Results 71 to 80 of about 68,974 (263)

Cryptolepine, a Plant Alkaloid, Inhibits the Growth of Non-Melanoma Skin Cancer Cells through Inhibition of Topoisomerase and Induction of DNA Damage

open access: yesMolecules, 2016
Topoisomerases have been shown to have roles in cancer progression. Here, we have examined the effect of cryptolepine, a plant alkaloid, on the growth of human non-melanoma skin cancer cells (NMSCC) and underlying mechanism of action.
Harish C. Pal, Santosh K. Katiyar
doaj   +1 more source

Integrated Clinical and Proteomic Profiling of CD19 Chimeric Antigen Receptor T Cell Therapy in Progressive Systemic Sclerosis

open access: yesArthritis &Rheumatology, EarlyView.
Objective To characterize the clinical, immunologic, and proteomic changes associated with CD19 chimeric antigen receptor T cell therapy in patients with progressive systemic sclerosis (SSc). Methods Patients with progressive SSc received CD19 chimeric antigen receptor (CAR)‐T cell therapy and were observed longitudinally for safety, clinical efficacy,
Chenhan Jia   +16 more
wiley   +1 more source

Evolutionary twist on topoisomerases: Conversion of gyrase to topoisomerase IV [PDF]

open access: yesProceedings of the National Academy of Sciences, 2010
Type II topoisomerases are essential enzymes found in all cells, where they maintain the topology of DNA in a well-defined state (1). The defining activity of type II topoisomerases is an ATP-dependent passage of a segment of dsDNA through a transient double-stranded break in a second segment of dsDNA (Fig. 1) (1, 2).
openaire   +2 more sources

Expert Perspectives: Defining and Managing Progressive Pulmonary Fibrosis in Systemic Sclerosis

open access: yesArthritis &Rheumatology, EarlyView.
Systemic sclerosis–associated interstitial lung disease (SSc‐ILD) is one of the leading causes of morbidity and mortality in SSc, affecting up to three‐quarters of patients. The disease course is highly heterogeneous, ranging from indolent, nonprogressive forms to rapidly progressive pulmonary fibrosis (PPF).
Devis Benfaremo   +7 more
wiley   +1 more source

QSAR Modeling on Benzo[<em>c</em>]phenanthridine Analogues as Topoisomerase I Inhibitors and Anti-cancer Agents

open access: yesMolecules, 2012
Benzo[<em>c</em>]phenanthridine (BCP) derivatives were identified as topoisomerase I (TOP-I) targeting agents with pronounced antitumor activity.
Thi-Ngoc-Phuong Huynh   +3 more
doaj   +1 more source

Effect of developmental changes on pharmacokinetics of drugs used in the treatment of infant acute lymphoblastic leukaemia—A comprehensive review

open access: yesBritish Journal of Clinical Pharmacology, EarlyView.
While the event‐free survival (EFS) of children treated for acute lymphoblastic leukaemia (ALL) has improved greatly in the last decades, the EFS for patients diagnosed with ALL before the age of one is still under 50%. This outcome further decreases when infants have a rearrangement in the gene encoding histone‐lysine N‐methyltransferase 2A (KMT2A ...
Tirsa de Kluis   +5 more
wiley   +1 more source

Discovery of New DNA Topoisomerase II Inhibitors using Structure Based Virtual Screening Method

open access: yesJournal of the Turkish Chemical Society, Section A: Chemistry, 2019
DNA topoisomerases are proved therapeutic targets of anticancer and antibacterial drugs. Structures of topoisomerase–DNA and inhibitor ternary complexes have revealed the exact binding sites and mechanisms of topoisomerase poisons. There are two isoforms
Tugba Ertan-Bolelli, Kayhan Bolelli
doaj   +1 more source

UGT1A1 genotype testing for irinotecan: A guideline developed by the UK Centre of Excellence in Regulatory Science and Innovation in Pharmacogenomics (CERSI‐PGx)

open access: yesBritish Journal of Clinical Pharmacology, EarlyView.
Abstract Irinotecan, a topoisomerase I inhibitor, is available as both non‐pegylated and pegylated formulations. The non‐pegylated formulation is licensed for use in advanced colorectal cancer either in combination with other agents or as monotherapy.
Dharmisha Chauhan   +24 more
wiley   +1 more source

Organelle‐Resolved Tetrazine‐trans‐Cyclooctene Click Chemistry for Cargo Delivery and Release

open access: yesChemistry – A European Journal, EarlyView.
Bioorthogonal click chemistry tools provide a means for specific intracellular conjugation of molecules. In this study, we used reactive tetrazine (Tz) and TCO moieties for labeling of organelles and organelle‐specific delivery and activation of doxorubicin prodrugs.
Oleh Durydivka   +6 more
wiley   +1 more source

Extracellularly Activatable Conjugates of RGD Peptidomimetics and Cryptophycin for αVβ3‐Targeted Cancer Therapy

open access: yesChemistry – A European Journal, EarlyView.
Integrin αVβ3‐targeting small‐molecule drug conjugates (SMDCs) were synthesized by conjugating a cryptophycin payload through a neutrophil elastase‐cleavable NPV‐PABC linker. RGD peptidomimetic and linker epimers served as controls for targeting and enzymatic cleavage, and the resulting conjugates displayed subnanomolar cytotoxicity in vitro.
Dominic Seißenschmidt   +3 more
wiley   +1 more source

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