Camptothecin metabolism

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August undefined, 2024

WebOct 1, 2006 · a Camptothecin is a 5-ring heterocyclic alkaloid that contains an a-hydroxylactone within its E-ring that is unstable at physiological pH. For all camptothecin derivatives, the carboxylate... WebJul 1, 2005 · 7-Ethyl-10-hydroxy-camptothecin (SN-38), the active metabolite of the anti-cancer agent irinotecan, contains a lactone ring that equilibrates with a carboxylate form. Since SN-38 lactone is the active and toxic form, it is prudent to examine whether the more soluble carboxylate is a surrogate for SN-38 lactone conjugation. Therefore, relative …

Topotecan: Uses, Interactions, Mechanism of Action - DrugBank

WebA recent study confirmed that Camptothecin could downregulate SLC25A6 and induce apoptosis in a mitochondria-dependent pathway . SLC25A6 isoforms are expressed in all tissues and in cultured fibroblasts at levels that depend on the state of oxidative metabolism [ … WebMar 1, 1990 · A new water-soluble derivative of camptothecin, 7-ethyl-10-[4-(1-piperidino)-1-piperidino]carbonyloxycamptothecin (CPT-11), did not exhibit potent antitumor activity … phone with best software

Clinical Pharmacokinetics and Metabolism of Irinotecan …

WebApr 13, 2024 · It is a semisynthetic analog of camptothecin, which was originally isolated from the Chinese/Tibetan ornamental tree Camptotheca acuminata [1,2,3]. Resistance model-based studies uncovered several mechanisms of cellular resistance to this agent and, accordingly, multiple approaches were tested in clinical trials to circumvent the … WebJun 10, 2024 · On the basis of annotated metabolites and enzymes identified 11, the camptothecin biosynthetic pathway in C. acuminata is similar to that of some other MIAs, such as vinblastine and vincristine... WebPurpose: Camptothecin (CPT) is a potent topoisomerase I inhibitor that has recently been undergoing phase I clinical trials. Though CPT shows high activity against various tumor … how do you spell observe

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Metabolism of camptothecin, a potent topoisomerase I

WebThe hairy roots (HR) of Ophiorrhiza pumila produce camptothecin (CPT), a monoterpenoid indole alkaloid used as a precursor in the synthesis of chemotherapeutic drugs. O. pumila HR culture is considered as a promising alternative source of CPT, WebOct 14, 2024 · The active metabolite ethyl-10-hydroxy-camptothecin (SN38) has been shown to significantly increase expression of p53 protein and pro-apoptosis proteins Bax, caspase-3, and caspase-9 in human hepatocellular carcinoma cell lines, and meanwhile decrease expression of the anti-apoptosis protein B-cell lymphoma (Bcl)-xL ( Takeba et … phone with best selfie cameraWebDec 1, 1999 · Camptothecin Resistance: Role of the ATP-binding Cassette (ABC), Mitoxantrone-resistance Half-Transporter (MXR), and Potential for Glucuronidation in MXR-expressing Cells. ... Although the importance of glucuronidation in hepatic drug metabolism is well known, it has received little attention as a possible mechanism of resistance in … phone with best sound quality

"WebJan 14, 2024 · Camptothecin, first reported in 1966 1, is a monoterpene indole alkaloid. It is commercially produced from plants, mainly Camptotheca acuminata and Nothapodytes … " - Camptothecin metabolism

Camptothecin metabolism

Metabolism of camptothecin, a potent topoisomerase I

WebIrinotecan (CPT-11) is a water-soluble derivative of camptothecan that inhibits topoisomerase I, a key enzyme for DNA replication and repair. The main side-effects of irinotecan are myelosuppression and severe diarrhea. Web9-Aminocamptothecin (9-amino-CPT) 是一种拓扑异构酶I的抑制剂，具有抗肿瘤活性。9-氨基喜树碱（处理96小时）对PC-3、PC-3M、DU145和LNCaP细胞抑制作用的IC50值分别为34.1、10、6.5和8.9 nM。立即从AbMole中国订购高品质Topoisomerase抑制剂9-Aminocamptothecin！

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Web5μM Camptothecin作用于HCT116细胞，诱导蛋白酶体调节的混合系白血病5(MLL5)蛋白降解，导致p53在Ser392位点磷酸化。由于Camptothecin的溶解性低及具有一定副作用，所以已经研发了多种Camptothecin类似物，其中两种如Topotecan和Irinotecan,已经获得FDA准核，用于癌症化学疗法中。 WebOct 15, 2024 · Camptothecin is a planar pentacyclic quinoline alkaloid with a molecular formula of C 20 H 16 N 2 O 4, and is insoluble in water. Ring A and B are quinoline rings, ring C is pyrrole ring, ring D is pyridone ring, and ring E is α-hydroxy lactone ring.

WebCamptothecin. Camptothecin is a naturally occurring alkaloid derived from the plant Camptotheca acuminata that was identified in an anticancer drug discovery screen in the … WebSep 11, 2007 · Camptothecin is an alkaloid isolated from the stem wood of the Chinese tree, Camptotheca acuminata. This compound selectively inhibits the nuclear enzyme DNA topoisomerase, type I. Several semisynthetic analogs of camptothecin have demonstrated antitumor activity. Type Small Molecule Groups Experimental Structure Similar …

WebBackground: Poly (lactic- co -glycolic acid) (PLGA) has emerged as a promising anticancer drug delivery scaffold. Camptothecin (CPT) has been fabricated into a variety of nano-sized formulations to improve drug action. We report an experimental study on the effect of CPT-encapsulated PLGA (PLGA-CPT) nanoparticles (NPs) on drug-metabolizing ... WebMar 15, 1990 · A new water-soluble derivative of camptothecin, 7-ethyl-10-[4-(1-piperidino)-1-piperidino]carbonyloxycamptothecin (CPT-11), did not exhibit potent …

WebJun 13, 2024 · Camptothecin is a potent anticancer drug which inhibits the enzyme, deoxyribonucleic acid topoisomerase I, during the S-phase of cell cycle (Zunino et al. 2002 ). Deoxyribonucleic acid topoisomerase I is an enzyme which is essential for replication and transcription of deoxyribonucleic acid.

WebApr 1, 2011 · 7- tert -Butyldimethylsilyl-10-hydroxycamptothecin (AR-67; also known as DB-67) is a novel lipophilic camptothecin analog in early-phase anticancer clinical trials. In … how do you spell obviouslyWebJan 1, 2024 · The camptothecin biosynthesis pathway is complex and only partly resolved. Camptothecin biosynthesis uses intermediates of the iridoid and shikimate pathways, which converge to form the... phone with best batteryWebMay 16, 2014 · Specialties: Bioinformatics, R, Linux, Gene Sequencing, Biomarker discovery, Environmental Health Sciences, Toxicology, Radiation Oncology Learn more about Karan B.'s work experience, education ... phone with best video stabilizationWebApr 10, 2024 · The compound camptothecin showed hydrogen bond interaction with A:TYR73, A:ASN69, and A:SER60, while hydrophobic interaction with A: ... could bind to the interface of the DNA-topoisomerase I complex of M. oryzae and affect the translation and carbohydrate metabolism/energy metabolism leading to cell death [59]. phone with audio jack 2022WebJan 14, 2024 · Camptothecin, first reported in 1966 1, is a monoterpene indole alkaloid. It is commercially produced from plants, mainly Camptotheca acuminata and Nothapodytes nimmoniana 2. how do you spell occasionalWebMay 1, 2024 · The camptothecin-derived agents exert their antitumor activities by specifically stabilizing the Top1–DNA covalent complexes (Top1cc) and blocking the DNA religation step. When exposed to these DNA damage agents, tumor cells quickly activate DNA damage response. phone with big buttons for seniorsWebDec 31, 2013 · Camptothecin (CPT) is a water-insoluble tryptophan-derived quinolone alkaloid and is a lead compound for two FDA (Food and Drug Administration) approved antineoplastic drugs, irinotecan and... phone with big camera