• recombinant
  • Two of the pyrrole carboxamides, PSI2106 and MDF2085, were especially notable in vitro inhibitors of recombinant human MKP-1 enzyme activity with IC 50 values of 8.0 ± 0.9 and 8.3 ± 0.8 μM, respectively. (aspetjournals.org)
  • If you cannot find the target and/or product is not available in our catalog, please click here to contact us and request the product or submit your request for custom elisa kit production , custom recombinant protein production or custom antibody production . (mybiosource.com)
  • Custom ELISA Kits, Recombinant Proteins and Antibodies can be designed, manufactured and produced according to the researcher's specifications. (mybiosource.com)
  • We have profiled the biochemical specificity of many of the kinase inhibitors across 442 purified recombinant kinases using the KINOMEscan method (outsourced to DiscoveRx ). (harvard.edu)
  • gene
  • A better understanding of the signal transduction systems and gene regulation by transcription factors involved in cytokine production has opened the way for the discovery of novel therapeutic compounds useful in treating patients with RA. (springer.com)
  • A mutation in this gene has been associated with hyperimmunoglobulin E syndrome (HIES) - a primary immunodeficiency characterized by elevated serum immunoglobulin E. Tyrosine kinase 2 has been shown to interact with FYN, PTPN6, IFNAR1, Ku80 and GNB2L1. (wikipedia.org)
  • Proto-oncogene tyrosine-protein kinase Fyn (p59-FYN, Slk, Syn, MGC45350, Gene ID 2534) is an enzyme that in humans is encoded by the FYN gene. (wikipedia.org)
  • IKK-β also known as inhibitor of nuclear factor kappa-B kinase subunit beta is a protein that in humans is encoded by the IKBKB (inhibitor of kappa light polypeptide gene enhancer in B-cells, kinase beta) gene. (wikipedia.org)
  • Vascular endothelial growth inhibitor (VEGI), also known as TNF-like ligand 1A (TL1A) and TNF superfamily member 15 (TNFSF15), is protein that in humans is encoded by the TNFSF15 gene. (wikipedia.org)
  • The protein encoded by this gene is a cytokine that belongs to the tumor necrosis factor (TNF) ligand family. (wikipedia.org)
  • The gene of cIAP1 resides on chromosome 11 and its protein has a quaternary structure. (wikipedia.org)
  • MAPKs are involved in directing cellular responses to a diverse array os stimuli, such as mitogens, osmotic stress, heat shock and proinflammatory cytokines regulating cell functions including proliferation, gene expression, differentiation, mitosis, cell survival or apoptosis. (wikipedia.org)
  • Each gene is expressed as either 46 kDa or 55 kDa protein kinases, depending upon how the 3' coding region of the corresponding mRNA is processed. (wikipedia.org)
  • If the bait and prey proteins interact (i.e., bind), then the AD and BD of the transcription factor are indirectly connected, bringing the AD in proximity to the transcription start site and transcription of reporter gene(s) can occur. (wikipedia.org)
  • If the two proteins do not interact, there is no transcription of the reporter gene. (wikipedia.org)
  • DnaJ homolog subfamily C member 3 is a protein that in humans is encoded by the DNAJC3 gene. (wikipedia.org)
  • The protein encoded by this gene contains multiple tetratricopeptide repeat (TPR) motifs as well as the highly conserved J domain found in DNAJ chaperone family members. (wikipedia.org)
  • Endotoxin
  • Using an endotoxaemia model in healthy human volunteers we evaluated the attenuation of clinical and cytokine response to endotoxin after inhibition of p38MAPK by an oral dose of RWJ-67657, a pyrindinyl imidazole. (mendeley.com)
  • selective
  • The lack of readily available selective MKP-1 inhibitors has severely limited interrogation of its biological role and was one rationale for using a recently described tricyclic pyrrole-2-carboxamide library in our screening efforts. (aspetjournals.org)
  • Overactivation of selective kinases or aberrant function of downstream transcription factors could help convert a normal immune response to a chronic disease state. (springer.com)
  • Barasertib-hQPA is a highly selective inhibitor of aurora-B kinase that has shown tumouricidal activity against a range tumour cell lines including those of leukaemic AML origin. (biomedcentral.com)
  • Initially, Tofacitinib was thought to be a selective JAK3 inhibitor but it later it was shown that it is also a potent inhibitor of JAK1 and JAK2. (wikipedia.org)
  • It has been difficult to develop sufficiently selective JAK3 inhibitors. (wikipedia.org)
  • phosphatases
  • Deactivation may be carried out by a direct pathway, removing the phosphate groups using phosphatases like PIAS or SHP-2 for example, or by an indirect pathway, which involves reducing cytokine signalling. (wikipedia.org)
  • Activation is carried out by two MAP kinase kinases, MKK4 and MKK7, and JNK can be inactivated by Ser/Thr and Tyr protein phosphatases. (wikipedia.org)
  • JAK2
  • The mammalian JAK family has four members: JAK1, JAK2, JAK3 and tyrosine kinase 2 (TYK2). (wikipedia.org)
  • Different inhibitors have been designed to target different kinases: inhibition of BCR/ABl constitutes the basis of the functioning of drugs like imatinib inhibition of FLT3 is carried out by drugs like lestaurtinib inhibition of JAK2 is carried out by the drug CYT387, which was successful in preclinical trials and is currently undergoing clinical trials. (wikipedia.org)
  • Interferon
  • In response to interferon, cells produce large amounts of an enzyme known as protein kinase R (PKR). (wikipedia.org)
  • In addition, interferons induce production of hundreds of other proteins-known collectively as interferon-stimulated genes (ISGs)-that have roles in combating viruses and other actions produced by interferon. (wikipedia.org)
  • molecules
  • IFNs belong to the large class of proteins known as cytokines, molecules used for communication between cells to trigger the protective defenses of the immune system that help eradicate pathogens. (wikipedia.org)
  • Particularly, many neuro-developmental inhibitor molecules are secreted by the cells within the scar that prevent complete physical and functional recovery of the central nervous system after injury or disease. (wikipedia.org)
  • Approved by FDA on 24 July 2015 Trap Fusion Proteins: Regeneron's novel and patented Trap technology creates high-affinity product candidates for many types of signaling molecules, including growth factors and cytokines. (wikipedia.org)
  • subunits
  • Aurora-B is the catalytic component of the chromosomal passenger complex (CPC), which is composed of three additional non-catalytic subunits that direct its activity: survivin, inner centromere protein (INCENP) and borealin. (biomedcentral.com)
  • activate
  • Microglia rapidly activate near the injury and secrete several cytokines, bioactive lipids, coagulation factors, reactive oxygen intermediates, and neurotrophic factors. (wikipedia.org)
  • The GPCR can then activate an associated G protein by exchanging the GDP bound to the G protein for a GTP. (wikipedia.org)
  • regulation
  • Collectively, our data indicate that CD151 exerts negative regulation over IgE-induced late phase responses and cytokine production in mast cells. (jimmunol.org)
  • Changes in its DNA sequence transform it into an oncogene that leads to the formation of a different protein with implications for normal cell regulation. (wikipedia.org)
  • Tyk2
  • Signalling through IL-4/IL-13 complexes is thought to occur through IL-4Rα-chain, which is responsible for activation of JAK-1 and Tyk2 kinases. (wikipedia.org)
  • Development of a Tyk2 inhibitor appears to be a rational approach in the drug discovery. (wikipedia.org)
  • chemokine
  • Amplification of cytokine/chemokine production is regulated by PI3K via an independent pathway mediated by PDK1 and Akt signaling ( 8 ). (jimmunol.org)
  • inhibition
  • The implication of the auroras in tumourigenesis and the fact that that they are kinases, amenable to small molecule inhibition, makes them attractive targets for anticancer drug development. (biomedcentral.com)
  • Inhibition of IKK and IKK-related kinases has been investigated as a therapeutic option for the treatment of inflammatory diseases and cancer. (wikipedia.org)
  • Indirect inhibition targets kinases associated with STAT5, or targets proteases that carry out terminal truncation of proteins. (wikipedia.org)
  • proliferation
  • 17. An isolated pseudosubstrate inhibitor of aPKC iota which specifically suppresses Hh pathway-promoted cancer cell proliferation and metastasis. (patentsencyclopedia.com)
  • Cytokines play pivotal roles in immunity and inflammation by regulating the survival, proliferation, differentiation, and function of immune cells, as well as cells from other organ systems. (wikipedia.org)
  • JAK3 is crucial in transmitting signals from cytokines that are responsible for either T-cell proliferation, differentiation, or development. (wikipedia.org)
  • JNK1 is involved in apoptosis, neurodegeneration, cell differentiation and proliferation, inflammatory conditions and cytokine production mediated by AP-1 (activation protein 1) such as RANTES, IL-8 and GM-CSF. (wikipedia.org)
  • apoptosis
  • In chronic lymphocytic leukemia (CLL) Dinaciclib promotes apoptosis and abrogates microenvironmental cytokine protection in chronic lymphocytic leukemia cells. (wikipedia.org)
  • cIAP1 (also named BIRC2) is the abbreviation for a human protein, cellular inhibitor of apoptosis protein-1. (wikipedia.org)
  • cIAP1 is an inhibitior of apoptosis protein. (wikipedia.org)
  • Studies show that when the protein is exposed to palmitate the concentration of cIAP1 decreases and, as a result, the apoptosis is no longer inhibited resulting in the death of the cell. (wikipedia.org)
  • Targets
  • Therefore, there is urgent need to characterize dysregulated TK signaling axes in patients with ALL and identify actionable kinase targets for the development of therapeutic strategies. (aacrjournals.org)
  • Therefore, this study highlights the application and potential of phosphotyrosine profiling for identifying clinically relevant kinase targets in leukemia. (aacrjournals.org)
  • transcription
  • The protein product of Proto-oncogene RAS can increase activity of p38, and thereby cause excessively high activity of transcription factor NF-κB. (wikipedia.org)
  • The Gal4 protein activated transcription of a protein involved in galactose utilization, which formed the basis of selection. (wikipedia.org)
  • isoforms
  • LRRC1: 2 isoforms of the human protein are produced by alternative splicing. (mybiosource.com)
  • LRRC36: 2 isoforms of the human protein are produced by alternative splicing. (mybiosource.com)
  • citation needed] The c-Jun N-terminal kinases consist of ten isoforms derived from three genes: JNK1 (four isoforms), JNK2 (four isoforms) and JNK3 (two isoforms). (wikipedia.org)
  • c-Jun N-terminal kinase isoforms have the following tissue distribution: JNK1 and JNK2 are found in all cells and tissues. (wikipedia.org)
  • tumor
  • Interferons (IFNs) are a group of signaling proteins made and released by host cells in response to the presence of several pathogens, such as viruses, bacteria, parasites, and also tumor cells. (wikipedia.org)
  • cIAP1 is a multi-functional protein which can be found in the cytoplasm of cells and in the nucleus of tumor cells. (wikipedia.org)
  • JAK3
  • It is not certain that whether JAK3 is sufficient to suppress the cytokine signaling as it can also be caused by stimulation of JAK1. (wikipedia.org)
  • JAK3 inhibitors target the catalytic ATP-binding site of JAK3 and have there been various moieties utilised to get a stronger affinity and selectivity to the ATP-binding pockets. (wikipedia.org)
  • Another ring system that has been utilised in JAK3 inhibitor derivatives is 1H-pyrrolo[2,3-b]pyridine, as it mimics the pyrrolopyrimidine scaffold. (wikipedia.org)
  • mammalian cells
  • Since then, the same principle has been adapted to describe many alternative methods, including some that detect protein-DNA interactions or DNA-DNA interactions, as well as methods that use different host organisms such as Escherichia coli or mammalian cells instead of yeast. (wikipedia.org)
  • reactive nitroge
  • 1996). In a screening for activity of 18 plant extracts on reactive oxygen species (ROS), reactive nitrogen species (RNS) and heat shock protein (hsp) production in human neutrophils, the dichloromethane extract of P. sagittalis presented the best activity (Perez Garcia et al. (thefreelibrary.com)
  • transcriptional
  • Pioneered by Stanley Fields and Ok-Kyu Song in 1989, the technique was originally designed to detect protein-protein interactions using the Gal4 transcriptional activator of the yeast Saccharomyces cerevisiae. (wikipedia.org)
  • genes
  • More than twenty distinct IFN genes and proteins have been identified in animals, including humans. (wikipedia.org)
  • Though STAT5A and STAT5B are encoded by separate genes, the proteins are 90% identical at the amino acid level. (wikipedia.org)
  • STAT5 proteins are involved in cytosolic signalling and in mediating the expression of specific genes. (wikipedia.org)
  • The exact size of the GPCR superfamily is unknown, but nearly 800 different human genes (or ~ 4% of the entire protein-coding genome) have been predicted to code for them from genome sequence analysis. (wikipedia.org)
  • responses
  • Strong responses and modulatory influences can be demonstrated, adding to the emerging view that microglial behavior is highly dependent on the (cytokine) environment and that reactions to a challenge may vary with the stimulation context. (jove.com)
  • cellular
  • Similar to the SAPK/JNK pathway, p38 MAP kinase is activated by a variety of cellular stresses including osmotic shock, inflammatory cytokines, lipopolysaccharides (LPS), Ultraviolet light, and growth factors. (wikipedia.org)