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

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

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

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

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

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

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)

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

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

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)

*  Lanosterol 14 alpha-demethylase
"Mutations in the CYP51 Gene Correlated with Changes in Sensitivity to Sterol 14Alpha-Demethylation Inhibitors in Field Isolates ... "Substrate Preferences and Catalytic Parameters Determined by Structural Characteristics of Sterol 14alpha-demethylase (CYP51) ... "Amino Acid Substitutions in the Cytochrome P-450 Lanosterol 14Alpha-Demethylase (CYP51A1) from Azole-resistant Candida albicans ... The effectiveness of imidazoles and triazoles (common azole subclasses) as inhibitors of 14α-demethylase have been confirmed ...
*  Mycosphaerella graminicola
... now relies on the application of azole fungicides which are demethylase inhibitors that inhibit lanosterol 14 alpha-demethylase ... Asci measure 11-14 × 30-40 μm. Ascospores are hyaline, elliptical, and 2.5-4 × 9-16 μm, with two cells of unequal length. ...
*  Itraconazole
... 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] ... These distinct activities are unrelated to inhibition of the cytochrome P450 lanosterol 14 alpha-demethylase and the exact ... The clinical formulation is a 1:1:1:1 mixture of four stereoisomers (two enantiomeric pairs). Fluconazole Lanosterol 14α- ...
*  Isavuconazonium
Inducers result in levels of isavuconazole that are too low and won't work, and inhibitors can cause high levels of ... Isavuconazole works by inhibiting lanosterol 14 alpha-demethylase, the enzyme responsible for converting lanosterol to ...
*  Ketoconazole
... shampoo in conjunction with an oral 5α-reductase inhibitor has been used off label to treat androgenic alopecia. ... Both isomers were relatively weak inhibitors of human placental aromatase. Resistance to ketoconazole has been observed in a ... Defects in the sterol 5-6 desaturase enzyme reduce the toxic effects of azole inhibition of the 14-alpha demethylation step. ... 624-. ISBN 978-0-7817-8355-2. J. Elks (14 November 2014). The Dictionary of Drugs: Chemical Data: Chemical Data, Structures and ...
*  Chromosome 11 (human)
Srp receptor alpha subunit TAF1D: TATA box binding protein associated factor RNA polymerase 1 subunit D TALDO1 encoding protein ... 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 LPXN: leupaxin LRFN4 encoding protein Leucine rich repeat and ... encoding protein Apoptosis inhibitor 5 APLNR: Apelin receptor (APJ receptor) APOA4: apolipoprotein A-IV ARCN1 encoding protein ...
*  Chromosome 7 (human)
... encoding protein Lysine demethylase 7A LRRC17: leucine-rich repeat containing protein 17 LSM5: U6 small nuclear RNA and mRNA ... inhibitor of growth protein 3 INTS1: encoding protein Integrator complex subunit 1 IQCE: IQ domain-containing protein E KDM7A: ... encoding enzyme Alpha-aminoadipic semialdehyde synthase, mitochondrial ARHGEF35: encoding protein Rho guanine nucleotide ... 2014-05-14]. Pertea M, Salzberg SL (2010). "Between a chicken and a grape: estimating the number of human genes". Genome Biol. ...
*  Steroidogenesis inhibitor
"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 symptoms in animals similar to those seen SLOS, and as such, like 24-DHCR inhibitors (see below), are ... Steroidogenic enzyme Neurosteroidogenesis inhibitor Vanden Bossche H (1992). "Inhibitors of P450-dependent steroid biosynthesis ...
*  Gilead Sciences
This acquisition gave Gilead first-in-class small molecule inhibitors of histone demethylases involved in regulating gene ... Ioannis Stamatopoulos (2017-02-12). "Pharma M&A In 2017: The Most Likely Deal Hunters". Seeking Alpha. Retrieved 2017-03-12. ... 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 ...
*  Chromatin remodeling
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). ... Hence, strategies are now being tried to overcome epigenetic silencing with synergistic combination of HDAC inhibitors or HDI ...
*  PELP-1
... 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 ...
*  2-oxoglutarate (2OG)-dependent dioxygenases
... 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 ... "Direct detection of oxygen intermediates in the non-heme Fe enzyme taurine/alpha-ketoglutarate dioxygenase". J. Am. Chem. Soc. ... The inhibitors that were regularly used to target 2OG-dependent dioxygenase include N-oxalylglycine (NOG), pyridine-2,4- ...
*  Reelin
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- ...
*  Epigenetics of neurodegenerative diseases
DNA methyltransferase inhibitors, and histone demethylase inhibitors (Urdinguio et al., 2009; Peedicayil, 2013). The majority ... "Sirtuin 2 inhibitors rescue alpha-synuclein-mediated toxicity in models of Parkinson's disease." Science 317.5837 (2007): 516-9 ... Vorinostat In an alpha-synuclein overexpressing Drosophila model of PD, vorinostat (as well as sodium butyrate) reduced alpha- ... Histone deacetylase (HDAC) inhibitors are the main compounds that have been tested to increase SMN2 mRNA expression. Inhibiting ...
*  Christopher J. Schofield
"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 ...
*  Meldonium
Potential Clinical Advantages of Tight Binding Inhibitors [Chapter 7, §7.8]". Evaluation of Enzyme Inhibitors in Drug Discovery ... 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 ... high affinity of …tight binding inhibitors allows one to minimize the dose of drug to which patients are exposed, thus limiting ...
*  Stress granule
Tsai WC, Reineke LC, Jain A, Jung SY, Lloyd RE (September 2017). "Histone arginine demethylase JMJD6 is linked to stress ... Mahboubi H, Barisé R, Stochaj U (July 2015). "5'-AMP-activated protein kinase alpha regulates stress granule biogenesis". ... "Ribonuclease/angiogenin inhibitor 1 regulates stress-induced subcellular localization of angiogenin to control growth and ... "Pur-alpha functionally interacts with FUS carrying ALS-associated mutations". Cell Death & Disease. 6: e1943. doi:10.1038/cddis ...
Lanosterol 14 alpha-demethylase - Wikipedia  Lanosterol 14 alpha-demethylase - Wikipedia
"Mutations in the CYP51 Gene Correlated with Changes in Sensitivity to Sterol 14Alpha-Demethylation Inhibitors in Field Isolates ... "Substrate Preferences and Catalytic Parameters Determined by Structural Characteristics of Sterol 14alpha-demethylase (CYP51) ... "Amino Acid Substitutions in the Cytochrome P-450 Lanosterol 14Alpha-Demethylase (CYP51A1) from Azole-resistant Candida albicans ... The effectiveness of imidazoles and triazoles (common azole subclasses) as inhibitors of 14α-demethylase have been confirmed ...
more infohttps://en.wikipedia.org/wiki/Lanosterol_14_alpha-demethylase
RCSB PDB 









- 5TZ1: Crystal structure of sterol 14-alpha demethylase (CYP51) from Candida albicans in complex with the...  RCSB PDB - 5TZ1: Crystal structure of sterol 14-alpha demethylase (CYP51) from Candida albicans in complex with the...
Structural analyses of Candida albicans sterol 14 alpha-demethylase complexed with azole drugs address the molecular basis of ... Classification: OXIDOREDUCTASE / OXIDOREDUCTASE INHIBITOR * Deposited: 2016-11-21 Released: 2017-03-15 ... Sterol 14-alpha demethylase A, B 490 Candida albicans EC#: 1.14.13.70 IUBMB Mutation: A48P, S263L Gene Name(s): ERG11 CYP51 ... Crystal structure of sterol 14-alpha demethylase (CYP51) from Candida albicans in complex with the tetrazole-based antifungal ...
more infohttp://www.rcsb.org/pdb/explore/explore.do?structureId=5TZ1
RCSB PDB 









- 1E9X: Cytochrome P450 14 alpha-sterol demethylase (CYP51) from Mycobacterium tuberculosis in complex with...  RCSB PDB - 1E9X: Cytochrome P450 14 alpha-sterol demethylase (CYP51) from Mycobacterium tuberculosis in complex with...
Sterol Demethylase (Cyp51) from Mycobacterium Tuberculosis in Complex with Azole Inhibitors ... Cytochrome P450 14 alpha-sterol demethylase (CYP51) from Mycobacterium tuberculosis in complex with 4-phenylimidazole. ...
more infohttp://www.rcsb.org/pdb/explore/materialsAndMethods.do?structureId=1E9X
KDM2A Gene - GeneCards | KDM2A Protein | KDM2A Antibody  KDM2A Gene - GeneCards | KDM2A Protein | KDM2A Antibody
Lysine Demethylase 2A, including: function, proteins, disorders, pathways, orthologs, and expression. GeneCards - The Human ... JMJD2 demethylase inhibitor, potent and cell-permeable. 1222800-79-4. SP2509. Demethylase 1 (LSD1) antagonist, novel Lysine- ... alpha proteobacteria (Wolbachia pipientis). *amoeba (Dictyostelium discoideum). *Archea (Pyrococcus horikoshii). *barley ( ... CpG islands recruit a histone H3 lysine 36 demethylase. (PMID: 20417597) Blackledge NP … Klose RJ (Molecular cell 2010) 3 4 60 ...
more infohttp://www.genecards.org/cgi-bin/carddisp.pl?gene=KDM2A
An Open Study of the Effect of Itraconazole Oral Solution for the Treatment of Fluconazole Refractory Oropharyngeal Candidiasis...  An Open Study of the Effect of Itraconazole Oral Solution for the Treatment of Fluconazole Refractory Oropharyngeal Candidiasis...
Cytochrome P-450 CYP3A Inhibitors. Cytochrome P-450 CYP2C9 Inhibitors. Cytochrome P-450 CYP2C19 Inhibitors. ... Enzyme Inhibitors. Molecular Mechanisms of Pharmacological Action. Steroid Synthesis Inhibitors. Hormone Antagonists. Hormones ... Patients who relapse during follow-up are re-treated for 14-28 days; if lesions clear, patients may enter the maintenance ... 14-alpha Demethylase Inhibitors. Cytochrome P-450 Enzyme Inhibitors. ...
more infohttps://www.clinicaltrials.gov/ct2/show/NCT00002133
Treatment With Tamoxifen in Cryptococcal Meningitis - Full Text View - ClinicalTrials.gov  Treatment With Tamoxifen in Cryptococcal Meningitis - Full Text View - ClinicalTrials.gov
2013 Apr 4;368(14):1291-1302. doi: 10.1056/NEJMoa1110404. Beardsley J, Wolbers M, Kibengo FM, Ggayi AB, Kamali A, Cuc NT, Binh ... Tamoxifen will be given orally in a dose of 300mg/day for the first 14 days following randomization. It will be administered by ... Intervention arm: Induction phase treatment (days 1-14): Tamoxifen will be given orally in a dose of 300mg/day for the first 14 ... Intracranial pressure (ICP) will be measured at study entry, day 3, 7, and 14, and at other times as clinically indicated. The ...
more infohttps://clinicaltrials.gov/ct2/show/NCT03112031?term=meningitis&rank=29
Study of Intradermal Quadrivalent Influenza Vaccine in Adults Aged 18 Through 64 Years - Full Text View - ClinicalTrials.gov  Study of Intradermal Quadrivalent Influenza Vaccine in Adults Aged 18 Through 64 Years - Full Text View - ClinicalTrials.gov
Enzyme Inhibitors. Molecular Mechanisms of Pharmacological Action. Steroid Synthesis Inhibitors. Hormone Antagonists. Hormones ... 14-alpha Demethylase Inhibitors. Cytochrome P-450 Enzyme Inhibitors. ...
more infohttps://clinicaltrials.gov/ct2/show/NCT01712984
An Open-label, Two-period, Fixed-sequence Study to Evaluate Multiple-dose Itraconazole Effect on The Single-dose PK of PF...  An Open-label, Two-period, Fixed-sequence Study to Evaluate Multiple-dose Itraconazole Effect on The Single-dose PK of PF...
Enzyme Inhibitors. Molecular Mechanisms of Pharmacological Action. Steroid Synthesis Inhibitors. Hormone Antagonists. Hormones ... History of regular alcohol consumption exceeding 7 drinks/week for females or 14 drinks/week for males (1 drink = 5 ounces (150 ... 14-alpha Demethylase Inhibitors. Cytochrome P-450 Enzyme Inhibitors. ...
more infohttps://www.clinicaltrials.gov/ct2/show/NCT02475746?term=Itraconazole&rank=28
Lysine Specific Demethylase 1 (LSD-1) Inhibitor -Pipeline Insight, 2018  Lysine Specific Demethylase 1 (LSD-1) Inhibitor -Pipeline Insight, 2018
Figures 1: Total Products for Lysine Specific Demethylase 1 (LSD-1) Inhibitor. Figure 2: Lysine Specific Demethylase 1 (LSD-1) ... Table 1: Total Pipeline Products for Lysine Specific Demethylase 1 (LSD-1) Inhibitor. Table 2: Lysine Specific Demethylase 1 ( ... 6. Lysine Specific Demethylase 1 (LSD-1) Inhibitor Pipeline Products in Non-clinical Stages 6.1 Drug Name : Company Name* ... Inhibitor The report assesses the active Lysine Specific Demethylase 1 (LSD-1) Inhibitor pipeline products by developmental ...
more infohttps://www.researchandmarkets.com/reports/4382669/lysine-specific-demethylase-1-lsd-1-inhibitor
ChemIDplus - 194798-83-9 - GHJWNRRCRIGGIO-UHFFFAOYSA-N - Fosfluconazole [INN:BAN] - Similar structures search, synonyms,...  ChemIDplus - 194798-83-9 - GHJWNRRCRIGGIO-UHFFFAOYSA-N - Fosfluconazole [INN:BAN] - Similar structures search, synonyms,...
2,4-Difluoro-alpha,alpha-bis(1H-1,2,4-triazol-1-ylmethyl)benzyl alcohol, dihydrogen phosphate (ester) ... 2,4-Difluoro-alpha,alpha-bis(1H-1,2,4-triazol-1-ylmethyl)benzyl alcohol, dihydrogen phosphate (ester) ...
more infohttps://chem.nlm.nih.gov/chemidplus/rn/194798-83-9
Anidulafungin/voriconazole - AdisInsight  Anidulafungin/voriconazole - AdisInsight
Glucan synthase inhibitors * Orphan Drug Status Orphan designation is assigned by a regulatory body to encourage companies to ...
more infohttp://adisinsight.springer.com/drugs/800026872?error=cookies_not_supported&code=6225a542-7561-44f3-8524-e03fc39a3328
Fluconazole transdermal - AdisInsight  Fluconazole transdermal - AdisInsight
Mechanism of Action 14-alpha demethylase inhibitors * Orphan Drug Status Orphan designation is assigned by a regulatory body to ...
more infohttps://adisinsight.springer.com/drugs/800019867?error=cookies_not_supported&code=add34677-bafa-46bd-b22e-88e166629e9b
VT 1129 - Drug Approvals International  VT 1129 - Drug Approvals International
... a small-molecule lanosterol demethylase inhibitor, developed using the company's Metallophile technology, for treating fungal ... The Fungal Cyp51 Inhibitors VT-1161 and VT-1129 Maintain in vitro Activity Against Candida albicans Isolates with Reduced ... VT-1129 has shown high potency and selectivity in in vitro studies and is an orally administered inhibitor of fungal CYP51, a ... Novel Metalloenzyme Inhibitors, VT-1161 and VT-1129, Exhibit Efficacy and Survival Benefit in a Murine Systemic Candidiasis ...
more infohttp://drugapprovalsint.com/vt-1129/
Isoconazole - Drugs Prescribing Information  Isoconazole - Drugs Prescribing Information
Allylamines (squalene epoxidase inhibitors) : Ergosterol inhibitors Topical: Amorolfine • Naftifine • Terbinafine Systemic: ... Ergosterol inhibitors Imidazoles Topical: Bifonazole • Clotrimazole • Econazole • Fenticonazole • Ketoconazole • Isoconazole • ... Echinocandins (β-glucan synthase inhibitors) : Cell wall target Anidulafungin • Caspofungin • Micafungin Pyrimidine analogues ...
more infohttp://drugspi.org/Isoconazole
Fluconazole - Drugs Prescribing Information  Fluconazole - Drugs Prescribing Information
Allylamines (squalene epoxidase inhibitors) : Ergosterol inhibitors Topical: Amorolfine • Naftifine • Terbinafine Systemic: ... Fluconazole is a potent inhibitor of CYP2C19 and a moderate inhibitor of CYP3A4 and CYP2C9: there is a risk of increased plasma ... Ergosterol inhibitors Imidazoles Topical: Bifonazole • Clotrimazole • Econazole • Fenticonazole • Ketoconazole • Isoconazole • ... Echinocandins (β-glucan synthase inhibitors) : Cell wall target Anidulafungin • Caspofungin • Micafungin Pyrimidine analogues ...
more infohttp://drugspi.org/Diflucan
Lanosterol 14 alpha-demethylase - Wikipedia  Lanosterol 14 alpha-demethylase - Wikipedia
... effects of P45014DM inhibitors on sterol biosynthesis downstream of lanosterol". Journal of Lipid Research. 32 (6): 893-902. ... "Sterol 14alpha-demethylase cytochrome P450 (CYP51), a P450 in all biological kingdoms". Biochimica et Biophysica Acta. 1770 (3 ... "Amino acid substitutions in the cytochrome P-450 lanosterol 14alpha-demethylase (CYP51A1) from azole-resistant Candida albicans ... "Substrate preferences and catalytic parameters determined by structural characteristics of sterol 14alpha-demethylase (CYP51) ...
more infohttps://en.wikipedia.org/wiki/Lanosterol_14%CE%B1-demethylase
AZW Download vtec assembly for honda element 2005 - My Blog  AZW Download vtec assembly for honda element 2005 - My Blog
alpha-demethylase inhibitors). Imidazoles. topical: Bifonazole, Clomidazole, Clotrimazole#, Croconazole, Econazole, ... inhibitors). topical: (Amorolfine, Butenafine, Naftifine, Terbinafine). systemic: (Terbinafine). -glucan synthase. inhibitors. ... Thymidylate synthase inhibitors. Flucytosine#. Mitotic inhibitors. Griseofulvin#. Others. Bromochlorosalicylanilide ... Imidazole has been used extensively as a corrosion inhibitor on certain transition metals, such as copper. Preventing copper ...
more infohttps://mechanicalwatch.org/pdf/azw-download-vtec-assembly-for-honda-element-2005
Avasimibe | P450 (e.g. CYP17) inhibitor | Read Reviews & Product Use Citations
		
	  Avasimibe | P450 (e.g. CYP17) inhibitor | Read Reviews & Product Use Citations
... cholesterol acyltransferase inhibitor with IC50 of 2.9, 13.9, 26.5 μM for CYP2C9, CYP1A2, and CYP2C19 Find all the information ... U73122 is a potent phospholipase C (PLC) inhibitor, which reduces agonist-induced Ca2+ increases in platelets and PMN. ... Abiraterone Acetate is an acetate salt form of Abiraterone which is a steroidal cytochrome CYP17 inhibitor with IC50 of 72 nM ... 3] Avasimibe inhibits ACTC with IC50 of 3.3 μM in IC-21 macrophages with consideration of the total inhibitor concentration in ...
more infohttps://www.selleckchem.com/products/Avasimibe
Abiraterone Acetate | P450 (e.g. CYP17) inhibitor | Read Reviews & Product Use Citations
		
	  Abiraterone Acetate | P450 (e.g. CYP17) inhibitor | Read Reviews & Product Use Citations
... inhibitor with an IC50 of 72 nM. Find all the information about Abiraterone Acetate (CB7630) for cell signaling research. ... P450 (e.g. CYP17) Inhibitors with Unique Features. * Pan P450 Inhibitor. Alizarin : CYP1A1, IC50=6.2 μM; CYP1A2, IC50=10.0 μM; ... Classic P450 Inhibitor. TAK-700 (Orteronel) : Potent and highly selective human 17,20-lyase inhibitor with IC50 of 38 nM, Phase ... Abiraterone Acetate is an acetate salt form of Abiraterone which is a steroidal cytochrome CYP17 inhibitor with IC50 of 72 nM ...
more infohttps://www.selleckchem.com/products/Abiraterone-Acetate-CB7630.html
  • Although lanosterol 14α-demethylase is present in a wide variety of organisms, this enzyme is studied primarily in the context of fungi , where it plays an essential role in mediating membrane permeability. (wikipedia.org)
  • The inhibition of its synthesis results in accumulation of toxic 14α-methylated sterols and the production of a defective cell membrane with altered permeability and leakage of cellular contents. (drugspi.org)
  • Blocking the synthesis of 7α,25-OHC in vivo with clotrimazole, a CYP7B1 inhibitor, reduced the content of 7α,25-OHC in the mouse spleen and promoted the migration of adoptively transferred pre-activated B cells to the T/B boundary (the boundary between the T-zone and B-zone in the spleen follicle), mimicking the phenotype of pre-activated B cells from EBI2-deficient mice. (nih.gov)
  • Memantine hydrochloride is a CYP2B6 and CYP2D6 inhibitor for recombinant CYP2B6 and CYP2D6 with K i of 0.51 nM and 94.9 μM, respectively. (abmole.com)
  • The enzymatic specificity and structures reported here provide a scaffold for the design and testing of specific inhibitors of CYP124. (pnas.org)