Results 71 to 80 of about 5,118 (209)

Identification and characterization of mechanism of action of P61-E7, a novel phosphine catalysis-based inhibitor of geranylgeranyltransferase-I.

open access: yesPLoS ONE, 2011
Small molecule inhibitors of protein geranylgeranyltransferase-I (GGTase-I) provide a promising type of anticancer drugs. Here, we first report the identification of a novel tetrahydropyridine scaffold compound, P61-E7, and define effects of this ...
Lai N Chan   +4 more
doaj   +1 more source

A somatic multiple myeloma mutation unravels a mechanism of oligomerization‐mediated product inhibition in GGPPS

open access: yesThe FEBS Journal, Volume 292, Issue 21, Page 5802-5817, November 2025.
Geranylgeranyl diphosphate synthase (GGPPS) plays a key role in multiple myeloma biology. Using crystallography, mass spectrometry, and fluorescence spectroscopy, this study shows that a somatic multiple myeloma cell line mutation destabilizes inter‐dimer interactions, resulting in increased GGPPS activity by facilitating product releas.
Ruba Yehia   +7 more
wiley   +1 more source

Simvastatin‐Mediated Molecular Mechanisms Underlying the Growth Inhibition of Testicular Leydig Tumour Cells

open access: yesJournal of Cellular and Molecular Medicine, Volume 29, Issue 16, August 2025.
ABSTRACT Leydig cell tumours (LCTs) are uncommon stromal neoplasms of the testis, accounting for less than 3% of all gonadal cancers. Most of them are benign, but the malignant ones are very aggressive without specific effective treatment. Several studies reported pharmacologic insight into the use of statins as anti‐tumour agents, but their efficacy ...
Arianna De Luca   +7 more
wiley   +1 more source

Development of an image-based screening system for inhibitors of the plastidial MEP pathway and of protein geranylgeranylation [v1; ref status: indexed, http://f1000r.es/4vt]

open access: yesF1000Research, 2015
We have recently established an in vivo visualization system for the geranylgeranylation of proteins in a stably transformed tobacco BY-2 cell line, which involves expressing a dexamethasone-inducible GFP fused to the prenylable, carboxy-terminal basic ...
Michael Hartmann   +4 more
doaj   +1 more source

Zebrafish-based small molecule screens for novel cardiovascular drugs [PDF]

open access: yes, 2013
The zebrafish is increasingly being adopted as an in vivo model of high throughput drug screening. In this brief review we outline the advantages and disadvantages of this approach and summarize recent screens that have attempted to identify novel small ...
Chico, T.J.A.   +2 more
core   +1 more source

Dysregulated Cholesterol Metabolism and Its Impact on the Tumour Immune Response in Colorectal Cancer

open access: yesJournal of Cellular and Molecular Medicine, Volume 29, Issue 15, August 2025.
ABSTRACT Colorectal cancer (CRC) ranks among the primary causes of cancer deaths worldwide. Cholesterol metabolism, tightly regulated through biosynthesis, uptake, efflux and conversion, plays a crucial role in CRC development and progression. Dysregulated cholesterol metabolism in cancer cells alters the tumour microenvironment (TME), promoting tumour
Chunyu Zhang   +4 more
wiley   +1 more source

Development of an image-based screening system for inhibitors of the plastidial MEP pathway and of protein geranylgeranylation [v2; ref status: indexed, http://f1000r.es/5p9]

open access: yesF1000Research, 2015
In a preceding study we have recently established an in vivo visualization system for the geranylgeranylation of proteins in a stably transformed tobacco BY-2 cell line, which involves expressing a dexamethasone-inducible GFP fused to the prenylable ...
Michael Hartmann   +4 more
doaj   +1 more source

Targeting inflammation to reduce cardiovascular disease risk: a realistic clinical prospect? [PDF]

open access: yes, 2017
Data from basic science experiments is overwhelmingly supportive of the causal role of immune-inflammatory response(s) at the core of atherosclerosis, and therefore the theoretical potential to manipulate the inflammatory response to prevent ...
Abbas   +173 more
core   +2 more sources

Two avian Plasmodium species trigger different transcriptional responses on their vector Culex pipiens

open access: yesMolecular Ecology, Volume 34, Issue 15, August 2025.
Abstract Malaria is a mosquito‐borne disease caused by protozoans of the genus Plasmodium that affects both humans and wildlife. The fitness consequences of infections by avian malaria are well known in birds, however, little information exists on its impact on mosquitoes.
Marta Garrigós   +4 more
wiley   +1 more source

Obesity Affects IVF Outcomes and Mevalonic Acid Rescues the Side Effects of Statins on Follicle Growth

open access: yesThe FASEB Journal, Volume 39, Issue 13, 15 July 2025.
Obesity reduces in vitro fertilization pregnancy success, with significant decreases in the number of retrieved oocytes, mature oocytes, and cleavage embryos. Mevalonic acid rescues potential productive toxicity of the lipid‐lowering drug simvastatin in follicular development.
Fei Mao   +8 more
wiley   +1 more source

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