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Bisindolylmaleimide
Bisindolylmaleimide is an organic compound that forms the core chemical structure of a variety of biologically active compounds. This core structure includes a central maleimide group with two indole groups attached. Examples of bisindolylmaleimide derivatives include: * Bisindolylmaleimide I * Enzastaurin * Ruboxistaurin * Tivantinib Tivantinib (ARQ197; by Arqule, Inc.) is an experimental small molecule anti-cancer drug. It is a bisindolylmaleimide that binds to the dephosphorylated MET kinase ''in vitro''. (MET is a growth factor receptor.) Tivantinib is being tested clin ... References External links {{heterocyclic-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Bisindolylmaleimide I
BIM-1 (GF 109203X) and the related compounds BIM-2, BIM-3, and BIM-8 are bisindolylmaleimide-based protein kinase C (PKC) inhibitors. These inhibitors also inhibit PDPK1, PDK1 explaining the higher inhibitory potential of LY33331 compared to the other BIM compounds a bisindolylmaleimide inhibitor toward PDPK1, PDK1. Function The protein kinase C inhibitor bis(indolyl)maleimide inhibitor BIM1 is clearly seen in the structure of PRKCI, PKCiota (residue 574-turn motif), need to be phosphorylated towards a PKCbeta-specific inhibitor site-directed mutagenesis of the compound for its full activation and co-crystallized as an asymmetric pair which is mediated by 3-phosphoinositide-dependent protein kinase-1 (PDPK1, PDK1) are downstream characteristics of PKCs and Protein Kinase B, PKB/AKT. Scope The bound BIM1 inhibitor blocks Protein kinase C#Catalytic, bilobal interactions, the ATP-binding site, features an ATP-competitive inhibitor, 2-methyl-1''H''-indol-3-yl-BIM-1, the crystal stru ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Enzastaurin
Enzastaurin is a synthetic bisindolylmaleimide with potential antineoplastic activity. Binding to the ATP-binding site, enzastaurin selectively inhibits protein kinase C beta, an enzyme involved in the induction of vascular endothelial growth factor (VEGF)-stimulated neo-angiogenesis. This agent may decrease tumor blood supply, preventing growth. Trials In 2013 it failed a phase III clinical trial for lymphoma Lymphoma is a group of blood and lymph tumors that develop from lymphocytes (a type of white blood cell). In current usage the name usually refers to just the cancerous versions rather than all such tumours. Signs and symptoms may include enl .... In 2022, there is an upcoming initial trial called PREVEnt to look into the effectiveness of Enzastaurin for the treatment of Vascular Elhers-Danlos syndrome (vEDS). References {{reflist External links Enzastaurin hydrochloride National Institutes of Health 2-Pyridyl compounds Piperidines Bisindolylmaleimides Or ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Ruboxistaurin
Ruboxistaurin (proposed brand name Arxxant) is an investigational drug for diabetic retinopathy being investigated by Eli Lilly and Company. It is a member of the bisindolylmaleimide family. In February 2006, Lilly submitted a New Drug Application for ruboxistaurin, and on August 18, 2006, Lilly received an approvable letter from the US FDA for ruboxistaurin, with a request for an additional clinical trial, which would take 5 years to complete. Lilly has not made any further request for approval and ruboxistaurin is not approved by the FDA for any medical use. Mechanism of action Ruboxistaurin is an inhibitor of protein kinase C In cell biology, Protein kinase C, commonly abbreviated to PKC (EC 2.7.11.13), is a family of protein kinase enzymes that are involved in controlling the function of other proteins through the phosphorylation of hydroxyl groups of serine and t ...-beta. References External linksEli Lilly and Company Product Pipeline Eli Lilly and Company bra ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Tivantinib
Tivantinib (ARQ197; by Arqule, Inc.) is an experimental small molecule anti-cancer drug. It is a bisindolylmaleimide that binds to the dephosphorylated MET kinase ''in vitro''. (MET is a growth factor receptor.) Tivantinib is being tested clinically as a highly selective MET inhibitor. However, the mechanism of action of tivantinib is still unclear. Tivantinib displays cytotoxic activity via molecular mechanisms that are independent from its ability to bind MET, notably tubulin binding, which likely underlies tivantinib cytotoxicity. Possible applications include non-small-cell lung carcinoma, hepatocellular carcinoma, and oesophageal cancer. In 2017, it was announced that a phase III clinical trial for advanced hepatocellular carcinoma Hepatocellular carcinoma (HCC) is the most common type of primary liver cancer in adults and is currently the most common cause of death in people with cirrhosis. HCC is the third leading cause of cancer-related deaths worldwide. It occur ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Organic Compound
In chemistry, organic compounds are generally any chemical compounds that contain carbon- hydrogen or carbon-carbon bonds. Due to carbon's ability to catenate (form chains with other carbon atoms), millions of organic compounds are known. The study of the properties, reactions, and syntheses of organic compounds comprise the discipline known as organic chemistry. For historical reasons, a few classes of carbon-containing compounds (e.g., carbonate salts and cyanide salts), along with a few other exceptions (e.g., carbon dioxide, hydrogen cyanide), are not classified as organic compounds and are considered inorganic. Other than those just named, little consensus exists among chemists on precisely which carbon-containing compounds are excluded, making any rigorous definition of an organic compound elusive. Although organic compounds make up only a small percentage of Earth's crust, they are of central importance because all known life is based on organic compounds. Livin ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Maleimide
Maleimide is a chemical compound with the formula H2C2(CO)2NH (see diagram). This unsaturated imide is an important building block in organic synthesis. The name is a contraction of maleic acid and imide, the -C(O)NHC(O)- functional group. Maleimides also describes a ''class'' of derivatives of the parent maleimide where the N''H'' group is replaced with alkyl or aryl groups such as a methyl or phenyl, respectively. The substituent can also be a small molecule (such as biotin, a fluorescent dye, an oligosaccharide, or a nucleic acid), a reactive group, or a synthetic polymer such as polyethylene glycol. Human hemoglobin chemically modified with maleimide-polyethylene glycol is a blood substitute called MP4. Organic chemistry Maleimide and its derivatives are prepared from maleic anhydride by treatment with amines followed by dehydration. A special feature of the reactivity of maleimides is their susceptibility to additions across the double bond either by Michael additions or ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Indole
Indole is an aromatic heterocyclic organic compound with the formula C8 H7 N. It has a bicyclic structure, consisting of a six-membered benzene ring fused to a five-membered pyrrole ring. Indole is widely distributed in the natural environment and can be produced by a variety of bacteria. As an intercellular signal molecule, indole regulates various aspects of bacterial physiology, including spore formation, plasmid stability, resistance to drugs, biofilm formation, and virulence. The amino acid tryptophan is an indole derivative and the precursor of the neurotransmitter serotonin. General properties and occurrence Indole is a solid at room temperature. It occurs naturally in human feces and has an intense fecal odor. At very low concentrations, however, it has a flowery smell, and is a constituent of many perfumes. It also occurs in coal tar. The corresponding substituent is called indolyl. Indole undergoes electrophilic substitution, mainly at position 3 (see diagr ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Derivative (chemistry)
In chemistry, a derivative is a compound that is derived from a similar compound by a chemical reaction. In the past, derivative also meant a compound that ''can be imagined to'' arise from another compound, if one atom or group of atoms is replaced with another atom or group of atoms, but modern chemical language now uses the term structural analog for this meaning, thus eliminating ambiguity. The term "structural analogue" is common in organic chemistry. In biochemistry, the word is used for compounds that at least theoretically can be formed from the precursor compound. Chemical derivatives may be used to facilitate analysis. For example, melting point (MP) analysis can assist in identification of many organic compounds. A crystalline derivative may be prepared, such as a semicarbazone or 2,4-dinitrophenylhydrazone (derived from aldehydes or ketones), as a simple way of verifying the identity of the original compound, assuming that a table of derivative MP values is avai ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
