The topical azoles inhibit the enzyme lanosterol 14-alpha-demethylase, a cytochrome P-450-dependent enzyme that converts lanosterol to ergosterol. (medscape.com)
The antifungal azoles target fungal ergosterol biosynthesis by inhibiting the fungal CYP450-dependent enzyme lanosterol 14-α-demethylase, which blocks the conversion of lanosterol to ergosterol and leads to accumulation of aberrant sterol compounds and depletion of ergosterol in the fungal cell membrane. (davidgessner.com)
Azole antifungals work by inhibiting the cytochrome P450 dependent enzyme lanosterol 14-alpha-demethylase, which converts lanosterol to ergosterol, the main sterol in the fungal cell membrane. (davidgessner.com)
The exact mechanism of action for luliconazole's anti-fungal activity is still not known, but luliconazole is thought to inhibit the enzyme lanosterol demethylase. (drugbank.com)
Ketoconazole inhibit the C-14 Alpha-demethylase enzyme leading to blockage of demethylation of lanosterol to ergosterol a part of fungal membrane. (medparhlo.com)
Specifically, difenoconazole inhibits the enzyme 14-alpha-demethylase, which is responsible for the conversion of lanosterol to ergosterol. (agriplexindia.com)
Fungi have a cytochrome p450 enzyme called fourteen-alpha-demethylase in their mitochondria and endoplasmic reticulums, which converts lanosterol to ergosterol. (osmosis.org)
Fungal5
It inhibits the enzyme 14-alpha-demethylase, preventing fungal cell wall formation. (medscape.com)
The mechanism of action for this antifungal activity is through the decrease of ergosterol synthesis, required for membrane integrity of fungal cells, via inhibition of the lanosterol 14 alpha-demethylase (14DM) catalyst. (ecancer.org)
This inhibition prevents the production of ergosterol, which leads to the disruption of the fungal cell membrane and the death of the fungus. (agriplexindia.com)
Bifonazole works by inhibiting the production of a substance called ergosterol, which is an essential component of fungal cell membranes.It acts to destabilize the fungal cyctochrome p450 51 enzyme (also known as Lanosterol 14-alpha demethylase). (lgmpharma.com)
The membrane also becomes fragile, which eventually leads to inhibition of fungal growth . (osmosis.org)
Histone demethylase3
This identified IOX1, a pan-histone demethylase inhibitor, which selectively downregulates α-globin expression without perturbing erythroid differentiation or general gene expression, more specifically β-like globin expression. (haematologica.org)
The histone demethylase JMJD2B is critical for p53-mediated autophagy and survival in Nutlin-treated cancer cells. (rush.edu)
This is the initial discovery of a histone demethylase responsible for eliminating mono- and dimethyl modifications from histones 3 lysine 4 (H3K4), histone 3 lysine 9 (H3K9), and histone 4 lysine 20 (H4K20). (biomedcentral.com)
Ergosterol2
Ergosterol biosynthesis inhibition by the thiocarbamate antifungal agents tolnaftate and tolciclate. (davidgessner.com)
Lanosterol demethylase is needed for the synthesis of ergosterol, which is a major component of the fungus cell membranes. (drugbank.com)
Azalanstat (INN, codenamed RS-21607) is an anti-obesity drug acting as a lanosterol 14α-demethylase inhibitor. (wikipedia.org)
Duvelisib, also known as IPI-145 and INK-1197, is a small-molecule inhibitor of phosphoinositide-3 kinases that was designed initially to prove that simultaneous inhibition of the isoforms delta and gamma can produce a broad adaptative and innate immune cell inhibitory activity. (drugbank.com)
Through this constitutive activity, NF-κB p50/p65 acts in tumors mainly as an inhibitor of apoptosis [ 8 , 14 ]. (oncotarget.com)
Inhibitors of Jumonji C domain-containing histone lysine demethylases overcome cisplatin and paclitaxel resistance in non-small cell lung cancer through APC/Cdh1-dependent degradation of CtIP and PAF15. (rush.edu)
Succinate further inhibits several dioxygenases involved in epigenetic regulation like ten-eleven translocation methylcytosine dioxygenase (TET) and jumonji C domain-containing histone lysine demethylases (JMJD3). (haematologica.org)
Antifungal activity is via inhibition of 1,3-beta-glucan synthase production of BETA-GLUCANS. (lookformedical.com)
Lysine2
Lysine-specific demethylase 1 (LSD1) is a protein that modifies histone and non-histone proteins and is known to influence a wide variety of physiological processes. (biomedcentral.com)
Network analysis confirmed p53 and NF-κB transcription factor-regulated gene clusters in irradiated and bystander cells and suggested novel regulators, such as KDM5B/JARID1B (lysine (K)-specific demethylase 5B) and HDACs (histone deacetylases), which could epigenetically coordinate gene expression after irradiation. (biomedcentral.com)
Membrane1
this inhibition disrupt the membrane structure and function. (medparhlo.com)
Synthesis3
A fungistatic azole with broad spectrum of activity because of its inhibition of enzyme 14-alpha-demethylase, which is needed by the fungus for cell wall synthesis. (medscape.com)
This reaction is the committed step of cholesterol synthesis and is regulated by feedback inhibition by cholesterol and its derivatives. (biochemden.com)
This aminoglycoside cause protein synthesis inhibition by 'irreversibly' bind to specific 30S-subunit proteins and 16S rRNA. (medicineindia.org)
Epigenetic1
Besides, numerous published studies consistently demonstrate that epigenetic alterations have a significant impact on the reprogramming of the TME [ 14 ]. (biomedcentral.com)
Protein4
In particular, this protein catalyzes the removal of the C-14α-methyl group from lanosterol. (davidgessner.com)
For example, bone morphogenetic protein receptor type 2 ( BMPR2 ) mutations are observed in 60-80% of familial (FPAH) cases, but data from population registries indicate that penetrance of the disease phenotype ranges from 14 to 42% [ 6 ]. (biomedcentral.com)
This approach was based on the assumption that the deregulation of a protein was causally linked to a disease state, and the pharmacological intervention through inhibition of the deregulated target was able to restore normal cell function. (biomedcentral.com)
Yak was used as the experimental object to clone the yak CCAAT/Enhancer binding protein alpha( CEBPα ) gene, predicted its protein structure and function, isolated yak adipocyte, and detected the expression of CEBPα in different tissues of yak and yak fat expression during cell induction and differentiation. (hbnxb.net)
Breast Cancer1
Fatty acid oxidation and autophagy promote endoxifen resistance and counter the effect of AKT inhibition in ER-positive breast cancer cells. (rush.edu)
Dioxygenase1
Alpha-ketoglutarate-dependent dioxygenase (ALKBH) is a DNA repair gene involved in the repair of alkylating DNA damage. (frontiersin.org)
Activity1
Examples include CYP5A1, thromboxane A 2 synthase, abbreviated to TBXAS1 ( T hrom B o X ane A 2 S ynthase 1 ), and CYP51, lanosterol 14-α-demethylase, sometimes unofficially abbreviated to LDM according to its substrate ( L anosterol) and activity ( D e M ethylation). (wikidoc.org)
This inhibition of AMPK ultimately leads to inhibition of mTOR and thus induces apoptosis in the HepG2 cells. (biomedcentral.com)
Drugs1
14. A drugs decrease the migration of granulocytes into the effected area Also Block cell division by binding to mitotic spindles? (medparhlo.com)
Responsible1
As a member of this family, lanosterol 14α-demethylase is responsible for an essential step in the biosynthesis of sterols. (davidgessner.com)
Cell1
Alpha ketoglutarate levels, regulated by p53 and OGDH, determine autophagy and cell fate/apoptosis in response to Nutlin-3a. (rush.edu)
Patients1
For pediatric patients aged 12 to 14 years weighing greater than or equal to 50 kg and those aged 15 years and older regardless of body weight use adult dosage. (nih.gov)
Human1
Description: This product includes all the assay kit components for 100 assays in 384-well plate assay format: 400 µl of 10 x Buffer, 33 µl of 100 x DNA template, 33 µl of 100 x dNTP mix, 30 µl of 100 x human DNA polymerase alpha (4 µM), 1550 µl of 2 x Dye, 1550 µl of 50 mM EDTA. (bioinfolab.org)