A2B receptor, also known as ADORA2B, is a G protein-coupled receptor, G-protein coupled adenosine receptor, and also denotes the human adenosine A2b receptor gene which encodes it. Mechanism This integral membrane protein stimulates adenylate cyclase activity in the presence of adenosine. This protein also interacts with netrin-1, which is involved in axon elongation. Gene The gene is located near the Smith-Magenis syndrome region on chromosome 17. Ligands Research into selective A2B ligands has lagged somewhat behind the development of ligands for the other three adenosine receptor subtypes, but a number of A2B-selective compounds have now been developed, and research into their potential therapeutic applications is ongoing. Agonists * BAY 60-6583 * NECA (N-ethylcarboxamidoadenosine) * (S)-PHPNECA - high affinity and efficacy at A2B, but poor selectivity over other adenosine receptor subtypes * LUF-5835 * LUF-5845 - partial agonist Antagonists and inverse agoni ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
G Protein-coupled Receptor
G protein-coupled receptors (GPCRs), also known as seven-(pass)-transmembrane domain receptors, 7TM receptors, heptahelical receptors, serpentine receptors, and G protein-linked receptors (GPLR), form a large group of evolutionarily-related proteins that are cell surface receptors that detect molecules outside the cell and activate cellular responses. Coupling with G proteins, they are called seven-transmembrane receptors because they pass through the cell membrane seven times. Text was copied from this source, which is available under Attribution 2.5 Generic (CC BY 2.5) license. Ligands can bind either to extracellular N-terminus and loops (e.g. glutamate receptors) or to the binding site within transmembrane helices (Rhodopsin-like family). They are all activated by agonists although a spontaneous auto-activation of an empty receptor can also be observed. G protein-coupled receptors are found only in eukaryotes, including yeast, choanoflagellates, and ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Adenosine Receptor
The adenosine receptors (or P1 receptors) are a class of purinergic G protein-coupled receptors with adenosine as the endogenous ligand. There are four known types of adenosine receptors in humans: A1, A2A, A2B and A3; each is encoded by a different gene. The adenosine receptors are commonly known for their antagonists caffeine and theophylline, whose action on the receptors produces the stimulating effects of coffee, tea and chocolate. Pharmacology Each type of adenosine receptor has different functions, although with some overlap. For instance, both A1 receptors and A2A play roles in the heart, regulating myocardial oxygen consumption and coronary blood flow, while the A2A receptor also has broader anti-inflammatory effects throughout the body. These two receptors also have important roles in the brain, regulating the release of other neurotransmitters such as dopamine and glutamate, while the A2B and A3 receptors are located mainly peripherally and are involved in process ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Gene
In biology, the word gene (from , ; "...Wilhelm Johannsen coined the word gene to describe the Mendelian units of heredity..." meaning ''generation'' or ''birth'' or ''gender'') can have several different meanings. The Mendelian gene is a basic unit of heredity and the molecular gene is a sequence of nucleotides in DNA that is transcribed to produce a functional RNA. There are two types of molecular genes: protein-coding genes and noncoding genes. During gene expression, the DNA is first copied into RNA. The RNA can be directly functional or be the intermediate template for a protein that performs a function. The transmission of genes to an organism's offspring is the basis of the inheritance of phenotypic traits. These genes make up different DNA sequences called genotypes. Genotypes along with environmental and developmental factors determine what the phenotypes will be. Most biological traits are under the influence of polygenes (many different genes) as well as gen ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
BAY 60-6583
A bay is a recessed, coastal body of water that directly connects to a larger main body of water, such as an ocean, a lake, or another bay. A large bay is usually called a gulf, sea, sound, or bight. A cove is a small, circular bay with a narrow entrance. A fjord is an elongated bay formed by glacial action. A bay can be the estuary of a river, such as the Chesapeake Bay, an estuary of the Susquehanna River. Bays may also be nested within each other; for example, James Bay is an arm of Hudson Bay in northeastern Canada. Some large bays, such as the Bay of Bengal and Hudson Bay, have varied marine geology. The land surrounding a bay often reduces the strength of winds and blocks waves. Bays may have as wide a variety of shoreline characteristics as other shorelines. In some cases, bays have beaches, which "are usually characterized by a steep upper foreshore with a broad, flat fronting terrace".Maurice Schwartz, ''Encyclopedia of Coastal Science'' (2006), p. 129. Bays were s ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
ISAM-140
ISAM-140 is a selective non- xanthinic adenosine A2B receptor atagonist. Discovered in 2016, has a K''i'' of 3.49 nM in A2B receptor and >1000-fold selectivity with respect to the other three adenosine receptor subtypes. It has been shown to help immune system to attack cancer cells in ''in vitro'' assays, by rescuing T and NK cell proliferation, cytokine Cytokines are a broad and loose category of small proteins (~5–25 kDa) important in cell signaling. Cytokines are peptides and cannot cross the lipid bilayer of cells to enter the cytoplasm. Cytokines have been shown to be involved in autocrin ... release and TIL infiltration. References {{reflist 2-Furyl compounds Esters Nitrogen heterocycles Heterocyclic compounds with 3 rings ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
MRS-1706
MRS-1706 is a selective inverse agonist for the adenosine A2B receptor. It inhibits release of interleukin Interleukins (ILs) are a group of cytokines (secreted proteins and signal molecules) that are expressed and secreted by white blood cells (leukocytes) as well as some other body cells. The human genome encodes more than 50 interleukins and related ...s and has an antiinflammatory effect. References Xanthines Phenol ethers Acetanilides Aromatic ketones Adenosine receptor antagonists {{antineoplastic-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
