Compounds that specifically inhibit STEROL 14-DEMETHYLASE. A variety of azole-derived ANTIFUNGAL AGENTS act through this mechanism.
An NADPH-dependent P450 enzyme that plays an essential role in the sterol biosynthetic pathway by catalyzing the demethylation of 14-methyl sterols such as lanosterol. The enzyme acts via the repeated hydroxylation of the 14-methyl group, resulting in its stepwise conversion into an alcohol, an aldehyde and then a carboxylate, which is removed as formic acid. Sterol 14-demethylase is an unusual cytochrome P450 enzyme in that it is found in a broad variety of organisms including ANIMALS; PLANTS; FUNGI; and protozoa.
A triterpene that derives from the chair-boat-chair-boat folding of 2,3-oxidosqualene. It is metabolized to CHOLESTEROL and CUCURBITACINS.
Enzymes that catalyse the removal of methyl groups from LYSINE or ARGININE residues found on HISTONES. Many histone demethylases generally function through an oxidoreductive mechanism.
A family of histone demethylases that share a conserved Jumonji C domain. The enzymes function via an iron-dependent dioxygenase mechanism that couples the conversion of 2-oxoglutarate to succinate to the hydroxylation of N-methyl groups.
Oxidoreductases, N-Demethylating are enzymes that catalyze the oxidation of N-methyl groups to carbonyl groups, typically found in xenobiotic metabolism, involving the removal of methyl groups from various substrates using molecular oxygen.

Tumor necrosis factor alpha increases P-glycoprotein expression in a BME-UV in vitro model of mammary epithelial cells. (1/31)

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Comparison of the inhibitory profiles of itraconazole and cimetidine in cytochrome P450 3A4 genetic variants. (2/31)

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Brain P450 epoxygenase activity is required for the antinociceptive effects of improgan, a nonopioid analgesic. (3/31)

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In vivo investigation in pigs of intestinal absorption, hepatobiliary disposition, and metabolism of the 5alpha-reductase inhibitor finasteride and the effects of coadministered ketoconazole. (4/31)

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Effects of strong CYP2D6 and 3A4 inhibitors, paroxetine and ketoconazole, on the pharmacokinetics and cardiovascular safety of tamsulosin. (5/31)

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Overexpression of CYP3A4, but not of CYP2D6, promotes hypoxic response and cell growth of Hep3B cells. (6/31)

Cytochrome P450s (P450s) contribute to carcinogenesis by activating procarcinogens and also metabolize anti-cancer drugs. The activity and protein levels of P450s are important in cancer risk and in cancer therapy. In this study, we found that overexpression of CYP3A4 induced growth of a human hepatoma cell line, Hep3B. Overexpression of CYP2D6, by comparison, decreased cell growth. An inhibitor of CYP3A4, ketoconazole, significantly suppressed the growth of Hep3B cells overexpressing CYP3A4, but an inhibitor of CYP2D6, quinidine, did not restore Hep3B cell growth to baseline levels. Overexpression of CYP3A4 increased the production of reactive oxygen species, but this was not the cause of the CYP3A4-induced growth. Previously, we showed that CYP3A4 can produce epoxyeicosatrienoic acids (EETs) from arachidonic acid. The CYP3A4-enhanced cell growth was attenuated by a putative EET receptor antagonist, 14,15-EEZE. CYP3A4 promoted progression of the cell cycle from the G1 to the S phase. CYP3A4 also induced a hypoxic response of Hep3B cells, detected as enhanced erythropoietin gene expression (a typical hypoxic response). The cell growth promoted by CYP3A4 was inhibited by PI3K inhibitor LY294002. These results suggest that CYP3A4 plays an important role in tumor progression, independent of the activation of carcinogens and metabolism of anti-cancer drugs.  (+info)

Substrate preferences and catalytic parameters determined by structural characteristics of sterol 14alpha-demethylase (CYP51) from Leishmania infantum. (7/31)

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Effectiveness of chronic treatment with ketoconazole in a patient with diabetic Cushing's disease resistant to surgery. (8/31)

Without treatment, Cushing's disease has significant morbidity and mortality. Where a surgical approach may not be feasible, or is refused by the patient, medical therapy becomes the only option. In this case report, we discuss the effects of two years of ketoconazole treatment on diabetes regulation and insulin resistance in a patient reluctant to agree to surgery. A 62 year-old female patient with uncontrolled type 2 diabetes mellitus was investigated. Cushing's disease was confirmed by the results of high urine free cortisol level and dexamethasone suppression tests. We discuss the effects of two years of 600 mg/day ketoconazole treatment on diabetes regulation and insulin resistance in a patient with Cushing's disease reluctant to agree to surgery. This case report illustrates the beneficial long-term effects of 24 months of ketoconazole treatment on the clinical and laboratory findings and also on steroid and glucose metabolism.  (+info)

14-alpha Demethylase Inhibitors are a class of antifungal medications that work by inhibiting the enzyme 14-alpha demethylase, which is essential for the synthesis of ergosterol, a critical component of fungal cell membranes. By inhibiting this enzyme, the drugs disrupt the structure and function of the fungal cell membrane, leading to fungal cell death.

Examples of 14-alpha Demethylase Inhibitors include:

* Fluconazole (Diflucan)
* Itraconazole (Sporanox)
* Ketoconazole (Nizoral)
* Posaconazole (Noxafil)
* Voriconazole (Vfend)

These medications are used to treat a variety of fungal infections, including candidiasis, aspergillosis, and cryptococcosis. However, they can also have significant drug-drug interactions and toxicities, so their use must be monitored closely by healthcare professionals.

Sterol 14-demethylase is an enzyme that plays a crucial role in the biosynthesis of sterols, particularly ergosterol in fungi and cholesterol in animals. This enzyme is classified as a cytochrome P450 (CYP) enzyme and is located in the endoplasmic reticulum.

The function of sterol 14-demethylase is to remove methyl groups from the sterol molecule at the 14th position, which is a necessary step in the biosynthesis of ergosterol or cholesterol. Inhibition of this enzyme can disrupt the normal functioning of cell membranes and lead to various physiological changes, including impaired growth and development.

Sterol 14-demethylase inhibitors (SDIs) are a class of antifungal drugs that target this enzyme and are used to treat fungal infections. Examples of SDIs include fluconazole, itraconazole, and ketoconazole. These drugs work by binding to the heme group of the enzyme and inhibiting its activity, leading to the accumulation of toxic sterol intermediates and disruption of fungal cell membranes.

Lanosterol is a steroid that is an intermediate in the biosynthetic pathway of cholesterol in animals and other eukaryotic organisms. It's a complex organic molecule with a structure based on four fused hydrocarbon rings, and it plays a crucial role in maintaining the integrity and function of cell membranes.

In the biosynthetic pathway, lanosterol is produced from squalene through a series of enzymatic reactions. Lanosterol then undergoes several additional steps, including the removal of three methyl groups and the reduction of two double bonds, to form cholesterol.

Abnormal levels or structure of lanosterol have been implicated in certain genetic disorders, such as lamellar ichthyosis type 3 and congenital hemidysplasia with ichthyosiform erythroderma and limb defects (CHILD) syndrome.

Histone demethylases are enzymes that remove methyl groups from histone proteins, which are the structural components around which DNA is wound in chromosomes. These enzymes play a crucial role in regulating gene expression by modifying the chromatin structure and influencing the accessibility of DNA to transcription factors and other regulatory proteins.

Histones can be methylated at various residues, including lysine and arginine residues, and different histone demethylases specifically target these modified residues. Histone demethylases are classified into two main categories based on their mechanisms of action:

1. Lysine-specific demethylases (LSDs): These enzymes belong to the flavin adenine dinucleotide (FAD)-dependent amine oxidase family and specifically remove methyl groups from lysine residues. They target mono- and di-methylated lysines but cannot act on tri-methylated lysines.
2. Jumonji C (JmjC) domain-containing histone demethylases: These enzymes utilize Fe(II) and α-ketoglutarate as cofactors to hydroxylate methyl groups on lysine residues, leading to their removal. JmjC domain-containing histone demethylases can target all three states of lysine methylation (mono-, di-, and tri-methylated).

Dysregulation of histone demethylases has been implicated in various human diseases, including cancer, neurological disorders, and cardiovascular diseases. Therefore, understanding the functions and regulation of these enzymes is essential for developing novel therapeutic strategies to target these conditions.

Jumonji domain-containing histone demethylases (JHDMs) are a family of enzymes that are responsible for removing methyl groups from specific residues on histone proteins. These enzymes play crucial roles in the regulation of gene expression by modifying the chromatin structure and influencing the accessibility of transcription factors to DNA.

JHDMs contain a conserved Jumonji C (JmjC) domain, which is responsible for their demethylase activity. They are classified into two main groups based on the type of methyl group they remove: lysine-specific demethylases (KDMs) and arginine-specific demethylases (RDMs).

KDMs can be further divided into several subfamilies, including KDM2/7, KDM3, KDM4, KDM5, and KDM6, based on their substrate specificity and the number of methyl groups they remove. For example, KDM4 enzymes specifically demethylate di- and tri-methylated lysine 9 and lysine 36 residues on histone H3, while KDM5 enzymes target mono-, di-, and tri-methylated lysine 4 residues on histone H3.

RDMs, on the other hand, are responsible for demethylating arginine residues on histones, including symmetrically or asymmetrically dimethylated arginine 2, 8, 17, and 26 residues on histone H3 and H4.

Dysregulation of JHDMs has been implicated in various human diseases, including cancer, neurological disorders, and cardiovascular diseases. Therefore, understanding the functions and regulation of JHDMs is essential for developing novel therapeutic strategies to treat these diseases.

Oxidoreductases are a class of enzymes that catalyze oxidation-reduction reactions, where a electron is transferred from one molecule to another. N-Demethylating oxidoreductases are a specific subclass of these enzymes that catalyze the removal of a methyl group (-CH3) from a nitrogen atom (-N) in a molecule, which is typically a xenobiotic compound (a foreign chemical substance found within an living organism). This process often involves the transfer of electrons and the formation of water as a byproduct.

The reaction catalyzed by N-demethylating oxidoreductases can be represented as follows:
R-N-CH3 + O2 + H2O → R-N-H + CH3OH + H2O2

where R represents the rest of the molecule. The removal of the methyl group is often an important step in the metabolism and detoxification of xenobiotic compounds, as it can make them more water soluble and facilitate their excretion from the body.

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 ...
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 ...
What inhibits 14 alpha demethylase?. August 29, 2022. By Michael Simons Life ... What inhibits 14 alpha demethylase?. Imidazoles inhibit the enzyme lanosterol-14-α-demethylase, a cytochrome P-450-dependent ... As a member of this family, lanosterol 14α-demethylase is responsible for an essential step in the biosynthesis of sterols. In ... Compounds that specifically inhibit STEROL 14-DEMETHYLASE. A variety of azole-derived ANTIFUNGAL AGENTS act through this ...
Matched Categories: … ACE Inhibitors and Diuretics ... zofenopril and diuretics ... Amino Acids, Peptides, and Proteins … ... A selective, irreversible inhibitor of Type B monoamine oxidase. It is used in newly diagnosed patients with Parkinsons ... Capmatinib is a small molecule kinase inhibitor targeted against c-Met (a.k.a. hepatocyte growth factor receptor [HGFR]), a ... Duvelisib, also known as IPI-145 and INK-1197, is a small-molecule inhibitor of phosphoinositide-3 kinases that was designed ...
15-Hydroxy-11 alpha,9 alpha-(epoxymethano)prosta-5,13-dienoic Acid. 15-Hydroxy-11 alpha,9 alpha-(epoxymethano)prosta-5,13- ... 1,4-alpha-Glucan Branching Enzyme. 1,4-alpha-Glucan Branching Enzyme (Structural Class). NDF-RT (Drug Classification). Drug ... 14-3-3 Proteins. 14-3-3 Proteins (Structural Class). NDF-RT (Drug Classification). Drug Classes (NDF-RT). Details. ... 14-alpha demethylase Inhibitors (Mechanism of Action). NDF-RT (Drug Classification). Drug Classes (NDF-RT). Details. ...
Inhibitor of fungal cytochrome P450 enzyme 14alpha-demethylase Show data source InterBioScreen - Bio-0041 ... It is highly selective inhibitor of fungal cytochrome P-450 sterol C-14 α-demethyllation. Fluconazole is a potent inhibitor of ... It is highly selective inhibitor of fungal cytochrome P-450 sterol C-14 α-demethyllation. Fluconazole is a potent inhibitor of ... A highly selective inhibitor of fungal cytochrome P-450 sterol C-14 α-demethylation.. ...
... alpha-demethylase]] inhibitors) , list1 = {{Navbox subgroup , groupstyle = background:PowderBlue; , group1 = [[Imidazole]]s , ... Thymidylate synthase inhibitor]]s , list1 = [[Flucytosine]],sup>#,/sup> , group2 = [[Mitotic inhibitor]]s , list2 = [[ ... inhibitors , list1 = {{Navbox subgroup , groupstyle = background-color: PowderBlue , group1 = [[Azole]]s,BR>([[Lanosterol 14 ... inhibitors) , list3 = topical: ([[Amorolfine]] * [[Butenafine]] * [[Naftifine]] * [[Terbinafine]]),BR>systemic: ([[Terbinafine ...
5-alpha Reductase Inhibitors. *5-Lipoxygenase-Activating Protein Inhibitors. *Adenosine Deaminase Inhibitors ... "Histone Deacetylase Inhibitors" is a descriptor in the National Library of Medicines controlled vocabulary thesaurus, MeSH ( ... Quatramer™ mediated co-delivery of PI3-Kd/HDAC6 dual inhibitor augments the anti-cancer efficacy of Epirubicin in breast cancer ... Histone deacetylase inhibitors enhance oncolytic herpes simplex virus therapy for malignant meningioma. Biomed Pharmacother. ...
Novel and stereoselective synthesis of 1 alpha hydroxylated vitamin d metabolites stereocontrolled synthesis of 24r 1 alpha 24 ... Adams, S.P.; Towler, D.A.; Gordon, J.I. 1988: Novel inhibitor peptides i us patent 4778878. october 18 1988. Official Gazette ... Linzen, B (Ed ) Invertebrate Oxygen Carriers; International Conference, Tutzing, West Germany, July 29-August 1, 1985 Xiv+521p ... A.Q.wasmeh M.; Bennett, B.; Check, I.J. 1985: Novel alpha 1 antitrypsin isoforms may account for low functional activity in ...
Lefort S, Thuleau A, Kieffer Y, Sirven P, Bieche I, Marangoni E, Vincent-Salomon A, Mechta-Grigoriou F (2017) CXCR4 inhibitors ... Corpas-Lopez V, Morillas-Marquez F, Navarro-Moll MC, Merino-Espinosa G, Diaz-Saez V, Martin-Sanchez J (2015) (-)-alpha- ... Gogoi B, Chowdhury P, Goswami N, Gogoi N, Naiya T, Chetia P (2021) Identification of potential plant based inhibitor against ... Karlgren M, Vildhede A, Norinder U, Wisniewski JR, Kimoto E, Lai Y, Haglund U, Artursson P (2012) Classification of inhibitors ...
D27.505.696.399.450.855.100 5-alpha Reductase Inhibitors D27.505.519.389.74 D27.505.519.389.870.200 D27.505.696.399.450.855.200 ... A8.713.49.500 Aromatase Inhibitors D27.505.519.389.99 D27.505.519.389.870.300 D27.505.696.399.450.327.149 D27.505.696.399. ... A8.675.100 Adrenergic Uptake Inhibitors D27.505.519.562.437.50 Adsorption G2.149.47 G1.595.37 Adult Children I1.880.225.281 ... A8.186.211.730.885.287.500.345.600 GABA Uptake Inhibitors D27.505.519.562.437.535 GABAergic Neurons A8.663.289 A8.675.289 ...
D27.505.696.399.450.855.100 5-alpha Reductase Inhibitors D27.505.519.389.74 D27.505.519.389.870.200 D27.505.696.399.450.855.200 ... A8.713.49.500 Aromatase Inhibitors D27.505.519.389.99 D27.505.519.389.870.300 D27.505.696.399.450.327.149 D27.505.696.399. ... A8.675.100 Adrenergic Uptake Inhibitors D27.505.519.562.437.50 Adsorption G2.149.47 G1.595.37 Adult Children I1.880.225.281 ... A8.186.211.730.885.287.500.345.600 GABA Uptake Inhibitors D27.505.519.562.437.535 GABAergic Neurons A8.663.289 A8.675.289 ...
D27.505.696.399.450.855.100 5-alpha Reductase Inhibitors D27.505.519.389.74 D27.505.519.389.870.200 D27.505.696.399.450.855.200 ... A8.713.49.500 Aromatase Inhibitors D27.505.519.389.99 D27.505.519.389.870.300 D27.505.696.399.450.327.149 D27.505.696.399. ... A8.675.100 Adrenergic Uptake Inhibitors D27.505.519.562.437.50 Adsorption G2.149.47 G1.595.37 Adult Children I1.880.225.281 ... A8.186.211.730.885.287.500.345.600 GABA Uptake Inhibitors D27.505.519.562.437.535 GABAergic Neurons A8.663.289 A8.675.289 ...
D27.505.696.399.450.855.100 5-alpha Reductase Inhibitors D27.505.519.389.74 D27.505.519.389.870.200 D27.505.696.399.450.855.200 ... A8.713.49.500 Aromatase Inhibitors D27.505.519.389.99 D27.505.519.389.870.300 D27.505.696.399.450.327.149 D27.505.696.399. ... A8.675.100 Adrenergic Uptake Inhibitors D27.505.519.562.437.50 Adsorption G2.149.47 G1.595.37 Adult Children I1.880.225.281 ... A8.186.211.730.885.287.500.345.600 GABA Uptake Inhibitors D27.505.519.562.437.535 GABAergic Neurons A8.663.289 A8.675.289 ...
D27.505.696.399.450.855.100 5-alpha Reductase Inhibitors D27.505.519.389.74 D27.505.519.389.870.200 D27.505.696.399.450.855.200 ... A8.713.49.500 Aromatase Inhibitors D27.505.519.389.99 D27.505.519.389.870.300 D27.505.696.399.450.327.149 D27.505.696.399. ... A8.675.100 Adrenergic Uptake Inhibitors D27.505.519.562.437.50 Adsorption G2.149.47 G1.595.37 Adult Children I1.880.225.281 ... A8.186.211.730.885.287.500.345.600 GABA Uptake Inhibitors D27.505.519.562.437.535 GABAergic Neurons A8.663.289 A8.675.289 ...
D27.505.696.399.450.855.100 5-alpha Reductase Inhibitors D27.505.519.389.74 D27.505.519.389.870.200 D27.505.696.399.450.855.200 ... A8.713.49.500 Aromatase Inhibitors D27.505.519.389.99 D27.505.519.389.870.300 D27.505.696.399.450.327.149 D27.505.696.399. ... A8.675.100 Adrenergic Uptake Inhibitors D27.505.519.562.437.50 Adsorption G2.149.47 G1.595.37 Adult Children I1.880.225.281 ... A8.186.211.730.885.287.500.345.600 GABA Uptake Inhibitors D27.505.519.562.437.535 GABAergic Neurons A8.663.289 A8.675.289 ...
D27.505.696.399.450.855.100 5-alpha Reductase Inhibitors D27.505.519.389.74 D27.505.519.389.870.200 D27.505.696.399.450.855.200 ... A8.713.49.500 Aromatase Inhibitors D27.505.519.389.99 D27.505.519.389.870.300 D27.505.696.399.450.327.149 D27.505.696.399. ... A8.675.100 Adrenergic Uptake Inhibitors D27.505.519.562.437.50 Adsorption G2.149.47 G1.595.37 Adult Children I1.880.225.281 ... A8.186.211.730.885.287.500.345.600 GABA Uptake Inhibitors D27.505.519.562.437.535 GABAergic Neurons A8.663.289 A8.675.289 ...
Caspase 9 Inhibitor manufacturer supplementary table S3, Supplementary CBP/p300 Inhibitor drug Material online). Within the ... inside the coding area of eburicol 14-alpha demethylase CB0940_11379, otherwise generally known as the gene encoding DMI ...
V.G. Kiptily, P. Beaumont, …, M. Curuia, …, S. Soare, et al., 2014, Fusion alpha-particle diagnostics for DT experiments on the ... Andreea Calianu, Radu Tamaian, Computational Design of New Teixobactin Analogues as Inhibitors of Lipid II Flippase MurJ, 2022 ... editia a XIV-a 2019, ISSN 2066-6586, pp. 28-34, 2019, Bucuresti, Romania ... Escaping alpha-particle monitor for burning plasmas, Nuclear Fusion, Volume 58, Issue 8, Article number 082009 DOI: 10.1088/ ...
Heterologous expression of mutated eburicol 14alpha-demethylase (CYP51) proteins of Mycosphaerella graminicola to assess ... The clinical candidate VT-1161 is a highly potent inhibitor of Candida albicans CYP51 but fails to bind the human enzyme. ... High resolution powder diffraction data from standard reference materials of Si, alpha-quartz, and LaB6 are used to ... encoding the azole target sterol 14alpha-demethylase. In this study, we have expressed wild-type and mutated M. graminicola ...
17-alpha-hydroxy-progesterone caproate [Chemical/Ingredient] * 2-Aminopurine [Chemical/Ingredient] * 4-Hydroxycoumarins [ ...
Fluconazole (Diflucan) is a strong inhibitor of 2C19 and a moderate inhibitor of 3A4 and 2C9. The enzyme inhibiting effect ... Effect of inhibitor depletion on inhibitory potency: tight binding inhibition of CYP3A by clotrimazole. Drug Metab Disp. 1999; ... Clotrimazole is an inhibitor of hepatic cytochrome P450 (CYP) 3A4, and tacrolimus is metabolized by CYP3A4.90,91 Administration ... Highly selective inhibitor of fungal cytochrome P450 sterol C-14 alpha-demethylase, which results in fungistatic activity ...
Warren, J.B.; Dollery, C.T.; Sciberras, D.; Goldberg, M.R. 1991: Assessment of MK-467, a peripheral alpha 2-adrenergic receptor ... Assessment of renin dependency of hypertension with a dipeptide renin inhibitor. Circulation 81(6): 1768-1774 ... Tuck, S.F.; Robinson, C.H.; Silverton, J.V. 1991: Assessment of the active site requirements of lanosterol 14 alpha demethylase ... site requirements of 5 aminolaevulinic acid dehydratase evaluation of substrate and product analogues as competitive inhibitors ...
... but luliconazole is thought to inhibit the enzyme lanosterol demethylase. Lanosterol demethylase is needed for the synthesis of ... Inhibitor. General Function. Vitamin d3 25-hydroxylase activity. Specific Function. Cytochromes P450 are a group of heme- ... InChI=1S/C14H9Cl2N3S2/c15-9-1-2-10(11(16)5-9)13-7-20-14(21-13)12(6-17)19-4-3-18-8-19/h1-5,8,13H,7H2/b14-12+/t13-/m0/s1 ... It transforms lanosterol into 4,4-dimethyl cholesta-8,14,24-triene-3-beta-ol.. Gene Name. ERG11. Uniprot ID. P10613. Uniprot ...
Characterization of the sterol 14alpha-demethylases of Fusarium graminearum identifies a novel genus-specific CYP51 function. A ... Changes in field dose-response curves for demethylation inhibitor (DMI) and quinone outside inhibitor (QoI) fungicides against ... Alterations in the predicted regulatory and coding regions of the sterol 14alpha-demethylase gene (CYP51) confer decreased ... Alterations in the predicted regulatory and coding regions of the sterol 14alpha-demethylase gene (CYP51) confer decreased ...
Targeting the CoREST complex with dual histone deacetylase and demethylase inhibitors. Nature Communications 9(1):53 ... Abbas SH, Pickett E, Lomas DA, Thorburn D, Gooptu B, Hurst JR, Marshall A. Non-invasive testing for liver pathology in alpha-1 ... Structural insights into inhibitor regulation of the DNA repair protein DNA-PKcs Nature. DOI:101038/s41586-021-04274-9. ... In Vitro Assessment of Putative PD-1/PD-L1 Inhibitors: Suggestions of an Alternative Mode of Action. ACS Med Chem Lett. 10(8): ...
This graph shows the total number of publications written about "Cytochrome P-450 CYP2B6 Inhibitors" by people in this website ... "Cytochrome P-450 CYP2B6 Inhibitors" is a descriptor in the National Library of Medicines controlled vocabulary thesaurus, MeSH ... Below are the most recent publications written about "Cytochrome P-450 CYP2B6 Inhibitors" by people in Profiles. ... Below are MeSH descriptors whose meaning is more general than "Cytochrome P-450 CYP2B6 Inhibitors". ...
Understanding alpha-globin gene regulation and implications for the treatment of beta-thalassemia. Ann N Y Acad Sci. 2016; 1368 ... histone methyltransferase inhibitor, chaetocin and lysine-specific histone demethylase 1 inhibitor, tranylcypromine (Figure 2B ... The histone demethylase inhibitor, IOX1, exerts the desired changes in erythroid cells and has potential as a lead compound to ... However, previous reports on IOX1 demonstrate that it acts as a broad range inhibitor of histone demethylase enzymes.1412 ...
INHIBITORS, ANTITUMOR ... fungal growth by acting on the heme group of lanosterol 14 ... alpha-demethylase enzyme (CYP51), thus blocking the biosynthesis of ergosterol. Citations Web of Science: 3 ...
  • Although the lanosterol 14α-demethylase is present in a wide variety of organisms, the enzyme is studied primarily in the context of fungi, where it plays an essential role in mediating membrane permeability. (wikipedia.org)
  • Other names in common use include obtusufoliol 14-demethylase, lanosterol 14-demethylase, lanosterol 14alpha-demethylase, and sterol 14alpha-demethylase. (wikipedia.org)
  • Imidazoles inhibit the enzyme lanosterol-14-α-demethylase, a cytochrome P-450-dependent enzyme that converts lanosterol to ergosterol. (davidgessner.com)
  • What reaction does lanosterol 14 alpha demethylase catalyze? (davidgessner.com)
  • As a member of this family, lanosterol 14α-demethylase is responsible for an essential step in the biosynthesis of sterols. (davidgessner.com)
  • Which class of antifungal drugs work by inhibiting lanosterol 14 alpha demethylase? (davidgessner.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)
  • It inhibits the fungal lanosterol 14 alpha-demethylase which thereby prevents the formation of ergosterol which is an essential component in the fungal cell membrane. (chembase.cn)
  • They suppress fungal growth by acting on the heme group of lanosterol 14 alpha-demethylase enzyme (CYP51), thus blocking the biosynthesis of ergosterol. (anadolu.edu.tr)
  • It blocks ergosterol synthesis by inhibiting the enzyme lanosterol 14-alpha-demethylase and sterol precursor accumulation. (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)
  • Histone Deacetylase Inhibitors" is a descriptor in the National Library of Medicine's controlled vocabulary thesaurus, MeSH (Medical Subject Headings) . (harvard.edu)
  • This graph shows the total number of publications written about "Histone Deacetylase Inhibitors" by people in Harvard Catalyst Profiles by year, and whether "Histone Deacetylase Inhibitors" was a major or minor topic of these publication. (harvard.edu)
  • Below are the most recent publications written about "Histone Deacetylase Inhibitors" by people in Profiles. (harvard.edu)
  • Nitrilase mediated mild hydrolysis of a carbon-14 nitrile for the radiosynthesis of 4-(7-hydroxycarbamoyl-[1-14 C-heptanoyl]-oxy)-benzoic acid methyl ester, [14 C]-SHP-141: A novel class I/II histone deacetylase (HDAC) inhibitor. (harvard.edu)
  • The impact of histone deacetylase inhibitors on immune cells and implications for cancer therapy. (harvard.edu)
  • Histone deacetylase inhibitors enhance oncolytic herpes simplex virus therapy for malignant meningioma. (harvard.edu)
  • 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)
  • 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)
  • 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)
  • A variety of azole-derived ANTIFUNGAL AGENTS act through this mechanism….14-alpha Demethylase Inhibitors. (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)
  • One class of drugs that explores this killing mechanism are the inhibitors of poly(ADP-ribose) polymerase (PARP) enzyme, an important DDR component. (encyclopedia.pub)
  • Because ergosterol constitutes a fundamental component of fungal membranes, many antifungal medications have been developed to inhibit 14α-demethylase activity and prevent the production of this key compound. (wikipedia.org)
  • 14α-Demethylase converts lanosterol to ergosterol in fungi (Figure 18-33). (davidgessner.com)
  • Lanosterol demethylase is needed for the synthesis of ergosterol, which is a major component of the fungus cell membranes. (drugbank.com)
  • Fluconazole oral is a synthetic oral antifungal (broad-spectrum bistriazole) that selectively inhibits fungal CYP450 and sterol C-14 alpha-demethylation, which prevents conversion of lanosterol to ergosterol, thereby disrupting cellular membranes. (medscape.com)
  • It is a triazole antifungal agent that inhibits fungal CYP450-mediated 14 alpha-lanosterol demethylation, which is essential in fungal ergosterol biosynthesis. (medscape.com)
  • A highly selective inhibitor of fungal cytochrome P-450 sterol C-14 α-demethylation. (chembase.cn)
  • The effectiveness of imidazoles and triazoles (common azole subclasses) as inhibitors of 14α-demethylase have been confirmed through several experiments. (wikipedia.org)
  • BRCAness as PARP Inhibitors" Encyclopedia , https://encyclopedia.pub/entry/13660 (accessed December 11, 2023). (encyclopedia.pub)
  • In enzymology, a sterol 14-demethylase (EC 1.14.13.70) is an enzyme of the Cytochrome P450 (CYP) superfamily. (wikipedia.org)
  • Ketorolac (Ketorolac tromethamine) is a non-selective COX inhibitor of COX-1 and COX-2 with IC50 of 1.23 μM and 3.50 μM, respectively. (absource.de)
  • Amprenavir is a potent PXR-selective agonist, and an HIV protease inhibitor, used to treat HIV. (absource.de)
  • The systematic name of this enzyme class is sterol,NADPH:oxygen oxidoreductase (14-methyl cleaving). (wikipedia.org)
  • PARP inhibitors (PARPis) can induce synthetic lethality in cancer cells with preexistent defects in the homologous recombination (HR) repair pathway, such as deleterious mutations of the breast cancer 1 (BRCA1) and breast cancer 2 (BRCA2) suppressor genes [ 7 ] [ 8 ] . (encyclopedia.pub)
  • The commonness of ERα positive luminal breast cancer together with the effectiveness and widespread use of ERα pathway inhibitors in treatment predicts that this biology will remain the major focus of research and drug development. (nature.com)
  • We highlight one of the most plausible associations on every single chromosome determined by mutational impact and gene annotation.Considerably Related Markers on ChromosomeThere have been two key genomic regions drastically related with tetraconazole sensitivity on chromosome 9: 13325481358331 and 1403629497163 bp ( Caspase 9 Inhibitor manufacturer supplementary table S3, Supplementary CBP/p300 Inhibitor drug Material online). (idhinhibitor.com)
  • The latter area notably contained a synonymous mutation (9_1451478) inside the coding area of eburicol 14-alpha demethylase CB0940_11379, otherwise generally known as the gene encoding DMI fungicide target CbCYP51. (idhinhibitor.com)
  • Alpha-ketoglutarate-dependent dioxygenase (ALKBH) is a DNA repair gene involved in the repair of alkylating DNA damage. (frontiersin.org)
  • Capmatinib is a small molecule kinase inhibitor targeted against c-Met (a.k.a. hepatocyte growth factor receptor [HGFR]), a receptor tyrosine kinase that, in healthy humans, activates signaling cascades involved in organ regeneration and tissue repair. (drugbank.com)
  • Design, synthesis, and anti-inflammatory activity characterization of novel brain-permeable HDAC6 inhibitors. (harvard.edu)
  • Ketoprofen is a dual COX1/2 inhibitor, used as a nonsteroidal anti-inflammatory drug to treat arthritis-related inflammatory pains. (absource.de)
  • Ibuprofen (Dolgesic) is an anti-inflammatory inhibitor targeting COX-1 and COX-2 with IC50 of 13 μM and 370 μM, respectively. (absource.de)
  • Currently, multiple LSD1 inhibitors are undergoing clinical trials and demonstrate considerable potential in the field of cancer treatment [ 12 ]. (biomedcentral.com)
  • Effectiveness of triennial screening with clinical breast examination: 14-years follow-up outcomes of randomized clinical trial in Trivandrum, India. (who.int)
  • Quatramer™ mediated co-delivery of PI3-Kd/HDAC6 dual inhibitor augments the anti-cancer efficacy of Epirubicin in breast cancer. (harvard.edu)
  • Fourteen novel mutations wereidentified. (pdftreatment.com)
  • Collectively, these alterations that mimic BRCA mutations are known as 'BRCAness' [ 14 ] . (encyclopedia.pub)
  • 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)
  • Besides, numerous published studies consistently demonstrate that epigenetic alterations have a significant impact on the reprogramming of the TME [ 14 ]. (biomedcentral.com)
  • This review examines how LSD1 modulates different cell behavior in TME and emphasizes the potential use of LSD1 inhibitors in combination with ICB therapy for future cancer research studies. (biomedcentral.com)
  • Sorafenib (Sor) is the only approved multikinase inhibitor indicated for the treatment of HCC. (biomedcentral.com)
  • 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)
  • iASPP oncoprotein is a key inhibitor of p53 conserved from worm to human. (nature.com)
  • Orlistat is a general lipase inhibitor with IC50 of 122 ng/ml for PL from human duodenal juice. (absource.de)
  • 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)
  • Comparing one dose of HPV vaccine in girls aged 9-14 years in Tanzania (DoRIS) with one dose of HPV vaccine in historical cohorts: an immunobridging analysis of a randomised controlled trial. (who.int)
  • Allopurinol is a purine analog inhibitor of the enzyme xanthine oxidase, used to treat gout or kidney stones, and to decrease levels of uric acid. (absource.de)
  • Below are the most recent publications written about "Cytochrome P-450 CYP2B6 Inhibitors" by people in Profiles. (uchicago.edu)
  • Recently, increased incidence of the pathogen on diverse crop species has been reported worldwide [ 12 - 14 ], highlighting the importance of this disease to crop production in drought prone regions. (biomedcentral.com)