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BB-Cl-Amidine
BB-Cl-Amidine is an experimental drug which acts as a non-subtype selective, irreversible inhibitor of the enzyme peptidylarginine deiminase (PAD). It has anti-cancer effects and is useful for various inflammatory conditions such as arthritis, and while it may be unlikely to be developed for human use due to toxicity concerns, it is widely used in scientific research. As well as its activity as a PAD inhibitor, BB-Cl-Amidine also inhibits the action of the Stimulator of interferon genes (STING) protein by preventing STING oligomerization and thereby terminating the signalling pathway. See also * AFM-30a * GSK484 GSK484 is an experimental drug which acts as a selective inhibitor of the enzyme peptidylarginine deiminase 4 (PAD4). It has antiinflammatory effects and has been researched for potential use in the treatment of various inflammatory conditions, ... * JBI-589 References {{reflist Experimental drugs Biphenyls Benzamides Benzimidazoles Amidines Organochlorid ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Peptidylarginine Deiminase
In enzymology, a protein-arginine deiminase (PAD) () is an enzyme that catalyzes a form of post translational modification called arginine de-imination or citrullination: :protein L-arginine + H2O \rightleftharpoons protein L-citrulline + NH3 Thus, the two substrates of this enzyme are protein L-arginine (arginine residue inside a protein) and H2O, whereas its two products are protein L-citrulline and NH3: : This enzyme belongs to the family of hydrolases, those acting on carbon-nitrogen bonds other than peptide bonds, specifically in linear amidines. The systematic name of this enzyme class is protein-L-arginine iminohydrolase. This enzyme is also called peptidylarginine deiminase. Structural studies As of late 2007, seven structures have been solved for this class of enzymes, with PDB accession codes , , , , , , and . Mammalian proteins Mammals have 5 protein-arginine deiminases, with symbols *PADI1, PADI2, PADI3, PADI4, PADI6 except for rodents, there the letter c ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
AFM-30a
AFM-30a is an experimental drug which was the first selective inhibitor to be developed of the enzyme peptidylarginine deiminase 2 (PAD2). It has been used to investigate the role of PAD2 in various inflammatory conditions and development of cancers. It was found to be active against pulmonary fibrosis in a mouse model. See also * BB-Cl-Amidine * GSK484 GSK484 is an experimental drug which acts as a selective inhibitor of the enzyme peptidylarginine deiminase 4 (PAD4). It has antiinflammatory effects and has been researched for potential use in the treatment of various inflammatory conditions, ... * JBI-589 References {{reflist Experimental drugs Amidines Benzamides Benzimidazoles Isoindolines Fluorocarbons ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
GSK484
GSK484 is an experimental drug which acts as a selective inhibitor of the enzyme peptidylarginine deiminase 4 (PAD4). It has antiinflammatory effects and has been researched for potential use in the treatment of various inflammatory conditions, primarily rheumatoid arthritis, but it has also been used to investigate the role of PAD4 in acute kidney injury, lung inflammation, heart muscle damage following heart attack, osteoporosis, diabetes, and some forms of cancer Cancer is a group of diseases involving Cell growth#Disorders, abnormal cell growth with the potential to Invasion (cancer), invade or Metastasis, spread to other parts of the body. These contrast with benign tumors, which do not spread. Po .... See also * AFM-30a * BB-Cl-Amidine * JBI-589 References {{reflist Experimental drugs Alcohols Alkylamines Benzamides Cyclopropanes Imidazoles Methoxy compounds Piperidines Indoles ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
JBI-589
JBI-589 is an experimental drug which acts as an orally active, selective inhibitor of the enzyme peptidylarginine deiminase 4 (PAD4). It has antiinflammatory effects and has been researched for potential use in the treatment of arthritis and some forms of cancer. See also * AFM-30a * BB-Cl-Amidine * GSK484 GSK484 is an experimental drug which acts as a selective inhibitor of the enzyme peptidylarginine deiminase 4 (PAD4). It has antiinflammatory effects and has been researched for potential use in the treatment of various inflammatory conditions, ... References {{reflist Experimental drugs Alkylamines Benzene derivatives 4-Fluorophenyl compounds Imidazopyridines Indoles Piperidines ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Arthritis
Arthritis is a general medical term used to describe a disorder that affects joints. Symptoms generally include joint pain and stiffness. Other symptoms may include redness, warmth, Joint effusion, swelling, and decreased range of motion of the affected joints. In certain types of arthritis, other organs such as the skin are also affected. Onset can be gradual or sudden. There are several types of arthritis. The most common forms are osteoarthritis (most commonly seen in weightbearing joints) and rheumatoid arthritis. Osteoarthritis usually occurs as an individual ages and often affects the hips, knees, shoulders, and fingers. Rheumatoid arthritis is an autoimmune disorder that often affects the hands and feet. Other types of arthritis include gout, lupus, and septic arthritis. These are inflammatory based types of rheumatic disease. Early treatment for arthritis commonly includes resting the affected joint and conservative measures such as heating or icing. Weight Weight ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Stimulator Of Interferon Genes
Stimulator of interferon genes (STING), also known as transmembrane protein 173 (TMEM173) and MPYS/MITA/ERIS is a regulator protein that in humans is encoded by the STING1 gene. STING plays an important role in innate immunity. STING induces type I interferon production when cells are infected with intracellular pathogens, such as viruses, mycobacteria and intracellular parasites. Type I interferon, mediated by STING, protects infected cells and nearby cells from local infection by binding to the same cell that secretes it (autocrine signaling) and nearby cells (paracrine signaling.) It thus plays an important role, for instance, in controlling norovirus infection. STING works as both a direct cytosolic DNA sensor (CDS) and an adaptor protein in Type I interferon signaling through different molecular mechanisms. It has been shown to activate downstream transcription factors STAT6 and IRF3 through TBK1, which are responsible for antiviral response and innate immune response ag ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Experimental Drugs
An experiment is a procedure carried out to support or refute a hypothesis, or determine the efficacy or likelihood of something previously untried. Experiments provide insight into cause-and-effect by demonstrating what outcome occurs when a particular factor is manipulated. Experiments vary greatly in goal and scale but always rely on repeatable procedure and logical analysis of the results. There also exist natural experimental studies. A child may carry out basic experiments to understand how things fall to the ground, while teams of scientists may take years of systematic investigation to advance their understanding of a phenomenon. Experiments and other types of hands-on activities are very important to student learning in the science classroom. Experiments can raise test scores and help a student become more engaged and interested in the material they are learning, especially when used over time. Experiments can vary from personal and informal natural comparisons ( ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Benzamides
Benzamide is an organic compound with the chemical formula of C7H7NO. It is the simplest amide derivative of benzoic acid. In powdered form, it appears as a white solid, while in crystalline form, it appears as colourless crystals. It is slightly soluble in water, and soluble in many organic solvents. It is a natural alkaloid Alkaloids are a broad class of natural product, naturally occurring organic compounds that contain at least one nitrogen atom. Some synthetic compounds of similar structure may also be termed alkaloids. Alkaloids are produced by a large varie ... found in the herbs of '' Berberis pruinosa''. Chemical derivatives A number of substituted benzamides are commercial drugs, including: See also * References External links Physical characteristics {{Authority control Phenyl compounds ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Benzimidazoles
Benzimidazole is a heterocyclic aromatic organic compound. This bicyclic compound may be viewed as fused rings of the aromatic compounds benzene and imidazole. It is a white solid that appears in form of tabular crystals. Preparation Benzimidazole was discovered during research on vitamin B12. The benzimidazole nucleus was found to be a stable platform on which drugs could be developed. Benzimidazole is produced by condensation of o-phenylenediamine with formic acid, or the equivalent trimethyl orthoformate: :C6H4(NH2)2 + HC(OCH3)3 → C6H4N(NH)CH + 3 CH3OH 2-Substituted derivatives are obtained when the condensation is conducted with aldehydes in place of formic acid, followed by oxidation. Reactions Benzimidazole is a base: :C6H4N(NH)CH + H+ → 6H4(NH)2CHsup>+ It can also be deprotonated with stronger bases: :C6H4N(NH)CH + LiH → Li 6H4N2CH + H2 The imine can be alkylated and also serves as a ligand in coordination chemistry. The most pro ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Amidines
Amidines are organic compounds with the functional group RC(NR)NR2, where the R groups can be the same or different. They are the imine derivatives of amides (RC(O)NR2). The simplest amidine is formamidine, HC(=NH)NH2. Examples of amidines include: * DBU * diminazene * benzamidine * Pentamidine * Paranyline Preparation A common route to primary amidines is the Pinner reaction. Reaction of the nitrile with alcohol in the presence of acid gives an iminoether. Treatment of the resulting compound with ammonia then completes the conversion to the amidine. Instead of using a Bronsted acid, Lewis acids such as aluminium trichloride promote the direct amination of nitriles, or, in certain exceptional cases, of amides. Dimethylformamide acetal reacts with primary amines to give amidines: :Me2NC(H)(OMe)2 + RNH2 → Me2NC=NHR + 2 MeOH Catalysis is likewise not required for direct amination of an imidoyl chloride. Amidines are also prepared by the addition of organolithi ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
