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Journal: Interaction of Camptothecin Anticancer Drugs with Ribosomal Proteins L15 and L11: A Molecular Docking Study. (Pubmed Central) - Mar 2, 2023 The mechanism is common to camptothecins SN38 (the active metabolite of irinotecan) and belotecan (BLT)...The main camptothecin structural elements implicated in the ribosomal protein interaction are the lactone moiety, the aromatic system and the 10-hydroxyl group. The study provides guidance to the design of modulators of ribosomal proteins L11 and L15, both considered anticancer targets.
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Journal: The design and discovery of topoisomerase I inhibitors as anticancer therapies. (Pubmed Central) - Jul 31, 2022 Currently, their limitations are being addressed by different stretegies. Future studies should focus not only on developing other active molecules but also on improving the bioavailability and pharmacokinetics of potent synthetic derivatives.
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[VIRTUAL] GlycoConnect™ ADCs based on topoisomerase 1 inhibitor exatecan (SYNtecan E™) show excellent in vivo efficacy and tolerability () - Mar 11, 2021 - Abstract #AACR2021AACR_3321; Camptothecins form a powerful class of chemotherapy drugs (e.g. irinotecan, topotecan, belotecan), based on their ability to inhibit topoisomerase I. Some camptothecins, such as DXd and SN-38, have also proven powerful payloads for antibody-drug conjugates (ADCs), as exemplified by the recent market approval of Enhertu® and Trodelvy®, respectively...Homogeneous and stable GlycoConnect™ADCs were generated from trastuzumab and SYNtecan E™ and compared head-to-head with DXd or SN-38payload, as well as deruxtecan, the linker-payload applied in Enhertu®...Taken together, these studies demonstrate the potential of SYNtecan E™ for application in stable and site-specific ADCs with excellent therapeutic index.1 van Geel et al. Chemoenzymatic Conjugation of Toxic Payloads to the Globally Conserved N-Glycan of NativemAbs Provides Homogeneous and Highly Efficacious Antibody−Drug Conjugates.
- |||||||||| tamoxifen / Generic mfg., paclitaxel / Generic mfg., irinotecan / Generic mfg.
Review, Journal: Systemic therapy for limited stage small cell lung carcinoma. (Pubmed Central) - Nov 21, 2020 Maintenance therapy following induction with chemotherapy, vandetanib and interferon-alpha have also been attempted...In this review, we discuss the various systemic therapy options in limited stage small cell lung carcinoma, from the historical regimens to the modern-day therapy and promising areas of research. We also discuss the role of growth factors, the optimal number of chemotherapy cycles, the use of prognostic and predictive factors, the optimal timing of chemotherapy and the treatment of special populations of patients including older patients, and patients with comorbidities.
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Biomarker, Review, Journal: Irinotecan: 25 years of cancer treatment. (Pubmed Central) - Jul 2, 2020 This review highlights recent discoveries in the field of IRT and its derivatives, including analogues of the active metabolite SN38 (such as FL118), the recently approved liposomal form Nal-IRI and SN38-based immuno-conjugates currently in development (such as sacituzumab govitecan)...It offers a large range of drug combinations with cytotoxic agents, targeted products and immuno-active biotherapeutics, to treat a variety of advanced solid carcinoma, sarcoma and cancers with progressive central nervous system diseases. A quarter of century after its first launch, IRT remains an essential anticancer drug, largely prescribed, useful to many patients and scientifically inspiring.
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Preclinical, Journal: Development of an enzyme‑linked immunosorbent assay for camptothecin. (Pubmed Central) - Dec 20, 2019 The cross‑reactivity results suggested that the assay developed in the present study possessed a high sensitivity to camptothecin. Therefore, this immunoassay technique may be suitable for monitoring the levels of camptothecin in compound analysis, clinical applications, and analyses of food and environmental samples.
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