• cAMP-depend
  • PKA is also known as cAMP-dependent protein kinase (EC 2.7.11.11). (wikipedia.org)
  • PKA is also commonly known as cAMP-dependent protein kinase, because it has traditionally been thought to be activated through release of the catalytic subunits when levels of the second messenger cAMP rise in response to a variety of signals. (wikipedia.org)
  • 2017
  • As of 2017[update], Read's research interests are in protein crystallography and maximum likelihood estimation. (wikipedia.org)
  • compounds
  • To demonstrate the efficiency of the proposed semi-supervised feature selection method in selecting the relevant descriptors, we applied the method and other feature selection methods on three QSAR data sets such as serine/threonine-protein kinase PLK3 inhibitors, ROCK inhibitors and phenol compounds. (springer.com)
  • Among a large series of compounds built around a benzo[c]-[2,aphthyridine-8-carboxylic acid scaffold, CX-4945 was chosen for its high potency and selectivity as an inhibitor of CK2. (wikipedia.org)
  • Numerous TKIs aiming at various tyrosine kinases have been generated by the originators of these compounds and proven to be effective anti-tumor agents and anti-leukemic agents. (wikipedia.org)
  • BIM-1 and the related compounds BIM-2, BIM-3, and BIM-8 are bisindolylmaleimide-based protein kinase C (PKC) inhibitors. (wikipedia.org)
  • regulates
  • mTOR regulates cellular metabolism, growth, and proliferation by forming and signaling through two protein complexes, mTORC1 and mTORC2. (wikipedia.org)
  • protease inhibitors
  • Darnag R, Minaoui B, Fakir M (2012) QSAR models for prediction study of HIV protease inhibitors using support vector machines, neural networks and multiple linear regression. (springer.com)
  • binds
  • Since then crystallographic studies have revealed that imatinib binds to the kinase domain of Abl only when the domain adopts the inactive or "closed" conformation. (wikipedia.org)
  • An enzyme inhibitor is a molecule that binds to an enzyme and decreases its activity. (wikipedia.org)
  • A well-characterised example of this is the ribonuclease inhibitor, which binds to ribonucleases in one of the tightest known protein-protein interactions. (wikipedia.org)
  • mTOR
  • The most established mTOR inhibitors are so-called rapalogs (rapamycin and its analogs), which have shown tumor responses in clinical trials against various tumor types. (wikipedia.org)
  • The discovery of mTOR was made a few decades ago while investigating the mechanism of action of its inhibitor, rapamycin. (wikipedia.org)
  • Several downstream pathways that regulate cell-cycle progression, translation, initiation, transcriptional stress responses, protein stability, and survival of cells are signaling through mTOR. (wikipedia.org)
  • The serine/threonine kinase mTOR is a downstream effector of the PI3K/AKT pathway, and forms two distinct multiprotein complexes, mTORC1 and mTORC2. (wikipedia.org)
  • Many human tumors occur because of dysregulation of mTOR signaling, and can confer higher susceptibility to inhibitors of mTOR. (wikipedia.org)
  • Therefore, mTOR is an interesting therapeutic target for treating multiple cancers, both the mTOR inhibitors themselves or in combination with inhibitors of other pathways. (wikipedia.org)
  • Activated Akt can then go on to activate or deactivate its myriad substrates (e.g. mTOR) via its kinase activity. (wikipedia.org)
  • staurosporine
  • This staurosporine analog is a highly potent cell permeable inhibitor of CaM kinase and phosphorylase kinase (IC50 = 1.8 and 1.7 nmol/L, respectively). (wikipedia.org)
  • The value of such calculations lies in understanding a variant was designed which showed improved binding characteristics of configurationally stable atropisomeric bisindolylmaleimides where the two kinase domains, and two different inhibitor conformers bind in different orientations, the hinge region of staurosporine-Pim-1 resembles co-crystallized as an asymmetric pair of biosynthetically 'related' indolocarbazole analogs. (wikipedia.org)
  • substrates
  • These two complexes have a separate network of protein partners, feedback loops, substrates, and regulators. (wikipedia.org)
  • In contrast to substrates and irreversible inhibitors, reversible inhibitors generally do not undergo chemical reactions when bound to the enzyme and can be easily removed by dilution or dialysis. (wikipedia.org)
  • activity
  • Acts by binding PAK4 in a substrate-like manner, inhibiting the protein kinase activity. (uniprot.org)
  • Jalali-Heravi M, Asadollahi-Baboli M (2009) Quantitative structure-activity relationship study of serotonin (5-HT7) receptor inhibitors using modified ant colony algorithm and adaptive neuro-fuzzy interference system (ANFIS). (springer.com)
  • Bozorgi AH, Bagheri M, Aslebagh R, Rajabi MS (2013) A structure-activity relationship survey of histone deacetylase (HDAC) inhibitors. (springer.com)
  • In brief, treatment with a novel TGF-beta type I receptor inhibitor, GW788388, significantly reduced TGF-beta activity, leading to the attenuation of systolic dysfunction and left ventricular remodeling in an experimental rat model of MI. (biomedsearch.com)
  • Specifically, hyperthyroidism increases the ex vivo activity of pyruvate dehydrogenase kinase, thereby inhibiting glucose oxidation via pyruvate dehydrogenase. (ox.ac.uk)
  • CX-4945 was originated by now-defunct Cylene Pharmaceuticals of San Diego, California, as the culmination of a lengthy process of rational, structure-based molecular modification of a lead compound known to have PARP inhibitor activity. (wikipedia.org)
  • With a replacement of the imidazole group with a benzamido group, the compound's specificity increased while its activity as a kinase inhibitor remained the same. (wikipedia.org)
  • The close relationship of DMPK to the Rho-kinases has led to speculation whether DMPK activity may be regulated in vivo by small G proteins, particularly of the Rho family. (wikipedia.org)
  • In this model, transient activation of kinase activity would occur in response to G protein second messengers, while longterm activation of DMPK could be mediated by a membrane associated protease that cleaves DMPK-1 to release cytosolic DMPK-2 in a persistently activated form. (wikipedia.org)
  • Since blocking an enzyme's activity can kill a pathogen or correct a metabolic imbalance, many drugs are enzyme inhibitors. (wikipedia.org)
  • Tyrosine kinase activity in the nucleus involves cell-cycle control and properties of transcription factors. (wikipedia.org)
  • Furthermore, tyrosine kinase activity has been determined to be correlated to cellular transformation. (wikipedia.org)
  • Imatinib
  • While drug screening was used to develop imatinib, second generation TKI's were developed with rational drug design approach due to increased knowledge in structural biology of the Bcr-Abl tyrosine kinase. (wikipedia.org)
  • In the development of imatinib, the structure of Bcr-Abl tyrosine kinase played a limited role because it was unknown. (wikipedia.org)
  • novel
  • Novel bradykinin signaling in adult rat cardiac myocytes through activation of p21-activated kinase. (biomedsearch.com)
  • Balanol was discovered in 1993 in the search for novel inhibitors of PKC, a member of a family of serine/threonine kinases whose overactivation is associated with numerous human diseases of signal transduction including cancer. (wikipedia.org)
  • Subsequently, Cantley and colleagues demonstrated that in vivo the enzyme prefers PtdIns(4,5)P2 as a substrate, producing the novel phosphoinositide PtdIns(3,4,5)P3 previously identified in neutrophils The phosphoinositol-3-kinase family is divided into four different classes: Class I, Class II, Class III, and Class IV. (wikipedia.org)
  • intracellular
  • Extracellular hormones such as glucagon and epinephrine begin an intracellular signalling cascade that triggers protein kinase A activation by first binding to a G protein-coupled receptor (GPCR) on the target cell. (wikipedia.org)
  • When a GPCR is activated by its extracellular ligand, a conformational change is induced in the receptor that is transmitted to an attached intracellular heterotrimeric G protein complex by protein domain dynamics. (wikipedia.org)
  • subunit
  • The FAT domain consists of repeats, referred to as HEAT (Huntingtin, Elongation factor 3, A subunit of protein phosphatase 2A and TOR1). (wikipedia.org)
  • The Gs alpha subunit of the stimulated G protein complex exchanges GDP for GTP and is released from the complex. (wikipedia.org)