Results 141 to 150 of about 32,790 (255)

A solid phase assay for topoisomerase I interfacial poisons and catalytic inhibitors

open access: yes, 2012
We report a mechanism-based screening technique to rapidly identify eukaryotic topoisomerase I targeting agents. The method is based on genetic tagging of topoisomerase I to immobilize the enzyme on a solid surface in a microtiter well format.

core   +1 more source

Cell‐Specific Expression and Cellular Compartmental Regulation in Camptothecin Biosynthesis

open access: yesPlant Biotechnology Journal, EarlyView.
ABSTRACT Plant secondary metabolites such as monoterpenoid indole alkaloids (MIAs) show tightly regulated biosynthesis and accumulation in specific organelles of distinct cell types. However, the cell‐specific expression patterns of anticancer MIA camptothecin biosynthetic genes in Ophiorrhiza pumila and the regulatory mechanisms of camptothecin ...
Xiaolong Hao   +12 more
wiley   +1 more source

A Solid Phase Assay For Topoisomerase I Interfacial Poisons And Catalytic Inhibitors

open access: yes, 2011
We report a mechanism based screening technique to rapidly identify eukaryotic topoisomerase I targeting agents. The method is based on genetic tagging of topoisomerase I to immobilize the enzyme on a solid surface in a microtiter well format.
Cyril, Vidusha
core  

RAD51 and RAD51 paralog inhibition sensitizes nonreplicating quiescent keratinocytes to UV radiation

open access: yesPhotochemistry and Photobiology, EarlyView.
UV radiation and other compounds generate DNA adducts that block transcription and induce cell death if not removed by the nucleotide excision repair system. In this work, we used a small‐scale pharmacological screen to discover that inhibition of the recombinase RAD51 sensitized nonreplicating quiescent keratinocytes to both UVR and other agents that ...
Saman Khan   +3 more
wiley   +1 more source

Study on molecular modelling of some topoisomerase I inhibitors

open access: yes, 2010
Pharmacophore analysis of a series of benzoxazine derivetives having eucaryotic topoisomerase I inhibitory activity were performed via HypoGen and HipHop methods.At the pharmacophore analysis using HypoGen method 38 compounds were studied.
Ataei, Sanaz
core  

Antibiotic‐mediated immune modulation in periodontitis

open access: yesPeriodontology 2000, EarlyView.
Abstract Periodontitis is a chronic inflammatory disease affecting the supporting structures of the teeth. Although initiated by dysbiotic microbial communities, its progression is largely driven by the host's uncontrolled inflammatory response. While antibiotics have conventionally been employed in periodontitis therapy for their antimicrobial ...
Lina J. Suárez   +6 more
wiley   +1 more source

BRCAness, SLFN11, and RB1 loss predict response to topoisomerase I inhibitors in triple-negative breast cancers. [PDF]

open access: yesSci Transl Med, 2020
Coussy F   +33 more
europepmc   +1 more source

The role of extracellular vesicles in cell–cell crosstalk in cardiotoxicity

open access: yesThe Journal of Physiology, EarlyView.
Abstract figure legend Administration of a pharmacological agent can result in off‐target cardiotoxicity which can be driven by cell–cell crosstalk between healthy and dysfunctional cardiac cells. Extracellular vesicles (EVs) are lipid bilayer structures that can move biological cargo between cells, facilitating cell–cell crosstalk.
Gabriella Bachynskyj‐Bilas   +5 more
wiley   +1 more source

Pharmacophore based discovery of dual inhibitors targeting TOP1 and TOP2A in resistant triple negative breast cancer

open access: yesDiscover Chemistry
Triple-negative breast cancer (TNBC) is an aggressive malignancy characterized by the absence of conventional hormonal receptors, leading to intrinsic resistance to standard therapies and poor clinical outcomes.
Enayi Onaji   +6 more
doaj   +1 more source

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