• Camptothecin (CPT) is a topoisomerase inhibitor. (wikipedia.org)
  • Scholars@Duke publication: Molecular cloning of a cDNA of a camptothecin-resistant human DNA topoisomerase I and identification of mutation sites. (duke.edu)
  • Camptothecin (CPT), a plant alkaloid with antitumor activity, is a specific inhibitor of eukaryotic DNA topoisomerase I. We have previously isolated and characterized a CPT-resistant topoisomerase I isolated from a CPT-resistant human leukemia cell line, CPT-K5. (duke.edu)
  • We have shown that colorectal cancer cell lines defective in DNA MMR exhibit an increased sensitivity to both camptothecin, a topoisomerase I inhibitor, and etoposide, a topoisomerase II inhibitor. (aacrjournals.org)
  • He revealed the interfacial inhibition paradigm based on molecular mechanisms of topoisomerase inhibitors, and has championed its broad relevance for molecular pharmacology and drug discovery. (cancer.gov)
  • New Topoisomerase I mutations are associated with resistance to camptothecin. (hal.science)
  • Contrary to other anticancer targets, topoisomerase I (TOP1) is targeted by only one chemical class of FDA-approved drugs: topotecan and irinotecan, the derivatives of the plant alkaloid, camptothecin. (usuhs.edu)
  • In addition to its role in these fundamental processes, the biological importance of eukaryotic DNA topoisomerase I is underscored by its identification as the target of the antitumor alkaloid camptothecin. (northwestern.edu)
  • Conclusion Crystallographic, biochemical and genetic data indicate that this 26 kDa fragment of yeast DNA topoisomerase I is involved in complex formation between the enzyme and DNA, and probably also in camptothecin-enzyme-DNA ternary complex formation. (northwestern.edu)
  • The antitumor drug camptothecin (CPT) and its analogs inhibit the rejoining step of the breakage/rejoining reaction, which traps the enzyme in covalent linkage with DNA (the cleavable complex). (tmu.edu.tw)
  • However, it has low solubility and adverse effects have been reported when used therapeutically, so synthetic and medicinal chemists have developed numerous syntheses of camptothecin and various derivatives to increase the benefits of the chemical, with good results. (wikipedia.org)
  • The activity of the fluoroindenoisoquinolines was mostly correlated with camptothecin derivatives and the parent indenoisoquinolines, consistent with TOP1 targeting. (usuhs.edu)
  • Camptothecin (CPT) and its derivatives are considered to be among the most effective anticancer drugs of the 21st century. (spiritindia.com)
  • 2020). Based on their promising clinical activity and their superior medicinal properties over the camptothecins, the indenoisoquinolines represent the first non-camptothecin TOP1 inhibitors for the treatment of cancers. (cancer.gov)
  • TOP1 is the molecular target of camptothecin and related drugs such as irinotecan and SN38 (irinotecan's active metabolite). (hal.science)
  • The indenoisoquinolines LMP400, LMP744, and LMP776 are novel noncamptothecin TOP1 inhibitors in clinical trial, which overcome the limitations of camptothecins. (usuhs.edu)
  • Nuclease treatment of the cell lysate to remove the covalently linked DNA from TOP1 revealed a distinct ladder of higher molecular weight bands having properties indicative of multi-ubiquitin (Ub) conjugates of TOP1. (tmu.edu.tw)
  • In a paper scheduled to be published in the nanoscience journal Small in June, researchers from UCLA?s California NanoSystems Institute and Jonsson Cancer Center report a novel approach using silica-based nanoparticles to deliver the anticancer drug camptothecin and other water-insoluble drugs into human cancer cells. (spiritindia.com)
  • Tamanoi and Zink devised a method for incorporating the representative hydrophobic anticancer drug camptothecin into the pores of fluorescent mesoporous silica nanoparticles and delivering the particles into a variety of human cancer cells to induce cell death. (spiritindia.com)
  • Nanoscale structures and materials such as nano?bers, colloidal nanoparticles, nanorods, nanowires, nanotubes and nanozymes have been investigated in many areas such as food safety, biosensing, molecular imaging, delivery of drugs, tissue engineering and anticancer treatment[ 3 - 5 ]. (ijpsonline.com)
  • To engineer these high-specificity drugs, they formed rod-shaped nanoparticles from a chemotherapeutic drug, camptothecin, and coated them with an antibody called trastuzumab that is selective for certain types of cancer cells, including breast cancer. (innovations-report.com)
  • Molecular complexes of topo I and topo II inhibitors from camptothecin and flavonoid families with model DNA oligomers. (science24.com)
  • Here we present the molecular docking study results of mTOR receptor bound to several ATP-competitive inhibitors. (springeropen.com)
  • The study is led by Fuyu Tamanoi, UCLA professor of microbiology, immunology and molecular genetics and director of the Jonsson Cancer Center?s Signal Transduction and Therapeutics Program Area, and Jeffrey Zink, UCLA professor of chemistry and biochemistry. (spiritindia.com)
  • Gunasekera earned a master's degree in bio-organic chemistry from the University of Houston-Clear Lake, a master's in molecular genetics and a doctorate in Biomedical Sciences at the Baylor University Medical Center in Dallas. (biola.edu)
  • The study was conducted jointly in the laboratories of Fuyu Tamanoi, a UCLA professor of microbiology, immunology and molecular genetics and director of the signal transduction and therapeutics program at UCLA's Jonsson Comprehensive Cancer Center, and Jeffrey Zink, a UCLA professor of chemistry and biochemistry. (uclahealth.org)
  • From the dynamic light scattering measurements, the hydrodynamic diameter values of camptothecin-loaded alkyldimethylamine oxide and nonionic micelles were found in the range of 4-42 nm and 5-120 nm, respectively. (edu.pl)
  • The values of the packing parameter of camptothecin-loaded dodecyldimethylamine oxide micelles indicate their spherical shape at all the investigated surfactant concentrations. (edu.pl)
  • In the current study, we demonstrate a strategy to coordinate the release of camptothecin (CPT) and α-tocopherylsuccinate (TOS) from hybrid micelles for nucleus and mitochondrion interferences. (statsignals.com)
  • An understanding of the mechanism of catalysis and interactions with camptothecin and other drugs has been hampered by a lack of detailed structural information. (northwestern.edu)
  • Camptothecin is an important chemotherapeutic agent used in the treatment of several cancers and most commonly used as first line drug in treatment of colon cancer. (jptcp.com)
  • Molecular Cancer Therapeutics , 17 (8), 1694-1704. (usuhs.edu)
  • Whereas, the role of circXRCC5 in glioma and its underlying molecular mechanism has not been reported. (bvsalud.org)
  • In the present study, a bioinformatics approach was used to investigate the molecular mechanisms and prognosis of ACC. (cancerindex.org)
  • This comprehensive review synthesizes current scientific literature to provide an in-depth analysis of various facets of the disease, including its molecular mechanisms, risk factors, emerging therapies, quality of life, supportive care, and economic impact. (pexacy.com)
  • The exploration still largely relies on serendipitous, because the construction requires a perfectly stable equilibrium among a series of complicated and meticulous balances, including amphipathicity, intermolecular interactions, chirality, and spatial molecular arrangement 20 . (nature.com)
  • The molecular interactions were validated using RIP and pull-down assays. (bvsalud.org)
  • 3. Ojima I. Guided molecular missiles for tumor-targeting chemotherapy case studies using the second-generation taxoids as warheads. (jptcp.com)
  • Furthermore, the underlying molecular mechanism of carcinogenesis is poorly understood, and prognostic prediction of ACC has low accuracy. (cancerindex.org)
  • Interestingly, our observations provide the rationale for the better responsiveness of MSI+ tumors to CPT-11, a camptothecin derivative, which we have observed in patients with metastatic colorectal cancers. (aacrjournals.org)
  • The treatment of mice with camptothecin-loaded MSNs led to shrinkage and regression of xenograft tumors. (uclahealth.org)
  • To solve these problems, an amphiphilic polymer-drug conjugate was prepared by attachment of low molecular weight (ie, 2 kDa) methoxy poly(ethylene glycol) methyl ether (mPEG) to gambogic acid (GA-mPEG 2000 ) through an ester linkage and characterized by 1H nuclear magnetic resonance. (dovepress.com)
  • Tests of the growth inhibition potential of MEC in seven human tumor cell lines showed that the compound was approximately 2-18-fold more cytotoxic than lurtotecan, topotecan, and 7-ethyl-10-hydroxy-20(S)-camptothecin (SN-38). (eur.nl)
  • The solubilisation of poorly soluble antineoplastic drug camptothecin by nonionic surfactants (polysorbates and octylphenol ethoxylates) and alkyldimethylamine oxide surfactants with the alkyl chain length 8 to 16 carbon atoms was investigated. (edu.pl)
  • However, prospective identification of targets in the clinic will not only illuminate their clinical significance, but will also further accelerate drug development-witness the way in which the introduction of gefitinib (Iressa) for lung cancer was followed in less than a decade by the identification of driver mutations, new targeted drugs, and the universal adoption of molecular profiling for treatment selection. (cancernetwork.com)
  • Additionally, GBM is characterized by high inter-tumor and intra-tumor heterogeneity at a cellular, molecular, histological, and clinical level leading to very different responses to therapeutic agents and failure of targeted therapies ( 9 , 10 ). (frontiersin.org)
  • A molecular model for protein-DNA interaction based on these data is proposed. (northwestern.edu)
  • TIAs have a wide variety of different molecular structures and biological activities [ 11 ]. (biomedcentral.com)
  • GO organizes genes into hierarchical categories based on biological process, molecular function and subcellular localization. (scienceopen.com)
  • Functional analyses were performed on these cell lines challenged with SN38 and we specifically monitored the double strands breaks with gammaH2AX staining and replication activity with molecular combing. (hal.science)
  • Near-Infrared Light Activates Molecular Nanomachines to Drill into and Kill Cells," Liu, D. (biola.edu)
  • Lysates from control (lanes 1-3) and camptothecin treated Jurkat cells (lanes 4-6) were probed with anti-human caspase-8 (clone 4-1-20, Cat. (bdbiosciences.com)
  • Mitragotri and collaborators at UCSB, including post-doctoral researchers Sutapa Barua and Jin-Wook Yoo, and former graduate student Poornima Kolhar, looked to human breast cancer cells to examine how shape works in synergy with molecular recognition to perform complex tasks within the human body. (innovations-report.com)
  • Personalized medicine and the need for molecular profiling have justifiably become the Holy Grail for the development of future successful weapons against cancer. (cancernetwork.com)
  • A simple computer model of camptothecin-loaded dodecyldimethylamine oxide micelle provided the diameter of the structure cross section which is consistent with the experimental values. (edu.pl)
  • 2012) Directeur, axe de recherche en imagerie médicale et radiothérapie. (usherbrooke.ca)
  • Camptothecin has also been found in other plants including Chonemorpha fragrans. (wikipedia.org)
  • 1992 ) to simulate chemical structures of the molecules at their minimum potential energy or most stable state in a real chemical system before subjecting them to the molecular docking process (Table 1 ). (springeropen.com)
  • The decreasing number of oxyethylene units and the extension of the hydrophobic part of nonionic surfactant molecule resulted in the increase of camptothecin solubility. (edu.pl)
  • Nuclear magnetic resonance data indicate that cleavage of the piperazino moiety occurred at the N-C bond of the B-ring, yielding 7-methyl-10,11-ethylenedioxy-20(S)-camptothecin (MEC). (eur.nl)
  • Additional studies have also shown that hemolymph from the silkworm ( Bombyx mori ) can inhibit insect and mammalian cell apoptosis that is induced by viruses and several chemical inducers, such as staurosporine, camptothecin, and actinomycin D [ 6 - 8 ]. (hindawi.com)
  • The chemical structures of metabolites were elucidated by comparing the retention time, accurate molecular mass, and fragmentation patterns of analytes with those of PPD. (westminster.ac.uk)
  • In addition, individuals in the low-risk group were more susceptible to axitinib and camptothecin, whereas lapatinib might be preferred for patients in the high-risk group. (hindawi.com)
  • Animals were divided into four groups: Group I: normal control, Group II: DMH treated, Group III: DMH+ CPT-SS-Biotin treated and Group IV: DMH+ standard camptothecin. (jptcp.com)