Kinesin spindle protein inhibitor

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Web23 feb. 2024 · BOS172722 (CCT289346) is a highly potent, selective, and orally bioavailable inhibitor of spindle assembly checkpoint kinase … WebDaniel Barbosa obtained an Integrated Master in Pharmaceutical Sciences in 2009, and a PhD in Pharmaceutical Sciences - Specialty of Toxicology in 2013, at Faculty of Pharmacy, University of Porto. His main areas of research are Neuroscience and Cell Division. Presently, he is especially interested in elucidating the mechanistic details of dynactin’s …

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Web15 apr. 2005 · Kinesin spindle protein (KSP) inhibitors. Part 1: The discovery of 3,5-diaryl-4,5-dihydropyrazoles as potent and selective inhibitors of the mitotic kinesin KSP … Web1 dec. 2008 · Kinesin spindle protein (KSP), a member of the kinesin superfamily of microtubule-based motors, plays a critical role in mitosis as it mediates centrosome … peters glen shadehouses \u0026 shelving

A Phase I-II Trial of Ispinesib, a Kinesin Spindle Protein Inhibitor ...

WebA phase I study of ispinesib, a kinesin spindle protein inhibitor, administered weekly for three consecutive weeks of a 28-day cycle in patients with solid tumors Invest New … In drug screening assays, we discovered that mitotic inhibitors targeting microtubules were within the top effective agents, including 5 conventional drugs (paclitaxel, docetaxel, cabazitaxel, vincristine sulfate, and cephalomannine) and one novel alternative, the KSP inhibitor SB743921. We focused … Meer weergeven To explore the potential drugs, we used four CCA cell lines for an untargeted high-throughput drug screen, including TFK1, CCLP1, MZ-CHA-1, and SK-CHA-1. Cells were seeded in 384-well plates and incubated … Meer weergeven To investigate the therapeutic value of KSP inhibitors in vivo, CCA cell lines were subcutaneously injected into nude mice to establish cell line-derived xenograft (CDX) models. Mice were randomly allocated to control or … Meer weergeven Next, we assessed the correlation between differentially expressed KSP-encoding gene KIF11 and clinical prognosis using the Human Protein Atlas (HPA) … Meer weergeven To further elucidate the mechanism of KSP inhibition in CCA, we performed RNA sequencing (RNA-seq) on CCLP1 cells after treatment with SB743921 (10 nM) for 8 and 16 h. … Meer weergeven WebModified Peptide Inhibitors of the Keap1-Nrf2 Protein-Protein Interaction Incorporating Unnatural Amino Acids Chembiochem 2024 Other authors Ligand- and structure-based in silico studies to... peters golvservice

Kinesin Spindle Protein (KSP) Inhibitors in Combination with ...

WebA phase I study of ispinesib, a kinesin spindle protein inhibitor, administered weekly for three consecutive weeks of a 28-day cycle in patients with solid tumors Invest New Drugs . 2011 Jun;29(3):467-72. doi: 10.1007/s10637-009-9374-x. WebCentrosome amplification is a hallmark of many types of cancer cells, and clustering of multiple centrosomes is critical for cancer cell survival and proliferation. Human kinesin-14 HSET/KFIC1 is essential for centrosome clustering, and its inhibition leads to the specific killing of cancer cells with extra centrosomes. starship logistics distribution 2018 incWeb14 jan. 2010 · Inhibitors of kinesin spindle protein (KSP) have emerged as candidate nonneurotoxic antimitotic cancer therapies. One of these KSP inhibitors, ispinesib, has been evaluated in a phase II clinical trial in women with locally advanced or metastatic breast cancer, producing several partial responses. starship logistics montreal

"WebDiscovery and Mechanistic Study of a Small Molecule Inhibitor for Motor Protein KIFC1 . × Close Log In. Log in with Facebook Log in with Google. or. Email. Password. Remember … " - Kinesin spindle protein inhibitor

Kinesin spindle protein inhibitor

(PDF) Discovery and Mechanistic Study of a Small Molecule Inhibitor …

WebExamples of such radiosensitizing agent include inhibitors of one or more of the following: Kif2b, MCAK, MPS1, Eg5/Kinesin-5 5, Polo-like kinase 4, MCAK, Bub1 and Hec1. Such agents specifically target proteins involved in maintaining or promoting faithful chromosome segregation. Log In Sign Up. Find a Lawyer; Web18 apr. 2024 · Kinesin spindle proteins (KSP) belonging to the kinesin-5 family play a crucial role during mitosis and unregulated cell proliferation. Evidence from preclinical studies and different phases of clinical trials have presented kinesin spindle protein as a promising target for cancer therapeutics.

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Web20 aug. 2014 · We also present results from a pilot lentiviral RNAi screen for kinases whose silencing modulates sensitivity to a mitotic spindle protein kinesin-5 inhibitor (kinesin-5i). Our… Show more Web21 feb. 2024 · Kinesin spindle protein inhibitors in cancer: from high throughput screening to novel therapeutic strategies. Bringing to a halt the cell cycle in …

WebIspinesib (SB-715992, CK0238273) is a potent, specific and reversible inhibitor of kinesin spindle protein (KSP) with Ki app of 1.7 nM in a cell-free assay, no inhibition to CENP-E, … Web21 feb. 2024 · KSP inhibitors are sub-divided into two main groups according to their mechanism of interaction within the KSP protein: 1. KSP (α2/loop L5/helix α3) inhibitors also named ATP uncompetitive 2. KSP (helix-α4 and -α6 pocket) inhibitors also named ATP binding competitive inhibitors KSP (α2/loop L5/helix α3) binding allosteric inhibitors

Web15 dec. 2009 · DOI: 10.1158/0008-5472.SABCS-09-6103 Corpus ID: 71978387; A Phase I-II Trial of Ispinesib, a Kinesin Spindle Protein Inhibitor, Dosed Every Two Weeks as First Line Chemotherapy for Advanced Locally Recurrent or Metastatic Breast Cancer.

Web29 okt. 1999 · A chemical genetic suppression screen to identify compounds that restore spindle bipolarity in cells treated with Monastrol, an inhibitor of the mitotic kinesin Eg5, revealed novel unexpected insights into the mechanism of …

WebDiscovery and Mechanistic Study of a Small Molecule Inhibitor for Motor Protein KIFC1 . × Close Log In. Log in with Facebook Log in with Google. or. Email. Password. Remember me on this computer. or reset password. Enter the email address you signed up … starship logistics llcWeb21 aug. 2013 · KSP is essential for the proper separation of spindle poles during mitosis. Agents that target KSP selectively act on cells undergoing cell division, which means that … starship logistics ottawaWebInhibitors of Kinesin Spindle Protein (KSP) have emerged as candidate non-neurotoxic anti-mitotic cancer therapies. One of these KSP inhibitors, ispinesib, has been evaluated in a Phase II clinical trial in women with … starship live youtubeWeb11 apr. 2024 · From this FACS-sorted polyclonal cell line, monoclonal cell lines were derived and screened for efficient Kin14VIb-mediated poleward transport using a simple high-throughput assay: cells treated with the Eg5 inhibitor STLC were scored for their capacity to recruit the dCas9-GFP-3xFKBP-bound loci toward the centrosomes of a monopolar … starship lobeliaWebHowever, a different endogenous kinesin Kif15 is capable of driving bipolar spindle assembly/maintenance in the absence of KSP activity, which leads to resistance against KSP inhibitors. Citation 106–108 It has been reported that Kif15 behavior is associated with dynamic microtubules, ie, Kif15 motility is suppressed by the reduction of microtubule … starship live camWebKSP (Eg5) Inhibition - Theory and Expreimental Studies The Kinesin Spindle Protein (KSP; also known as Eg5 or KIF11) is a Kinesin-5 subfamily member and has been the focus of a significant drug development effort throughout the … starship loginWeb1 apr. 2006 · Mitotic kinesins are microtubule-associated motor proteins that utilize the energy from ATP hydrolysis for bipolar spindle assembly, maintenance and elongation, … starship locations