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Adenosine Receptor A2b
The adenosine A2B receptor, also known as ADORA2B, is a 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 agonists * Compound 38: antago ... [...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. They are coupled with G proteins. They pass through the cell membrane seven times in the form of six loops (three extracellular loops interacting with ligand molecules, three intracellular loops interacting with G proteins, an N-terminal extracellular region and a C-terminal intracellular region) of amino acid residues, which is why they are sometimes referred to as seven-transmembrane receptors. Text was copied from this source, which is available under Attribution 2.5 Generic (CC BY 2.5) licence/ref> Ligands can bind either to the extracellular N-terminus and loops (e.g. glutamate receptors) or to the binding site wi ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Adenosine Receptor
The adenosine receptors (or P1 receptors) are a class of Purinergic receptor, purinergic G protein-coupled receptors with adenosine as the endogenous ligand (biochemistry), ligand. There are four known types of adenosine receptors in humans: Adenosine A1 receptor, A1, Adenosine A2A receptor, A2A, Adenosine A2B receptor, A2B and Adenosine A3 receptor, A3; each is encoded by a different gene. The adenosine receptors are commonly known for their antagonists caffeine, theophylline, and theobromine, 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 circulation, 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, r ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Gene
In biology, the word gene has two meanings. The Mendelian gene is a basic unit of heredity. 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 non-coding genes. During gene expression (the synthesis of Gene product, RNA or protein from a gene), DNA is first transcription (biology), copied into RNA. RNA can be non-coding RNA, directly functional or be the intermediate protein biosynthesis, template for the synthesis of a protein. The transmission of genes to an organism's offspring, is the basis of the inheritance of phenotypic traits from one generation to the next. These genes make up different DNA sequences, together called a genotype, that is specific to every given individual, within the gene pool of the population (biology), population of a given species. The genotype, along with environmental and developmental factors, ultimately determines the phenotype ... [...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. The term ''embayment'' is also used for , such as extinct bays or freshwater environments. 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 wit ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
ISAM-140
ISAM-140 is a selective non- xanthinic adenosine A2B receptor antagonist. Discovered in 2016, it has a K''i'' of 3.49 nM on the A2B receptor and >1000-fold selectivity with respect to the other three adenosine receptor subtypes. It has been shown to help the 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 produced by a broad range of cells, including immune cells like macrophages, B cell, B lymphocytes, T cell, T lymphocytes ... 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] |
