The effectiveness of imidazoles and triazoles (common azole subclasses) as inhibitors of 14α-demethylase have been confirmed ... lanosterol 14alpha-demethylase, and sterol 14alpha-demethylase. This enzyme participates in biosynthesis of steroids. These are ... Lepesheva GI, Waterman MR (March 2007). "Sterol 14alpha-demethylase cytochrome P450 (CYP51), a P450 in all biological kingdoms ... "Amino acid substitutions in the cytochrome P-450 lanosterol 14alpha-demethylase (CYP51A1) from azole-resistant Candida albicans ...

... (INN, codenamed RS-21607) is an anti-obesity drug acting as a lanosterol 14α-demethylase inhibitor. "International ... July 1993). "Selective inhibition of mammalian lanosterol 14 alpha-demethylase: a possible strategy for cholesterol lowering". ... August 1995). "Azalanstat (RS-21607), a lanosterol 14 alpha-demethylase inhibitor with cholesterol-lowering activity". ... Lanosterol 14α-demethylase inhibitors, Thioethers, All stub articles, Gastrointestinal system drug stubs). ...

November 2007). "Small-molecule scaffolds for CYP51 inhibitors identified by high-throughput screening and defined by X-ray ... Lepesheva GI, Waterman MR (March 2007). "Sterol 14alpha-demethylase cytochrome P450 (CYP51), a P450 in all biological kingdoms ... "Substrate preferences and catalytic parameters determined by structural characteristics of sterol 14alpha-demethylase (CYP51) ... Aoyama Y, Yoshida Y (August 1991). "Different substrate specificities of lanosterol 14a-demethylase (P-45014DM) of ...

... azole fungicides which are demethylase inhibitors that inhibit lanosterol 14 alpha-demethylase (CYP51) activity. The last ... The fungicides that have been shown to be effective include quinone outside inhibitors (QoIs), which, like most fungicides, are ... Asci measure 11-14 × 30-40 μm. Ascospores are hyaline, elliptical, and 2.5-4 × 9-16 μm, with two cells of unequal length. ...

... is pharmacologically distinct from other azole antifungal agents in that it is the only inhibitor in this class ... Absorption of itraconazole is impaired when taken with an antacid, H2 blocker or proton pump inhibitor.[citation needed] ... CYP3A4 inhibitors, Dioxolanes, Johnson & Johnson brands, Janssen Pharmaceutica, Lanosterol 14α-demethylase inhibitors, Orphan ... These distinct activities are unrelated to inhibition of the cytochrome P450 lanosterol 14 alpha-demethylase and the exact ...

For example, the azole antifungals such as ketoconazole or itraconazole can be both substrates and inhibitors of the P- ... Azole antifungals also are both substrates and inhibitors of the cytochrome P450 family CYP3A4, causing increased concentration ... Orotomide (F901318) - pyrimidine synthesis inhibitor Piroctone olamine Pentanenitrile Potassium iodide - preferred treatment ... Inhibitors and Inducers". FDA. American Academy of Dermatology (February 2013). "Five Things Physicians and Patients Should ...

... inhibitors. Inhibitors that compete against the substrate were also developed, such as peptidyl-based inhibitors that target ... Walport LJ, Hopkinson RJ, Schofield CJ (December 2012). "Mechanisms of human histone and nucleic acid demethylases". Curr. Opin ... Alpha-ketoglutarate-dependent hydroxylases are a major class of non-heme iron proteins that catalyse a wide range of reactions ... Poppe L, Tegley CM, Li V, Lewis J, Zondlo J, Yang E, Kurzeja RJ, Syed R (November 2009). "Different modes of inhibitor binding ...

7α-Hydroxylase inhibitors, 11β-Hydroxylase inhibitors, 21-Hydroxylase inhibitors, Acetamides, Aldosterone synthase inhibitors, ... Cholesterol side-chain cleavage enzyme inhibitors, CYP2D6 inhibitors, CYP3A4 inhibitors, CYP17A1 inhibitors, Dioxolanes, ... Oral ketoconazole has been used clinically as a steroidogenesis inhibitor in men, women, and children at dosages of 200 to ... Ketoconazole shampoo in conjunction with an oral 5α-reductase inhibitor such as finasteride or dutasteride has been used off ...

... a lysine-specific demethylase-1 inhibitor drug used to treat Ewing's Sarcoma. GRCh38: Ensembl release 89: ENSG00000273238 - ... The AlphaFold Database predicts that there are four alpha helices in the human TMEM271 protein. TMEM271 mRNA is found to be ... AlphaFold predictive modeling shows four alpha helices located from residues 5 to 37, 45 to 71, 117 to 151, and 199 to 257. ... Retrieved 2022-12-14. "TMEM114 protein expression summary - The Human Protein Atlas". www.proteinatlas.org. Retrieved 2023-02- ...

AASS: encoding enzyme Alpha-aminoadipic semialdehyde synthase, mitochondrial ACTR3B: actin-related protein 3B AEBP1: AE binding ... inhibitor of growth protein 3 INTS1: encoding protein Integrator complex subunit 1 IQCE: IQ domain-containing protein E KDM7A: ... encoding protein Lysine demethylase 7A LCHN: protein encoded by the KIAA1147 gene LHFPL3: LHFPL tetraspan subfamily member 3 ... MyoD family inhibitor domain containing METTL2B: methyltransferase-like protein 2B MINDY4: MINDY lysine 48 deubiquitinase 4 ...

... ribonuclease inhibitor 1 RNU2-2: encoding protein RNA, U2 small nuclear 2 ROM1: retinal outer segment membrane protein 1 RPL27A ... lysine demethylase 2A KIAA1549L encoding protein KIAA1549-like KRTAP5-6: encoding protein Keratin associated protein 5-6 LPXN: ... Srp receptor alpha subunit Suppression of tumorigenicity 2: encoding protein Suppression of tumorigenicity 2 TAF1D: TATA box ... encoding protein Apoptosis inhibitor 5 APLNR: Apelin receptor (APJ receptor) APOA4: apolipoprotein A-IV ARCN1 encoding protein ...

"Inhibitors of sterol synthesis. Metabolism of 5 alpha-cholest-8(14)-en-3 beta-ol-15-one after intravenous administration to ... A steroidogenesis inhibitor, also known as a steroid biosynthesis inhibitor, is a type of drug which inhibits one or more of ... 7-DHCR inhibitors produce an acquired form of SLOS in animals, and as such, like 24-DHCR inhibitors (see below), are probably ... Steroidogenic enzyme Neurosteroidogenesis inhibitor Vanden Bossche H (1992). "Inhibitors of P450-dependent steroid biosynthesis ...

Lysine-specific demethylase 5B also known as histone demethylase JARID1B is a demethylase enzyme that in humans is encoded by ... JARID1B belongs to the alpha-ketoglutarate-dependent hydroxylase superfamily. Jarid1B (also known as KDM5B or PLU1) is in the ... 4-pyridine-dicarboxylic acid as an in vitro and in cell inhibitor". The FEBS Journal. 279 (11): 1905-14. doi:10.1111/j.1742- ... Zou MR, Cao J, Liu Z, Huh SJ, Polyak K, Yan Q (June 2014). "Histone demethylase jumonji AT-rich interactive domain 1B (JARID1B ...

Ezh1/2 inhibitors also activate cellular antiviral pathways. Specifically, in cells treated with Ezh1/2 inhibitors, greater ... Polycomb complex recruitment by LAT, VP16 recruits OCT1 and HCF1, which in turn recruit histone demethylases JMJD2s and LSD1, ... along with upregulation of interferon-alpha (IFN-α) and interleukin-8 (IL-8). These pathways are not specific to HSV; treatment ... The Ezh1/2 inhibitors GSK126, GSK343, and UNC1999 as well as astemizole, which interferes with Ezh1/2 association in PRC, were ...

In a double-blind study by Slavin in 1992, terconazole showed a 75% mycological cure over a short-term period (7-14 days) and ... This occurs by transforming lanosterol into 4,4'-dimethyl cholesta-8,14,24-triene-3-β-ol. This stops respiration by prohibiting ... Within a normal yeast cell, lanosterol is demethylated using 14α-demethylation. This process creates zymosterol: a major ... "Selective inhibition of 14 alpha-desmethyl sterol synthesis in Candida albicans by terconazole, a new triazole antimycotic". ...

The alpha and beta subunit are similar in structure and both contain the following domains: N-terminus - a bHLH domain for DNA ... March 2019). "Histone demethylase KDM6A directly senses oxygen to control chromatin and cell fate". Science. 363 (6432): 1217- ... Maxwell PH, Eckardt KU (March 2016). "HIF prolyl hydroxylase inhibitors for the treatment of renal anaemia and beyond". Nature ... The alpha subunits of HIF are hydroxylated at conserved proline residues by HIF prolyl-hydroxylases, allowing their recognition ...

Aromatase inhibitors, Fungicides, Lanosterol 14α-demethylase inhibitors, Triazoles). ... or demethylation inhibiting fungicide due to its binding with and inhibiting the 14-alpha demethylase enzyme from demethylating ...

DNA methyltransferase inhibitors, and histone demethylase inhibitors. The majority of epigenetic drugs tested for use against ... Vorinostat In an alpha-synuclein overexpressing Drosophila model of PD, vorinostat (as well as sodium butyrate) reduced alpha- ... "Sirtuin 2 inhibitors rescue alpha-synuclein-mediated toxicity in models of Parkinson's disease". primary. Science. 317 (5837): ... Currently, no HDAC inhibitors are in use for the mitigation of symptoms in MS patients however, some are in pre-clinical trials ...

The mechanism of action of meldonium is to act as a fatty acid oxidation inhibitor, presumably by inhibiting enzymes in the ... Meldonium has also been found to induce anticonvulsant and antihypnotic effects involving alpha 2-adrenergic receptors, as well ... akin to the action of histone demethylases), dimethylamine, and (1-methylimidazolidin-4-yl)acetic acid, "an unexpected product ... Meldonium is a relatively weak inhibitor to carnitine acetyltransferase (when compared to γ-butyrobetaine hydroxylase), with an ...

HDAC inhibitors can induce p21 (WAF1) expression, a regulator of p53's tumor suppressoractivity. HDACs are involved in the ... Benevolenskaya EV (August 2007). "Histone H3K4 demethylases are essential in development and differentiation". Biochemistry and ... factor implicated in the tumorigenesis and progression of breast cancer via its binding to the estrogen receptor alpha (ERα). ... HDAC inhibitors. Current front-runner candidates for new drug targets are Histone Lysine Methyltransferases (KMT) and Protein ...

It is a reversible inhibitor of eukaryotic nuclear DNA replication that blocks progression past the S phase. Its mechanism is ... Research into the mechanism has hinted at it potentially preventing tubulin from forming its alpha/beta heterodimer. Taxol ... The suspected mechanism is dependent on p27Kip1, a cyclin-dependent kinase inhibitor. p27Kip1 protein levels are elevated in ... Liao H, Thorner J (April 1980). "Yeast mating pheromone alpha factor inhibits adenylate cyclase". Proceedings of the National ...

... of histone H3 methylation that facilitates oestrogen receptor-alpha target gene activation by regulating lysine demethylase 1 ... Recent studies described an inhibitor (D2) that block PELP1 interactions with AR. Since PELP1 interacts with histone ... ERR-alpha, PR, GR, AR, and RXR. PELP1 also functions as a coregulator of several other transcription factors, including AP1, ... lysine-specific demethylase 1 (KDM1), PRMT6, and CARM1. PELP1 also interacts with cell cycle regulators such as pRb. E2F1, and ...

In cancer, 2-hydroxyglutarate serves as a competitive inhibitor for a number of enzymes that facilitate reactions via alpha- ... There are also changes on the genetic and epigenetic level through the function of histone lysine demethylases (KDMs) and ten- ... Their carbon skeletons (i.e. the de-aminated amino acids) may either enter the citric acid cycle as intermediates (e.g. alpha- ... To turn them into amino acids the alpha keto-acids formed from the citric acid cycle intermediates have to acquire their amino ...

DNMT1 inhibitors in animals have been shown to increase the expression of both reelin and GAD67, and both DNMT inhibitors and ... as demethylases open up the RELN gene. The activation of dendrite growth by reelin is apparently conducted through Src family ... a site distinct from the region of reelin shown to associate with VLDLR/ApoER2 binds to the alpha-3-beta-1 integrin receptor. ... Methylation inhibitors and histone deacetylase inhibitors, such as valproic acid, increase reelin mRNA levels, while L- ...

27-Hydroxylase inhibitors, CYP3A4 inhibitors, Fluoroarenes, Lanosterol 14α-demethylase inhibitors, Merck & Co. brands, Orphan ... It does this by blocking the synthesis of ergosterol by inhibiting of the enzyme lanosterol 14α-demethylase and accumulation of ... Posaconazole is significantly more potent at inhibiting 14-alpha demethylase than itraconazole. Posaconazole is active against ...

"Pan-Histone Demethylase Inhibitors Simultaneously Targeting Jumonji C and Lysine-Specific Demethylases Display High Anticancer ... l-alpha-aminoadipoyl)-l-cysteinyl-d-alpha-aminobutyrate". Biochemical Journal. 372 (3): 687-693. doi:10.1042/bj20021627. ISSN ... "A selective jumonji H3K27 demethylase inhibitor modulates the proinflammatory macrophage response". Nature. 488 (7411): 404-408 ... The histone demethylases are of interest both with respect to their links to diseases, including cancer and inflammatory ...

This acquisition gave Gilead first-in-class small molecule inhibitors of histone demethylases involved in regulating gene ... Ioannis Stamatopoulos (February 12, 2017). "Pharma M&A In 2017: The Most Likely Deal Hunters". Seeking Alpha. Retrieved March ... for $400 million, giving Gilead control of the compound NDI-010976 (an ACC inhibitor) and other preclinical ACC inhibitors for ... The acquisition brings drug candidate CYT387, an orally-administered, once-daily, selective inhibitor of the Janus kinase (JAK ...

Nuclear factor (NF)-κB inhibitor ε (NFKBIE) directly inhibits NF-κB1 activity and is significantly co-expressed with NF-κB1, ... This includes for instance alpha-ketoglutarate, which is required for histone demethylation, and acetyl-Coenzyme A, which is ... Histones H3 and H4 can also be manipulated through demethylation using histone lysine demethylase (KDM). This recently ... "The histone methyltransferase inhibitor BIX01294 enhances the cardiac potential of bone marrow cells". Stem Cells and ...

Menéndez-Arias L, Álvarez M, Pacheco B (October 2014). "Nucleoside/nucleotide analog inhibitors of hepatitis B virus polymerase ... and cooperating with histone methylases and demethylases to change cell expression patterns. HBx is partly responsible for the ... "Solution structure of stem-loop alpha of the hepatitis B virus post-transcriptional regulatory element". Nucleic Acids Research ... "A mutant hepatitis B virus core protein mimics inhibitors of icosahedral capsid self-assembly". Biochemistry. 48 (8): 1736-42. ...

October 2015). "Pur-alpha functionally interacts with FUS carrying ALS-associated mutations". Cell Death & Disease. 6 (10): ... Tsai WC, Reineke LC, Jain A, Jung SY, Lloyd RE (November 2017). "Histone arginine demethylase JMJD6 is linked to stress granule ... September 2013). "Ribonuclease/angiogenin inhibitor 1 regulates stress-induced subcellular localization of angiogenin to ... April 2016). "Pur-alpha regulates cytoplasmic stress granule dynamics and ameliorates FUS toxicity". Acta Neuropathologica. 131 ...