IrinotecanDerivativesInhibitorAnalogsAlkaloidAnticancer drugHuman DNA topoisomeraseInhibitorsCamptothecaDerivativeTopotecanTOP1CompoundAdultMicellesReplicationProteinsProdrugResistanceDrugFoundCancerIncreaseNormalChemotherapyConjugateTopoisomerase inhibitorCompoundsEndophyteTree Camptotheca acuminataToxicitiesHPLCClinicalChonemorphaSustainableYieldRetainEvaluationPlantProductionCellsPowerfulEffectivePhasePlantsPriceProcessPatientsChemical
Irinotecan3
- 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)
Derivatives5
- 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)
Inhibitor6
- 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)
Analogs1
- 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)
Alkaloid2
- 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)
Anticancer drug1
- 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)
Human DNA topoisomerase1
Inhibitors1
- The indenoisoquinolines LMP400, LMP744, and LMP776 are novel noncamptothecin TOP1 inhibitors in clinical trial, which overcome the limitations of camptothecins. (usuhs.edu)
Camptotheca3
- 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)
Derivative2
- 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)
Topotecan1
TOP11
- Camptothecin (CPT) induces down-regulation of topoisomerase I (TOP1) via an ubiquitin/26S proteasome pathway. (tmu.edu.tw)
Compound1
Adult1
- 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)
Micelles3
- 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)
Replication1
- Camptothecin has been found to inhibit an enzyme called topoisomerase I, which plays a critical role in DNA replication and repair. (selfgrowth.com)
Proteins1
- 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)
Prodrug1
- 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)
Resistance1
- New Topoisomerase I mutations are associated with resistance to camptothecin. (hal.science)
Drug2
- 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)
Found3
- 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)
Cancer1
- By inhibiting this enzyme, camptothecin prevents cancer cells from dividing and can induce cell death . (selfgrowth.com)
Increase1
- 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)
Normal1
- 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)
Chemotherapy2
- The chemotherapy drug camptothecin and ionizing radiation both attack cancer cells by causing double-strand DNA breaks. (news-medical.net)
- This led to the discovery that the chemotherapy drug camptothecin dissociates SENP6 from RPA70, allowing it to be modified by SUMO 2/3. (news-medical.net)
Conjugate3
- CRLX101 is a nanoparticle-drug conjugate with a camptothecin payload. (medscape.com)
- Schematic Structure of an Antibody-Drug Conjugate (ADC) (en.wikipedia.org) Invention Summary: Topoisomerase 1 (Top1) is an essential enzyme in mammalian cells and is a validated target for the treatment of human cancers. (researchwithnj.com)
- Formulated with Sonus' proprietary vitamin-E based TOCOSOL technology, TOCOSOL Camptothecin is a novel camptothecin compound that is a conjugate of SN-38. (iptoday.com)
Topoisomerase inhibitor1
- Camptothecin (CPT) is a topoisomerase inhibitor. (wikipedia.org)
Compounds2
- The active drug in this study belongs to a family of camptothecins, compounds known to promote cell death and destroy tumors. (eurekalert.org)
- Today, all the camptothecin products approved worldwide can be produced with Fermions manufacturing process, which is extremely reproducible and shows a lower impurity profile compared to nature-derived compounds. (pharmaceutical-business-review.com)
Endophyte3
- Hence, this research aims to establish a sustainable and high Camptothecin yielding endophyte, as an alternative source for commercial production of Camptothecin. (expresspharma.in)
- Production and bioprocessing of camptothecin from Aspergillus terreus, an endophyte of Cestrum parqui, restoring their biosynthetic potency by Citrus limonum peel extracts. (bvsalud.org)
- Aspergillus terreus ON908494.1, an endophyte of Cestrum parqui was morphologically and molecularly verified, displaying the most potent camptothecin biosynthetic potency . (bvsalud.org)
Tree Camptotheca acuminata1
- Camptothecin is a natural product derived from the Oriental tree Camptotheca acuminata which has shown activity in a number of experimental tumors. (nih.gov)
Toxicities1
- Similarly to other camptothecins, the identified dose-limiting toxicities for AR-67 were neutropenia, thrombocytopenia and fatigue. (uky.edu)
HPLC1
- The chemical identity of A. terreus camptothecin was confirmed from the HPLC , FTIR and LC-MS/MS analyses, gave the same molecular structure and mass fragmentation patterns of authentic one. (bvsalud.org)
Clinical3
- AR-67 is a lipophilic third generation camptothecin analogue, currently under early stage clinical trials. (uky.edu)
- TOCOSOL Camptothecin is in a Phase 1 clinical trial that was initiated in September 2006. (iptoday.com)
- In addition to the continuing development of TOCOSOL Paclitaxel, Sonus moved its second product candidate, TOCOSOL Camptothecin, into a Phase 1 clinical trial in September 2006. (iptoday.com)
Chonemorpha1
- Camptothecin has also been found in other plants including Chonemorpha fragrans. (wikipedia.org)
Sustainable2
- Elaborating on the technical aspects of the research, Khwajah Mohinudeen, an IIT Madras PhD Research Scholar who worked on this study, said, "Researchers from the Plant Cell Bioprocessing laboratory at IIT Madras have been able to successfully isolate the highest-yielding strain of Camptothecin reported to date with sustainable production up to reactor level. (expresspharma.in)
- The feasibility of complete restoring of camptothecin biosynthetic- machinery of A. terreus for stable and sustainable production of camptothecin , pave the way for using this fungal isolate as new platform for scaling-up the camptothecin production . (bvsalud.org)
Yield4
- So, the optimal medium components for maximum yield of camptothecin by A. terreus was acid why (2.0 mL/L), Diaion HP20 (2.0 g/L), Amberlite XAD (2.0 g/L), dextrin (5.0 g/L), glucose (10.0 g/L), salicylic acid (2.0 g/L), serine (4.0 g/L), cysteine (4.0 g/L) and glutamate (10.0 g/L), at pH 6 for 15 days incubation. (bvsalud.org)
- By the 5th generation of A. terreus, the camptothecin yield was reduced by 60%, comparing to zero culture . (bvsalud.org)
- Evaluation of biomass and camptothecin production showed that the PGRs influenced biomass and CPT yield of the callus cultures. (notulaebiologicae.ro)
- Optimization of camptothecin production and biomass yield from endophytic fungus Fusarium solani strain ATLOY-8. (notulaebiologicae.ro)
Retain1
- In this thesis, the method development and investigation of different liposomal formulations to incorporate and retain Camptothecin (CPT) is described. (uit.no)
Evaluation1
- Somatic embryogenesis, plant regeneration, and evaluation of camptothecin content in Nothapodytes foetida. (notulaebiologicae.ro)
Plant1
- Nearly 1,000 tons of plant material is required to extract just one ton of Camptothecin. (expresspharma.in)
Production2
- IIT Madras Researchers have now developed an alternative method of Camptothecin production to meet the demand and conserve the natural sources. (expresspharma.in)
- The metabolic potency of fungi as camptothecin producer elevates their prospective use as an industrial platform for commercial production , however, the loss of camptothecin productivity by fungi with the storage and subculturing are the major obstacle. (bvsalud.org)
Cells2
- HeLa cells, incubated with camptothecin during the G 1 phase of the cell cycle, show nuclear fluorescence with fluorescein-labeled antinucleoside antibodies. (elsevierpure.com)
- The purified putative camptothecin displayed a strong anticancer activity towards HepG-2 and MCF-7 with IC50 values 0.96 and 1.4 µM, respectively, with no toxicity to OEC normal cells . (bvsalud.org)
Powerful1
- As well as, the purified camptothecin displayed a significant antifungal activity towards fungal human pathogen Candida albicans , Aspergillus flavus , and A. parasiticus, ensuring the unique structural activity relationships of A. terreus camptothecin , as a powerful dually active anticancer and antimicrobial agent . (bvsalud.org)
Effective1
- We can provide you with the safest and most effective Camptothecin. (buyextracts.com)
Phase2
- Phase I/II trial of nano-camptothecin CRLX101 with capecitabine and radiotherapy as neoadjuvant treatment for locally advanced rectal cancer. (medscape.com)
- With pivotal Phase 3 data expected in the third quarter of 2007 for TOCOSOL Paclitaxel, our lead product candidate, coupled with the potential for TOCOSOL Camptothecin and additional preclinical pipeline opportunities, we are continuing our commitment to build a portfolio of innovative drugs that will provide added benefits for cancer patients. (iptoday.com)
Plants1
- Thus, screening for endophytic fungal isolates inhabiting ethnopharmacological plants with an obvious metabolic stability and sustainability for camptothecin biosynthesis could be one of the most feasible paradigms. (bvsalud.org)
Price1
- Where can i purchase Camptothecin price and where to get Camptothecin for sale? (buyextracts.com)
Process1
- When a mutant that cannot be SUMOylated is substituted for RPA70, the repair process is defective, giving the cell increased sensitivity to camptothecin and radiation. (news-medical.net)
Patients1
- 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)
Chemical1
- Interestingly, the productivity of camptothecin by A. terreus has been completely restored and over increased (210 µg/L), comparing to the 3rd generation A. terreus (90 µg/L) upon addition of methanolic extracts of Citrus limonum peels, revealing the presence of some chemical signals that triggers the camptothecin biosynthetic machinery . (bvsalud.org)