AnatomyOrganismsDiseasesChemicals and DrugsAnalytical, Diagnostic and Therapeutic Techniques and EquipmentPhenomena and ProcessesDisciplines and OccupationsInformation Science
Aurora KinasesAurora Kinase BAurora Kinase AAurora Kinase CProtein-Serine-Threonine KinasesPhosphatidylinositol 3-KinasesProtein Kinase InhibitorsProtein KinasesMAP Kinase Signaling SystemCalcium-Calmodulin-Dependent Protein Kinasessrc-Family KinasesProtein Kinase CEnzyme InhibitorsPhosphorylationp38 Mitogen-Activated Protein KinasesCyclic AMP-Dependent Protein KinasesMitosisMitogen-Activated Protein Kinase 1IsoenzymesMitogen-Activated Protein Kinase KinasesMitogen-Activated Protein Kinase 3Protein-Tyrosine KinasesJNK Mitogen-Activated Protein Kinasesp21-Activated KinasesCDC2 Protein KinaseCyclin-Dependent KinasesSignal TransductionCell Line, TumorSpindle ApparatusCreatine KinaseCasein Kinase IIMAP Kinase Kinase KinasesCell Cycle ProteinsCyclooxygenase 2 InhibitorsEnzyme ActivationMitogen-Activated Protein KinasesRibosomal Protein S6 KinasesChromosome SegregationProtein BindingMAP Kinase Kinase 1eIF-2 KinaseCasein KinasesExtracellular Signal-Regulated MAP KinasesKineticsDose-Response Relationship, DrugPyruvate KinaseMolecular Sequence DataReceptor Protein-Tyrosine KinasesThymidine KinaseHeLa CellsApoptosisPhosphotransferases (Alcohol Group Acceptor)KinetochoresGlycogen Synthase Kinase 3Substrate SpecificityIndolesCell LineMutationCyclooxygenase InhibitorsBlotting, WesternProto-Oncogene ProteinsCells, CulturedAmino Acid SequencePyrimidinesMAP Kinase Kinase 4PyrazolesTransfectionrho-Associated KinasesProtein Kinase C-deltaProtein Kinase C-alphaI-kappa B Kinase1-Phosphatidylinositol 4-KinaseMicrotubule-Associated ProteinsBenzamidesCDC2-CDC28 KinasesIntracellular Signaling Peptides and ProteinsPiperazinesCell CycleRecombinant ProteinsCyclooxygenase 2PyridinesSulfonamidesProto-Oncogene Proteins c-aktCell ProliferationBinding SitesProtein Structure, TertiaryProstaglandin-Endoperoxide SynthasesRNA, MessengerSerinePhosphoproteinsRNA, Small InterferingCentrosomeCyclic GMP-Dependent Protein KinasesOrganophosphatesGene Expression Regulation, EnzymologicCytokinesisAntineoplastic AgentsJanus Kinase 2Cell DivisionDiacylglycerol Kinase
InhibitsSerine-threoniEGFRInhibitionIC50AntitumorPDGFRIC50sHydrochloridePhosphorylationAllostericEnzymesCytokinesisMTORJAK2Family kinasesPI3KTyrosine kinasesCell proliferationBioavailablePhosphatase InhibitorsSpindlePotentlyAnticancer agentsReversibleAgonistNanomolarAntagonistCompetitive inhibitorOrally administeredMammalianProtein tyrosine phMitosisMAPKPLK4Multi-targetedActivitySelectivityHighlyGeneTherapeuticAnti-inflammatoryClinical
Inhibits10
  • JNJ-7706621 is a potent aurora kinase inhibitor, and also inhibits CDK1 and CDK2 , with IC 50 s of 9 nM, 3 nM, 11 nM, and 15 nM for CDK1 , CDK2 , aurora-A and aurora-B , respectively. (medchemexpress.com)
  • Hesperadin is an ATP competitive indolinone inhibitor of Aurora A and B . Hesperadin inhibits Aurora B with an IC 50 of 250 nM. (medchemexpress.com)
  • TA-02 is a p38 MAPK inhibitor with IC50 of 20 nM.TA-02 especially inhibits TGFBR-2. (targetmol.jp)
  • Taken together, these results demonstrate that the ORIC small molecule CD73 inhibitor potently inhibits the adenosine pathway, which restores anti-tumor immunity and therefore holds potential for patients with multiple myeloma. (oricpharma.com)
  • GC36199 GW284543 GW284543 (UNC10225170), a MEK5-selective inhibitor, inhibits MEK5 in a dose-dependently way as determined by reductions in pERK5, and decreases endogenous MYC protein. (glpbio.cn)
  • PD173074 is an effective FGFR1 inhibitor (IC50: 25 nM) and also inhibits VEGFR2 (IC50: 100-200 nM) in cell-free assays. (targetmol.com)
  • PF-477736 is a specifc, effective and ATP-competitive Chk1 inhibitor (Ki: 0.49 nM ) and also inhibits FGFR3, Aurora-A, VEGFR2, Flt3, Fms (CSF1R), Ret and Yes. (targetmol.com)
  • Ranitidine is a potent, selective and orally active histamine H2-receptor antagonist with an IC50 of 3.3 μM that inhibits gastric secretion. (adooq.com)
  • Ilorasertib hydrochloride (ABT-348 hydrochloride) is an ATP-competitive multitargeted kinase inhibitor, which inhibits Aurora C, Aurora B, and Aurora A (IC50s: 1. (targetmol.com)
  • GC62145 Chiauranib Chiauranib (CS2164) selectively inhibits multiple kinase targets aurora B kinase (AURKB), colony-stimulating factor 1 receptor (CSF1R), and vascular endothelial growth factor receptor (VEGFR)/platelet-derived growth factor receptor (PDGFR)/c-Kit , thereby inhibiting the rapid proliferation of tumor cells, enhancing the antitumor immunity, and inhibiting tumor angiogenesis, to achieve the anti-tumor efficacy. (glpbio.cn)
Serine-threoni5
  • Aurora kinases constitute a family of serine-threonine kinases that are strongly associated with cancer. (cogershop.com)
  • Aurora kinases belong to serine/threonine kinases. (cancer-research-network.com)
  • A family of highly conserved serine-threonine kinases that are involved in the regulation of MITOSIS. (lookformedical.com)
  • Mammalian aurora-A belongs to a multigenic family of mitotic serine/threonine kinases comprising two other members: aurora-B and aurora-C. In this review we will focus on aurora-A that starts to localize to centrosomes only in S phase as soon as centrioles have been duplicated, the protein is then degraded in early G1. (lookformedical.com)
  • Aurora kinases are serine/threonine kinases that are essential for cell proliferation. (targetmol.com)
EGFR9
  • METHODS: This phase II study (ClinicalTrials.gov identifier: NCT04619004) was designed to evaluate HER3-DXd in patients with advanced EGFR-mutated NSCLC previously treated with EGFR tyrosine kinase inhibitor (TKI) therapy and platinum-based chemotherapy (PBC). (bvsalud.org)
  • We analyzed the clinical data and performed immunohistochemistry for Epidermal growth factor receptor (EGFR) and Aurora kinase A (Aurora-A) expression in 180 SCCHN patients. (oncotarget.com)
  • Patients characterized by elevated EGFR and elevated Aurora-A protein expression in tumor tissue represent a risk group with poor disease-free and overall survival (EGFR low Aurora-A low versus EGFR high Aurora-A high , p=0.024). (oncotarget.com)
  • Treating SCCHN cell lines with a pan-Aurora kinase inhibitor resulted in defective cytokinesis, polyploidy and apoptosis, which was effective irrespective of the EGFR status. (oncotarget.com)
  • Combined Aurora kinase and EGFR targeting using a monoclonal anti-EGFR antibody was more effective compared to single EGFR and Aurora kinase inhibition. (oncotarget.com)
  • Comparing pan-Aurora kinase and Aurora-A targeting hints towards a strong and clinically relevant biological effect mediated via Aurora kinase B. Taken together, our findings characterize a new poor risk group in SCCHN patients defined by elevated EGFR and Aurora-A protein expression. (oncotarget.com)
  • Our results demonstrate that combined targeting of EGFR and Aurora kinases represents a therapeutic means to activate cell cycle checkpoints and apoptosis in SCCHN. (oncotarget.com)
  • Taken together, these data confirm ORIC-114 as a potent, selective, irreversible, brain penetrant EGFR exon 20 inhibitor, and a promising therapeutic candidate, including for patients with CNS metastases. (oricpharma.com)
  • Lapatinib, used in the form of Lapatinib Ditosylate, is a potent EGFR and ErbB2 inhibitor with IC50 of 10.8 and 9.2 nM in cell-free assays, respectively. (absource.de)
Inhibition7
  • The inhibition of Aurora kinases in order to arrest mitosis and subsequently inhibit tumor growth via apoptosis of proliferating cells has generated significant discussion within the literature. (rcsb.org)
  • Analysis of DNA content and indirect immunofluoresence demonstrates that SNS-314 induces defects in cytokinesis and spindle checkpoint that are consistent with Aurora kinase inhibition. (cogershop.com)
  • Analysis of SNS-314 treated tumors confirms that the anti-tumor activity is consistent with Aurora kinase inhibition. (cogershop.com)
  • Intriguingly, cells exposed to PFI-1 showed significant downregulation of Aurora B kinase, thus attenuating phosphorylation of the Aurora substrate H3S10, providing an alternative strategy for the specific inhibition of this well-established oncology target. (ox.ac.uk)
  • LSA has speedy and profound effects on critical aspects of cell biology including inhibition of cell adhesion activation of PKC and activation of the mitogen-activated protein kinases (MAPK) ERK1/2 and p38 [8 12 13 Figure 1 shRNA screen for genetic determinants of lasonolide A (LSA) sensitivity. (biomedigs.org)
  • Description: Measuring inhibition of kinase activity in a biochemical assay. (guidetomalariapharmacology.org)
  • Furthermore, pharmacological inhibition of MELK activity by small-molecule inhibitor OTSSP167 significantly inhibited cell proliferation, anchorage-independent colony formation, blocked cell cycle progression, and induced apoptosis in different NB cell lines including a drug-resistant cell line. (oncotarget.com)
IC5021
  • BI-3406 is an orally active, highly potent and selective between KRAS and Son of Sevenless 1 (SOS1) interaction inhibitor(IC50 : 6 nM),with anticancer activity. (targetmol.jp)
  • MAPK13-IN-1 is a potent MAPK13 (p38δ) inhibitor (IC50: 620 nM). (targetmol.jp)
  • AZ12672857 is an inhibitor of EphB4 with IC50 of 1.3 nM. (targetmol.com)
  • SI-2 hydrochloride is a highly promising inhibitor of SRC-3 SMI: SRC-3 (PPI)(IC50 values of 3-20 nM for breast cancer cell death), with acceptable oral availabil. (targetmol.com)
  • AD57 is a potent inhibitor of both c-Src and Abl with IC50 of 0.025 μM and 0.041 μM, respectively. (targetmol.com)
  • CHIR-124 is an effective Chk1 inhibitor (IC50: 0.3 nM). (targetmol.com)
  • Ceapin-A7 is a selective blocker of ATF6α signaling in response to ER stress, with an IC50 of 0.59 μM. (adooq.com)
  • Aurora inhibitor 1 is a potent Aurora inhibitor (IC50: ≤ 4 nM and ≤13 nM for Aurora A and Aurora B kinase). (targetmol.com)
  • MBM-17 is a potent inhibitor of NIMA-related kinase 2 (Nek2,IC50 of 3 nM). (targetmol.com)
  • MBM-55 is an effective inhibitor of NIMA related kinase 2 (NEK2) with an IC50 of 1 nM. (targetmol.com)
  • SNS-314 Mesylate is an effective and specific Aurora A/B/C inhibitor (IC50: 9/31/3 nM). (targetmol.com)
  • SC-514 is a selective, orally active, ATP-competitive IKK-2 inhibitor (IC50=11.2±4.7 μM), obstructs NF-κB-dependent gene expression. (targetmol.com)
  • AT9283 is an effective multi-targeted inhibitor of JAK2(IC50=1.2 nM) and JAK3(IC50=1.1 nM), Aurora A, Aurora B and Abl(T315I). (targetmol.com)
  • CCT 137690 is a highly specific and oral-available aurora kinase inhibitor, for aurora A(IC50=15 nM ), B(IC50=25 nM) and C(IC50=19 nM). (targetmol.com)
  • Ketorolac (Ketorolac tromethamine) is a non-selective COX inhibitor of COX-1 and COX-2 with IC50 of 1.23 μM and 3.50 μM, respectively. (absource.de)
  • Ibuprofen (Dolgesic) is an anti-inflammatory inhibitor targeting COX-1 and COX-2 with IC50 of 13 μM and 370 μM, respectively. (absource.de)
  • Allopurinol Sodium is a xanthine oxidase inhibitor with an IC50 of 7.82±0.12 μM. (absource.de)
  • Orlistat is a general lipase inhibitor with IC50 of 122 ng/ml for PL from human duodenal juice. (absource.de)
  • Imidapril HCl is an angiotensin-converting enzyme (ACE) inhibitor with IC50 of 2.6 nM, used for the treatment of hypertension. (absource.de)
  • Azasetron HCl is a selective 5-HT3 receptor antagonist with IC50 of 0.33 nM used in the management of nausea and vomiting induced by cancer chemotherapy. (absource.de)
  • Gabexate Mesylate is a serine protease inhibitor with IC50 of 0.19 μM which is used therapeutically in the treatment of pancreatitis and disseminated intravascular coagulation. (absource.de)
Antitumor1
  • Exarafenib is a potent and orally available pan-RAF inhibitor.Exarafenib has antitumor activity and acts by inhibiting downstream MAPK pathway signaling.Exarafen. (targetmol.jp)
PDGFR3
  • PDGFR (platelet-derived growth factor receptor) is a group of cell surface tyrosine kinase receptors for members of the PDGF (platelet-derived growth factor) family. (glpbio.cn)
  • GC39314 Tyrphostin AG1433 Tyrphostin AG1433 (AG1433, SU1433) is a selective platelet-derived growth factor receptor β (PDGFRβ) and vascular endothelial growth factor receptor 2 (VEGFR-2, Flk-1/KDR) inhibitor with IC50s of 5.0 μM and 9.3 μM, respectively. (glpbio.cn)
  • GC38380 Vorolanib X-82 (Vorolanib, CM082) is an oral, multikinase, dual inhibitor of vascular endothelial growth factor receptor (VEGFR) and platelet-derived growth factor receptor (PDGFR) with antiangiogenic and antineoplastic activities. (glpbio.cn)
IC50s5
  • TA-01 is a potent CK1 and p38 MAPK inhibitor, with IC50s of 6.4 nM, 6.8 nM, 6.7 nM for CK1ε, CK1δ and p38 MAPK, respectively. (targetmol.jp)
  • CGP77675 is a potent and selective inhibitor of Src family kinase with IC50s of 5-20 and 40 nM for the phosphorylation of peptide substrates and autophosphorylat. (targetmol.com)
  • Hck-IN-1 is a selective Nef-dependent Hck inhibitor (IC50s: 2.8 μM and >20 μM for Nef:Hck complex and Hck) with antiretroviral activity. (targetmol.com)
  • SCH-1473759 is an inhibitor of the aurora (IC50s: 4 and 13 nM for Aurora A and B, respectively). (targetmol.com)
  • SCH-1473759 hydrochloride is an inhibitor of aurora(aurora A and B with IC50s of 4 and 13 nM, respectively). (targetmol.com)
Hydrochloride2
  • TC-A 2317 hydrochloride is an inhibitor of Aurora kinase A with a Ki of 1.2 nM compared to Aurora kinase B with a Ki of 101 nM. (targetmol.com)
  • Temocapril HCl is the hydrochloride of Temocapril, which is a long-acting angiotensin-converting enzyme (ACE) inhibitor, used for the treatment of hypertension. (absource.de)
Phosphorylation3
  • Phosphorylation of Histone H3 on serine 10, a known Aurora B cellular target, is inhibited with an EC50 of ~9nM following treatment of cells with SNS-314. (cogershop.com)
  • It has been shown that S338 phosphorylation on RAF1 is carried out via autophosphorylation and via phosphorylation by PAKs (p21-activated kinases) [17 18 19 20 RAF kinases in turn activate the MEK/ERK cascade which was recently found to be rapidly activated by LSA [12]. (biomedigs.org)
  • BTK, a TEC-family tyrosine kinase activated by the B-cell antigen receptor, contains a variety of regulatory domains and it is subject to complex regulation by membrane phospholipids, protein ligands, phosphorylation, and dimerization. (elifesciences.org)
Allosteric1
  • Together, these data provide the first structural elucidation of full-length BTK and allow a deeper understanding of allosteric control over the BTK kinase domain during distinct stages of activation. (elifesciences.org)
Enzymes1
  • The Aurora enzymes are particularly significant because they are involved in a direct path to the nucleosome by phosphorylating histone H3. (wikipedia.org)
Cytokinesis1
MTOR2
  • Different subclasses of PI3K/mTOR, Aurora and EZH2 inhibitors were identified that relate to different mechanisms of activity or different genetic targeting. (oncolines.com)
  • PI3K inhibitors block the PI3K/AKT/mTOR pathway and thus slow down cancer growth. (pi3k-inhibitors.com)
JAK21
  • AT9283 is a multi-targeted kinase inhibitor with potent activity against Aurora A/B , JAK2 /3 , Abl (T315I) and Flt3 ( IC 50 s ranging from 1 to 30 nM). (medchemexpress.com)
Family kinases2
  • Src family kinases contain six conserved domains: a N-terminal myristoylated segment, a SH2 domain, a SH3 domain, a linker region, a tyrosine kinase domain, and C-terminal tail. (targetmol.com)
  • Structures of the autoinhibited SRC family kinases were solved in 1997 revealing, for the first time, the compact arrangement of the SH3 and SH2 domains assembled onto the distal side of the catalytic kinase domain [ 4 ]. (elifesciences.org)
PI3K1
  • Therefore, we hypothesized the improved anticancer efficacy of QUE in combination with isoenzyme inhibitors-rottlerin (ROT-PKCδ inhibitor), G0 6983 (PKCα inhibitor), and PI-103 (p110α-class I PI3K inhibitor) in MCF-7 and RAW 264.7 cells. (pi3k-inhibitors.com)
Tyrosine kinases3
  • Selective for Bcr-Abl over a panel of serine, threonine and tyrosine kinases. (tocris.com)
  • Src kinase family is a family of non-receptor tyrosine kinases that includes nine members: Src, Yes, Fyn, and Fgr, forming the SrcA subfamily, Lck, Hck, Blk, and Lyn in the SrcB subfamily, and Frk in its own subfamily. (targetmol.com)
  • The TEC kinases are the second largest sub-family of non-receptor tyrosine kinases in the human genome after the SRC family [ 1 - 3 ]. (elifesciences.org)
Cell proliferation1
Bioavailable1
  • PF-07321332 is an orally bioavailable 3C-like protease (3CLPRO) inhibitor. (adooq.com)
Phosphatase Inhibitors1
  • PCC can be induced by cell fusion between interphase and mitotic cells or by the action of chemicals mainly phosphatase inhibitors such as for example calyculin A or okadaic acidity [14]. (biomedigs.org)
Spindle6
  • Aurora A influences centrosome maturation and spindle assembly, while Auroras B and C direct chromosome alignment and segregation. (rndsystems.com)
  • Alisertib (MLN 8237) is an orally active and selective Aurora A kinase inhibitor ( IC 50 =1.2 nM), which binds to Aurora A kinase resulting in mitotic spindle abnormalities, mitotic accumulation. (medchemexpress.com)
  • Aurora kinases control multiple events during cell cycle progression and are essential for mitotic and meiotic bipolar spindle assembly and function. (cancer-research-network.com)
  • An aurora kinase that localizes to the CENTROSOME during MITOSIS and is involved in centrosome regulation and formation of the MITOTIC SPINDLE. (lookformedical.com)
  • Works in various organisms have revealed that the kinase is involved in centrosome separation, duplication and maturation as well as in bipolar spindle assembly and stability. (lookformedical.com)
  • The protein kinase TTK is a component of the spindle assembly checkpoint, a protein machinery that regulates correct segregation of chromosomes over daughter cells during cell division. (oncolines.com)
Potently1
  • NTRC has developed a series of highly selective inhibitors of TTK enzyme activity that potently inhibit proliferation of human cancer cells and tumour growth in mouse models. (oncolines.com)
Anticancer agents1
Reversible2
  • PF-03814735 is a potent, orally available, ATP-competitive and reversible aurora A and aurora B inhibitor with IC 50 s of 0.8 and 0.5 nM, respectively. (medchemexpress.com)
  • Potent, reversible AMPK activator. (hellobio.com)
Agonist3
  • Nanrilkefusp alfa is a Selective and Potent Agonist Fusion Protein of IL-15. (cancer-research-network.com)
  • Perlapine is a potent and selective hM3Dq DREADD agonist (EC50 = 2.8 nM). (adooq.com)
  • Amprenavir is a potent PXR-selective agonist, and an HIV protease inhibitor, used to treat HIV. (absource.de)
Nanomolar1
Antagonist8
  • Selective A 2A antagonist. (tocris.com)
  • Felodipine is a 1,4-dihydropyridine antagonist and calcium channel protein inhibitor. (adooq.com)
  • DL-AP5 is the racemic version of the selective N-methyl-D-aspartate (NMDA) receptor antagonist. (adooq.com)
  • Avacopan (CCX168) is an orally administered and selective C5a receptor (C5aR) antagonist. (adooq.com)
  • L 888607 Racemate is a selective antagonist of prostaglandin D2 receptor subtype 1 (DP1) (Kis: 132 nM and 17 nM for DP1 and thromboxane A2 receptor (TP), respect. (targetmol.com)
  • Blonanserin is a relatively selective serotonin (5-HT)2A and dopamine D2 antagonist, used the treatment of schizophrenia. (absource.de)
  • Levosulpiride is a selective antagonist for D2 dopamine receptors used as an antipsychotic and prokinetic agent. (absource.de)
  • On the other hand, (-)-raclopride and remoxipride, two medicines that preferentially bind D2 over D4 receptors had been ineffective, aswell as the selective D3 receptor antagonist U 99194. (cell-metabolism.com)
Competitive inhibitor2
  • GSK-1070916 is a potent and selective ATP-competitive inhibitor of aurora B and aurora C with K i s of 0.38 and 1.5 nM, respectively, and is >250- fold selective over Aurora A. (medchemexpress.com)
  • Methyldopa (Aldomet) is a DOPA decarboxylase competitive inhibitor with an ED50 of 21.8 mg/kg. (absource.de)
Orally administered1
  • In September 2022, Puma entered into an exclusive license agreement for the development and commercialization of the anti-cancer drug alisertib, a selective, small molecule, orally administered inhibitor of aurora kinase A. Initially, Puma intends to focus the development of alisertib on the treatment of small cell lung cancer and breast cancer. (pumabiotechnology.com)
Mammalian2
  • The mammalian Aurora kinase family contains three serine/threonine kinase members that participate in cell division. (rndsystems.com)
  • There are three mammalian aurora kinase genes, encoding aurora A, B and C. Intense investigation has focused on aurora A and B as they appear to play a role in oncogenesis with aurora A identified as a low penetrance tumor susceptibility gene in mice and humans. (wikipedia.org)
Protein tyrosine ph1
Mitosis4
MAPK5
  • As with other MAPK cascades, the membrane-proximal component is a MAPKKK, typically a MEKK or a mixed lineage kinase (MLK). (targetmol.jp)
  • The MAPKKK phosphorylates and activates MKK3/6, the p38 MAPK kinases. (targetmol.jp)
  • VX-702 is a highly specific p38α MAPK inhibitor, 14-fold higher selectivity for the p38α than p38β. (targetmol.jp)
  • This resulted in the recognition of RAF1 a serine/threonine protein kinase that plays a key role in the Ras/MAPK signaling pathway. (biomedigs.org)
  • MEK1/2, also known as MAPKK (mitogen-activated protein kinase kinase), is a kinase enzyme which phosphorylates MAPK (mitogen-activated protein kinase). (glpbio.cn)
PLK43
  • Cell viability assessment across a cancer cell line panel revealed that the highly selective ORIC PLK4 inhibitors showed greater potency in TRIM37 high cancer cell lines as compared to TRIM37 low cell lines. (oricpharma.com)
  • Importantly, cell potency in TRIM37 high cancer cells was rescued with knockdown of TRIM37, illustrating that selective PLK4 inhibitors are synthetic lethal with TRIM37 amplification. (oricpharma.com)
  • Centrinone-B (LCR-323) is a potent and highly selective inhibitor of PLK4 (Ki: 0.59 nM). (targetmol.com)
Multi-targeted1
  • TAK-901 is a multi-targeted aurora inhibitor with IC 50 s of 21 and 15 nM for aurora A and B, respectively. (medchemexpress.com)
Activity7
  • Residues Lys-162 and Asp-274 are essential for Aurora-2 kinase activity but do not hydrogen bond to each other as seen in crystal structures of several other protein kinases. (wikipedia.org)
  • In particular, compound 21 (SNS-314) is a potent and selective Aurora kinase inhibitor that exhibits significant activity in pre-clinical in vivo tumor models. (rcsb.org)
  • It has potent anti-inflammatory activity. (targetmol.jp)
  • Richards, M.L. 2-phenylimidazopyridines, a new series of Golgi compounds with potent antiviral activity. (eurekaselect.com)
  • Daurichromenic acid is a terpenophenol with a potent anti-HIV activity. (adooq.com)
  • Increased target residence time correlated with increased activity of TTK inhibitors in cancer cell line proliferation assays. (oncolines.com)
  • Flunixin Meglumin is a potent inhibitor of the enzyme cyclooxygenase (COX) used as analgesic agent with anti-inflammatory and antipyretic activity. (absource.de)
Selectivity2
  • The development of the phthalazinone template resulted in a potent Aurora-A selective series of compounds (typically >1000-fold selectivity over Aurora-B) that display good pharmacological profiles with significantly improved oral bioavailability compared to the well studied Aurora inhibitor VX-680. (rcsb.org)
  • MK-0457 is a pan-Aurora kinase inhibitor (Kis: 0.6/18/4.6 nM for Aurora A/Aurora B/Aurora C). It shows selectivity against more than 190 different kinases. (targetmol.com)
Highly5
  • Barasertib-HQPA (AZD2811) is a highly selective Aurora B inhibitor with an IC 50 of 0.37 nM in a cell-free assay. (medchemexpress.com)
  • AMG 900 is a potent and highly selective pan-Aurora kinases inhibitor with IC 50 of 5 nM, 4 nM and 1 nM for Aurora A , B and C , respectively. (medchemexpress.com)
  • TCS7010 is a potent and highly selective Aurora A inhibitor with with an IC 50 of 3.4 nM. (medchemexpress.com)
  • PFI-1, a highly selective protein interaction inhibitor, targeting BET Bromodomains. (ox.ac.uk)
  • Here, we present a potent and highly selective dihydroquinazoline-2-one inhibitor, PFI-1, which efficiently blocks the interaction of BET BRDs with acetylated histone tails. (ox.ac.uk)
Gene2
  • The zinc finger domain of Tzfp binds to the tbs motif located at the upstream flanking region of the Aie1 (aurora-C) kinase gene. (lookformedical.com)
  • Pancreatic cancer has also been reported to have a strong relationship with BRCA gene mutations, which indicates that pancreatic cancer patients may benefit from PARP inhibitors. (biomedcentral.com)
Therapeutic1
  • The present invention also relates to use of the derivatives and the pharmaceutically acceptable salt thereof or the pharmaceutical composition comprising the same in the preparation of therapeutic agents, in particular Bruton tyrosine kinase inhibitors, and preparing a medicament for treating and/or preventing tumors and inflammatory associated diseases. (justia.com)
Anti-inflammatory1
  • Ketoprofen is a dual COX1/2 inhibitor, used as a nonsteroidal anti-inflammatory drug to treat arthritis-related inflammatory pains. (absource.de)
Clinical6
  • In contrast, less selective compounds, including from the clinical literature, did not display differential potency in TRIM37 high versus low cancer cell lines. (oricpharma.com)
  • Oss, April, 8th, 2016 - At the AACR 2016 conference, to be held in New Orleans next week, Jos de Man, Senior Investigator Chemistry at NTRC, will present on the unique binding mode of NTRC's TTK kinase inhibitor clinical candidate NTRC 0066-0. (oncolines.com)
  • In 2022, a total of four drugs (TUOYI ® , JUNMAIKANG ® , MINDEWEI (民得維 ® ) and etesevimab) were commercialized in China or abroad, around 30 assets are undergoing clinical trials with ongericimab, bevacizumab and PARP inhibitor under Phase III clinical trials, and over 20 drug candidates are under pre-clinical drug development. (cambodiatribune.com)
  • The exceptional potency from the hepatitis C virus (HCV) NS5A inhibitor BMS-790052 has translated into an impact in proof-of-concept clinical trials. (cell-metabolism.com)
  • However, PARP inhibitor resistance has partially precluded their use in clinical applications, and the major mechanism underlying this resistance is the restoration of HRR. (biomedcentral.com)
  • Therefore, determining how to use PARP inhibitors in more clinical applications and how to avoid adverse effects, as well as prognosis and treatment response biomarkers, require additional research. (biomedcentral.com)