• 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)
  • Alert FDA Approves Bosutinib for Children With CML The agency approved the tyrosine kinase inhibitor for pediatric patients with chronic phase Ph+ chronic myelogenous leukemia that is newly diagnosed or resistant or intolerant to prior therapy. (medscape.com)
  • citation needed] Kinome Cyclin-dependent kinase Signal transduction Andrews, Paul D. (wikipedia.org)
  • Association between cyclin-dependent kinase inhibitor 2B antisense RNA 1 and zinc finger homeobox 3 gene polymorphisms and COVID-19 severity. (cdc.gov)
  • So far three Aurora-kinase inhibitors have been described: ZM447439, hesperadin and VX-680. (wikipedia.org)
  • ZM447439 Hesperadin VX-680 The structure and active site of Aurora-2-adenosine complex has been determined. (wikipedia.org)
  • 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)
  • The mammalian Aurora kinase family contains three serine/threonine kinase members that participate in cell division. (rndsystems.com)
  • 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)
  • Applying "drug target constellation" (DTECT) mapping, we further show that protein levels of TTF1 and cMYC predict response to targeted therapies including aurora kinase, Bcl2, and HSP90 inhibitors. (oncotarget.com)
  • The expression of BCL2 varies in T-ALL depending on its stage of maturation, thereby T-ALL displays a heterogenous response to the BCL2-specific inhibitor venetoclax. (lu.se)
  • Ann273, thanks for the info on Alisertib and FGFR status/FGFR inhibitors. (breastcancer.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)
  • Discovery of GSK1070916, a potent and selective inhibitor of Aurora B/C kinase. (idrblab.net)
  • Felodipine is a 1,4-dihydropyridine antagonist and calcium channel protein inhibitor. (adooq.com)
  • Furthermore, Aurora kinases are known to be oncogenic and overexpressed in various forms of cancerous growth, including leukemia, colon cancer, prostate cancer and breast cancer tumors. (wikipedia.org)
  • Exceptional responders were identified, including complete resolution of liver metastases and prolonged stable disease, with tumors suggestive of N-myc and Aurora-A overactivity. (unitn.it)
  • A genomic network model is used to identify aurora kinase inhibitor-sensitive lung tumors, new Illumina Accelerator start-ups are announced, AI algorithms are being used to improve prostate cancer identification and treatment, and a blood-based DNA methylation test can detect liver cancer. (bio-itworld.com)
  • The Mount Sinai team used a genomics network model to measure tumor invasiveness-distinguishing aggressive tumors from so-called "indolent" ones, which often cannot be told apart via chest CT scan-and identify those that will respond to aurora kinase inhibitors, molecules that can inhibit gene signature regulators. (bio-itworld.com)
  • Alisertib inhibits the interaction between N-myc and its stabilizing factor Aurora-A, inhibiting N-myc signaling, and suppressing tumor growth. (unitn.it)
  • Patient organoids exhibited concordant responses to alisertib and allowed for the dynamic testing of Aurora-N-myc complex disruption. (unitn.it)
  • Conclusions: Although the study did not meet its primary endpoint, a subset of patients with advanced prostate cancer and molecular features supporting Aurora-A and N-myc activation achieved significant clinical benefit from single-agent alisertib. (unitn.it)
  • An AXL-specific inhibitor (bemcentinib) partly blocked PDGF-induced mobile proliferation and decreased phosphorylation of AXL and PDGF receptor as well as the downstream indicators (AKT1 and ERK1/2). (nipponkaigi-tokyo.com)
  • PURPOSE: Patritumab deruxtecan, or HER3-DXd, is an antibody-drug conjugate consisting of a fully human monoclonal antibody to human epidermal growth factor receptor 3 (HER3) attached to a topoisomerase I inhibitor payload via a stable tetrapeptide-based cleavable linker. (bvsalud.org)
  • Aurora kinases, so named because the scattered mitotic spindles generated by mutant forms resemble the Aurora Borealis, have gained a great deal of attention as possible anticancer drug targets. (wikipedia.org)
  • 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)
  • However, their potential is presently compromised by the threat of side effects and by a lack of pharmacological inhibitors of Myc. (nih.gov)
  • Pharmacological response data for targeted inhibitors of SRC, WNT, GSK3b, aurora kinase, PI3 kinase, and mTOR, showed significant differences in sensitivity across cell lines assigned to different subtypes. (tudelft.nl)
  • Verapamil is a calcium channel blocker and a potent and orally active first-generation P-glycoprotein (P-gp) inhibitor. (adooq.com)
  • Aurora kinase inhibitors are a putative drug class for treating cancer. (wikipedia.org)
  • This family of proteins includes a wide variety of classes, including CYCLIN-DEPENDENT KINASES, mitogen-activated kinases, CYCLINS, and PHOSPHOPROTEIN PHOSPHATASES as well as their putative substrates such as chromatin-associated proteins, CYTOSKELETAL PROTEINS, and TRANSCRIPTION FACTORS. (bvsalud.org)
  • The Aurora enzymes are particularly significant because they are involved in a direct path to the nucleosome by phosphorylating histone H3. (wikipedia.org)
  • These kinases lead to β-catenin stabilization through phosphorylation-dependent inactivation of GSK-3β either directly or indirectly. (lu.se)
  • Further, second-generation FLT3 inhibitors, such as AC220 and crenolanib, suppressed this signaling both in vitro and in vivo. (lu.se)
  • Cells were cleaned with ice-cold PBS and lysed on glaciers DRAK2-IN-1 with M-PER lysis buffer (Pierce Biotechnology, Inc) supplemented with protease and phosphatase inhibitors (Thermo Fisher Scientific). (nipponkaigi-tokyo.com)
  • PF-07321332 is an orally bioavailable 3C-like protease (3CLPRO) inhibitor. (adooq.com)
  • We observed that dexamethasone exposure caused upregulation of Aurora kinase and its various downstream effector kinases such as JAK, p38, mTOR, and S6K. (lu.se)
  • SCARA5 expression is significantly downregulated in various tumor tissues including liver cancer (LC), rectal cancer, and glioblastoma [ 15 , 16 ] and might affect cell proliferation and invasion abilities by the focal adhesion kinase (FAK) signaling pathway and epithelial-mesenchymal transition (EMT) [ 5 , 17 - 20 ]. (hindawi.com)
  • Aurora A influences centrosome maturation and spindle assembly, while Auroras B and C direct chromosome alignment and segregation. (rndsystems.com)
  • Plant-derived antigen was evaluated to induce FadD32 Inhibitor-1 the mucosal and systemic immune system responses in mice. (mslideas.com)
  • The hinge (yellow), glycine-rich loop (blue), and activation loop (red) are key features of the protein kinase fold involved in binding adenosine. (wikipedia.org)
  • The protein backbone atoms of residues Glu-211, Ala-213 in the hinge region of Aurora-2, and the sidechain of residue Trp-277, located in the activation loop, bind adenosine through specific hydrogen bonds. (wikipedia.org)
  • Kinomic profiling of principal mesangial cells treated with PDGF uncovered activation of many protein-tyrosine kinases, including AXL. (nipponkaigi-tokyo.com)
  • The research team used a genetically engineered mouse model to define the role of aurora kinases in early progression of the disease. (bio-itworld.com)
  • They identified and tested aurora kinase inhibitors, including AMG900, as an effective treatment to intercept lung cancer progression in the models. (bio-itworld.com)
  • BrdU cell proliferation assay was performed after incubation with PDGF-AB with or without inhibitors for 22 hours regarding to manufacturers guidelines (Roche Diagnostics). (nipponkaigi-tokyo.com)
  • Jones D, Noble M, Wedge SR, Robson CN, Gaughan L. Aurora A regulates expression of AR-V7 in models of castrate resistant prostate cancer . (ncl.ac.uk)
  • Indeed, we observed partial restoration of dexamethasone sensitivity with a combination of dexamethasone and inhibitors targeting either these kinases or β-catenin. (lu.se)
  • MK-0457, an Aurora kinase and BCR-ABL inhibitor, was studied on a Phase I/II study in 77 patients with refractory hematologic malignancies. (northwestern.edu)
  • 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)
  • Fragment-Based Discovery of the Pyrazol-4-yl urea (AT9283), a Multi-targeted Kinase Inhibitor with Potent Aurora Kinase Activity. (astx.com)
  • A promising new biomarker, SLFN11, has been identified which could predict response to a PARP inhibitor (plus a possible induced synergistic effect with immunotherapy) in SCLC. (medpagetoday.com)
  • Alert FDA Approves New Drug for Generalized Myasthenia Gravis Zilucoplan is the first once-daily, subcutaneous, self-administered, targeted C5 complement inhibitor for adults with gMG who are AChR antibody positive. (medscape.com)
  • The Aurora kinase family facilitates cell division through various processes and is overexpressed in a wide variety of human cancers, leading to aneuploidy. (usuhs.edu)