• 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)
  • TOP1 is the molecular target of camptothecin and related drugs such as irinotecan and SN38 (irinotecan's active metabolite). (hal.science)
  • Several derivatives of camptothecin, such as irinotecan and topotecan, have been developed and approved for the treatment of various cancers, including colorectal, lung, and ovarian cancers. (selfgrowth.com)
  • Camptothecin (CPT) is a topoisomerase inhibitor. (wikipedia.org)
  • In this study we focused our attention on the behavior of four nuclear matrix proteins during the various stages of apoptosis in the HL-60 cell line exposed to the DNA topoisomerase I inhibitor, camptothecin. (nih.gov)
  • 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)
  • At the cellular level, WRN loss results in rapid replicative senescence, chromosomal instability and sensitivity to various DNA damaging agents including the topoisomerase inhibitor, camptothecin (CPT). (brighton.ac.uk)
  • 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)
  • However, WS cells have been reported to show abnormal sensitivity to the drug camptothecin (an inhibitor of topoisomerase type I). A rapid assay for this sensitivity would be a useful marker of loss of wrn function. (brighton.ac.uk)
  • The presentation, "VIVACITAS ONCOLOGY PRESENTS OUR LEAD COMPOUND, AR-67, A NOVEL 3RD GENERATION CAMPTOTHECIN IN RECURRENT GLIOBLASTOMA," details AR-67 (Topoisomerase I Inhibitor) as a highly potent and novel lipophilic small molecule compound in a Phase II recurrent Glioblastoma Multiforme (reGBM) trial. (globenewswire.com)
  • 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)
  • Non-toxic camptothecin prodrugs are prepared by esterifying the 20-position hydroxyl group of camptothecin derivatives. (rti.org)
  • Camptothecin (CPT) analogues and derivatives serve as a novel class of effective anticancer agents that exert their action against DNA topoisomerase I. This paper presents procedures for the rapid, high frequency regeneration of a camptothecin producing plant, Ophiorrhiza prostrata D. Don from leaf and internode explants via shoot organogenesis. (ejbiotechnology.info)
  • The activity of the fluoroindenoisoquinolines was mostly correlated with camptothecin derivatives and the parent indenoisoquinolines, consistent with TOP1 targeting. (usuhs.edu)
  • Camptothecin and its derivatives are inhibitors of topoisomerase I, have known activity against several agricultural pests, and are also approved for the treatment of several cancers. (westminster.ac.uk)
  • 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)
  • Camptothecin is an alkaloid compound used as an anti-cancer agent. (goldbio.com)
  • Semisynthetic derivative of camptothecin, an alkaloid extract from the Camptotheca acuminate tree. (medscape.com)
  • The proposed tumor-cell targeted formulation was shown to be able to simultaneously host the model anticancer drug camptothecin and a pyrene-modified BODIPY fluorophore, based on dynamic light scattering, small-angle X-ray scattering, and cryogenic transmission electron microscopy. (unica.it)
  • Scholars@Duke publication: Molecular cloning of a cDNA of a camptothecin-resistant human DNA topoisomerase I and identification of mutation sites. (duke.edu)
  • The indenoisoquinolines LMP400, LMP744, and LMP776 are novel noncamptothecin TOP1 inhibitors in clinical trial, which overcome the limitations of camptothecins. (usuhs.edu)
  • 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)
  • Camptothecin (Camptotheca acuminata), (GoldBio Catalog # C-705) has also been produced by endosymbiotic fungi present in Camptotheca acuminata, which is a tree predominantly found in southern China. (goldbio.com)
  • Our experiments showed that camptothecins (CPTs) are primarily accumulated in glandular trichomes in Camptotheca. (benthamopen.com)
  • Camptothecin (CPT), first isolated from Chinese tree Camptotheca acuminate, produces rapid and prolonged inhibition of DNA synthesis and induction of DNA damage by targeting topoisomerase I (top1), which is highly activated in cancer cells . (bvsalud.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)
  • We identified rubitecan (a synthetic derivative of camptothecin) as a hit compound that reduced A. aegypti larval motility. (westminster.ac.uk)
  • In these patients, as well as in patients from the Phase I trial, no Grade 3 or 4 diarrhea was observed, which is one of the challenges of the earlier generation Camptothecin-based compounds. (globenewswire.com)
  • Camptothecin (CPT) induces down-regulation of topoisomerase I (TOP1) via an ubiquitin/26S proteasome pathway. (tmu.edu.tw)
  • We extended our investigation to adult mosquitoes and found that camptothecin increased lethality when delivered in a blood meal to A. aegypti adults at 100 µM and 10 µM, and completely blocked egg laying when fed at 100 µM. (westminster.ac.uk)
  • 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)
  • 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)
  • The 125- and 160-kDa proteins localized in the nucleolus and precisely within certain granules which are known to appear in the nucleolar area after camptothecin administration. (nih.gov)
  • This enzyme, which is the unique molecular target of the natural anticancer compound camptothecin, acts by nicking one DNA strand and forming a transient protein-DNA covalent complex. (mdpi.com)
  • To increase drug loading and combination therapy, we covalently conjugated paclitaxel (PTX) and camptothecin (CPT) through a disulfide linker into a prodrug, designated PTX-S-S-CPT. (abo.fi)
  • New Topoisomerase I mutations are associated with resistance to camptothecin. (hal.science)
  • 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)
  • 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)
  • Camptothecin has also been found in other plants including Chonemorpha fragrans. (wikipedia.org)
  • Camptothecin is found in Mappia foetida ( Nothapodytes foetida ), a plant native to eastern India. (goldbio.com)
  • Using this assay, we have found that a significantly increased level of strand breaks can be demonstrated in WS cells treated with camptothecin compared with normal controls. (brighton.ac.uk)
  • Camptothecin has been found to inhibit an enzyme called topoisomerase I, which plays a critical role in DNA replication and repair. (selfgrowth.com)
  • By inhibiting this enzyme, camptothecin prevents cancer cells from dividing and can induce cell death . (selfgrowth.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)
  • We are excited to present at this year's 5th Meridian Clinical Trials conference and share perspectives on developing new therapies in various disease areas to improve the lives of patients and to demonstrate AR-67's therapeutic potential in reGBM, as well as in other difficult-to-treat cancers for which Camptothecins are administered in combination therapies," said Tina Runk, EVP of Clinical Operations, Co-Founder, and Director of Vivacitas. (globenewswire.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)