|
GW788388
GW 788388 is a synthetic compound which acts as a potent and selective inhibitor for TGF beta receptor 1. It has applications in research into various disorders such as liver, kidney and heart disease (especially associated with Chagas disease), and potential antiviral Antiviral drugs are a class of medication used for treating viral infections. Most antivirals target specific viruses, while a broad-spectrum antiviral is effective against a wide range of viruses. Antiviral drugs are a class of antimicrobials ... properties. See also * Galunisertib * LY-2109761 References Kinase inhibitors Pyrazoles Disubstituted pyridines 2-Pyridyl compounds {{pharm-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
LY-2109761
LY-2109761 is a synthetic compound which acts as a potent and selective inhibitor for the growth factor receptor TGF beta receptor 1. It is used for research into conditions such as pulmonary fibrosis and cancer. See also * Galunisertib * GW788388 GW 788388 is a synthetic compound which acts as a potent and selective inhibitor for TGF beta receptor 1. It has applications in research into various disorders such as liver, kidney and heart disease (especially associated with Chagas disease), ... References Growth factors Kinase inhibitors Receptor antagonists {{respiratory-system-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
TGF Beta Receptor 1
Transforming growth factor beta receptor I (activin A receptor type II-like kinase, 53kDa) is a membrane-bound TGF beta receptor protein of the TGF-beta receptor family for the TGF beta superfamily of signaling ligands. ''TGFBR1'' is its human gene. Function The protein encoded by this gene forms a heteromeric complex with type II TGF-β receptors when bound to TGF-β, transducing the TGF-β signal from the cell surface to the cytoplasm. The encoded protein is a serine/threonine protein kinase. Mutations in this gene have been associated with Loeys–Dietz aortic aneurysm syndrome (LDS, LDAS). Interactions TGF beta receptor 1 has been shown to interact with: * Caveolin 1, * Endoglin, * FKBP1A, * FNTA, * Heat shock protein 90kDa alpha (cytosolic), member A1 * Mothers against decapentaplegic homolog 7, * PPP2R2A, * STRAP, * TGF beta 1, and * TGF beta receptor 2. Inhibitors * GW-788388 * LY-2109761 * Galunisertib (LY-2157299) * SB-431542 * SB-52 ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Chagas Disease
Chagas disease, also known as American trypanosomiasis, is a tropical parasitic disease caused by ''Trypanosoma cruzi''. It is spread mostly by insects in the subfamily Triatominae, known as "kissing bugs". The symptoms change throughout the infection. In the early stage, symptoms are typically either not present or mild and may include fever, swollen lymph nodes, headaches, or swelling at the site of the bite. After four to eight weeks, untreated individuals enter the chronic phase of disease, which in most cases does not result in further symptoms. Up to 45% of people with chronic infections develop heart disease 10–30 years after the initial illness, which can lead to heart failure. Digestive complications, including an enlarged esophagus or an enlarged colon, may also occur in up to 21% of people, and up to 10% of people may experience nerve damage. is commonly spread to humans and other mammals by the kissing bug's bite wound and the bug's infected feces. The disea ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Antiviral
Antiviral drugs are a class of medication used for treating viral infections. Most antivirals target specific viruses, while a broad-spectrum antiviral is effective against a wide range of viruses. Antiviral drugs are a class of antimicrobials, a larger group which also includes antibiotic (also termed antibacterial), antifungal and antiparasitic drugs, or antiviral drugs based on monoclonal antibodies. Most antivirals are considered relatively harmless to the host, and therefore can be used to treat infections. They should be distinguished from virucides, which are not medication but deactivate or destroy virus particles, either inside or outside the body. Natural virucides are produced by some plants such as eucalyptus and Australian tea trees. Medical uses Most of the antiviral drugs now available are designed to help deal with HIV, herpes viruses, the hepatitis B and C viruses, and influenza A and B viruses. Viruses use the host's cells to replicate and this makes it ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Galunisertib
Galunisertib (LY2157299) is a small molecular experimental cancer drug previously in development by Eli Lilly. It is a TGF-b inhibitor. Development of galunisertib by Eli Lilly was discontinued in January 2020. Galunisertib was investigated in a phase II trial for treatment of hepatocellular carcinoma. Pre-clinically, combination of galunisertib with PD-L1 Programmed death-ligand 1 (PD-L1) also known as cluster of differentiation 274 (CD274) or B7 homolog 1 (B7-H1) is a protein that in humans is encoded by the ''CD274'' gene. Programmed death-ligand 1 (PD-L1) is a 40kDa type 1 transmembrane prote ... blockade resulted in improved tumor growth inhibition. References {{reflist Experimental cancer drugs ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Kinase Inhibitors
In biochemistry, a kinase () is an enzyme that catalyzes the transfer of phosphate groups from high-energy, phosphate-donating molecules to specific substrates. This process is known as phosphorylation, where the high-energy ATP molecule donates a phosphate group to the substrate molecule. As a result, kinase produces a phosphorylated substrate and ADP. Conversely, it is referred to as dephosphorylation when the phosphorylated substrate donates a phosphate group and ADP gains a phosphate group (producing a dephosphorylated substrate and the high energy molecule of ATP). These two processes, phosphorylation and dephosphorylation, occur four times during glycolysis. Kinases are part of the larger family of phosphotransferases. Kinases should not be confused with phosphorylases, which catalyze the addition of inorganic phosphate groups to an acceptor, nor with phosphatases, which remove phosphate groups (dephosphorylation). The phosphorylation state of a molecule, whether it be a ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Pyrazoles
Pyrazole is an organic compound with the formula . It is a heterocycle characterized as an azole with a 5-membered ring of three carbon atoms and two adjacent nitrogen atoms, which are in ortho-substitution. Pyrazoles are also a class of compounds that have the ring C3N2 with adjacent nitrogen atoms. Pyrazole itself has few applications but many substituted pyrazoles are of commercial interest. Notable drugs containing a pyrazole ring are celecoxib (celebrex) and the anabolic steroid stanozolol. Properties Pyrazole is a weak base, with p''K''b 11.5 (p''K''a of the conjugate acid 2.49 at 25 °C). According to X-ray crystallography, the compound is planar. The two C-N distances are similar, both near 1.33 Å History The term pyrazole was given to this class of compounds by German Chemist Ludwig Knorr in 1883. In a classical method developed by German chemist Hans von Pechmann in 1898, pyrazole was synthesized from acetylene and diazomethane. Preparation Pyrazoles are syn ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
