Results 131 to 140 of about 6,711,495 (336)

Inhibition of cyclin‐dependent kinases 12/13 using CT7439 as a treatment for colorectal cancer with CDK12 upregulation

open access: yesMolecular Oncology, EarlyView.
The proposed mechanism of action for the CDK12/13 inhibitor and cyclin K degrader, CT7439. CDK12/13 inhibition interrupts transcription elongation, leading to increased DNA damage that results in cell death. This agent is a potentially novel treatment option for patients with colorectal cancer. Created in BioRender. Cyclin‐dependent kinase (CDK) 12 and
Wylie K. Watlington   +10 more
wiley   +1 more source

In vitro and in silico modelling of ROS1‐positive non‐small cell lung cancer reveals fusion‐dependent tyrosine kinase inhibitor responses

open access: yesMolecular Oncology, EarlyView.
Drug resistance limits treatment success in a subset of lung cancers driven by ROS1 gene alterations. Using patient‐derived cells and computer simulations, we studied three key mutations and how they affect five targeted drugs. The mutations reduced drug effectiveness in different ways by altering protein structure and behavior.
Farhan Ul Haq   +8 more
wiley   +1 more source

Cancer‐associated mutations in endometriosis reframe a benign disease through molecular oncology

open access: yesMolecular Oncology, EarlyView.
This review aims to comprehensively analyse cancer‐associated somatic mutations (CAMs) present in endometriotic lesions, emphasizing their biological roles, spatial distribution and implications for translational applications in medicine. By contextualizing a benign state within a genomic framework, this analysis seeks to establish its value as a ...
Clarissa Mujacic   +15 more
wiley   +1 more source

Bioactivity and enzyme inhibition properties of Stevia rebaudiana

open access: yes, 2016
Objective: The main study was to evaluate the anti- inflammatory, anti-oxidant, and the gastro-protective properties of extracts of Stevia rebaudiana. In addition the purpose of the study was to investigate new, natural inhibition of urease and xanthine ...
Can, Zehra   +3 more
core   +1 more source

Pharmacological chromatin remodeling enhances response to estrogen therapy in ER+ breast cancer

open access: yesMolecular Oncology, EarlyView.
Estrogen therapy elicits clinical benefit in ~ 30% of patients with endocrine‐resistant estrogen receptor (ER)‐positive breast cancer. Based on findings that ER transcriptional activation underlies response to estrogen therapy, we tested the effects of epigenetic dysregulation via pharmacological inhibition of histone deacetylases (HDACi).
Anneka L. Johnson Thomas   +16 more
wiley   +1 more source

Human serum paraoxonase-1 (hPON1): In vitro inhibition effects of moxifloxacin hydrochloride, levofloxacin hemihidrate, cefepime hydrochloride, cefotaxime sodium and ceftizoxime sodium

open access: yes, 2015
In this study, we investigated the effects of antibacterial drugs (moxifloxacin hydrochloride, levofloxacin hemihidrate, cefepime hydrochloride, cefotaxime sodium and ceftizoxime sodium) on human serum paraoxonase-1 (hPON1) enzyme activity from human ...
Söyüt H., Türkeş C., Beydemir Ş.
core   +1 more source

DDIapp—A Web‐Based Application for Static Drug–Drug Interaction Assessment

open access: yesCPT: Pharmacometrics & Systems Pharmacology
In this work we describe the development of a web‐based application for static drug–drug interaction (DDI) risk assessment in accordance with the International Council for Harmonization (ICH) M12 guidance.
Hirotaka Watase   +5 more
doaj   +1 more source

Bioluminescent Enzyme Inhibition Based Assay of Metal Nanoparticles [PDF]

open access: yesЖурнал Сибирского федерального университета: Серия Биология, 2017
The bioluminescent enzymatic bioassays for assessment of nanomaterial biotoxicity using the soluble or immobilized coupled enzyme system of luminous bacteria NAD(P)Н:FMN-oxidoreductase + luciferase (Red + Luc) as a test system were employed in this study.
Yana V. Fritsler   +2 more
doaj  

PANoptosis in the pathogenesis of myelodysplastic syndromes

open access: yesMolecular Oncology, EarlyView.
PANoptosis, a combination of three types of programmed cell death, is mediated by a large protein complex called a PANoptosome. In healthy bone marrow hematopoietic cells, PANoptosis is restricted by inhibitory signaling. In MDS, bone marrow cells become sensitive to the PANoptotic stimuli due to the aberrant inactivation of inhibitory signaling or ...
Rohit Thalla   +4 more
wiley   +1 more source

BeckResearchLab/USP-inhibition: USP-inhibition|05.30.17

open access: yes, 2017
<p>This release contains a working implementation of QSAR for enzyme inhibition prediction and drug lead generation.</p ...
dacb   +3 more
core   +1 more source

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