A5078987885- Chromatin Remodeling and Cancer
- Cancer Mechanisms and Therapy
- Protein Degradation and Inhibitors
- Retinoids in leukemia and cellular processes
- Peptidase Inhibition and Analysis
- Mechanisms of cancer metastasis
- Estrogen and related hormone effects
- Acute Myeloid Leukemia Research
- Epigenetics and DNA Methylation
- Research on Leishmaniasis Studies
- interferon and immune responses
- Pharmacogenetics and Drug Metabolism
- Renin-Angiotensin System Studies
- Cancer-related Molecular Pathways
- Cancer-related gene regulation
- Virus-based gene therapy research
- Microtubule and mitosis dynamics
- Vitamin D Research Studies
- Cancer Treatment and Pharmacology
- Synthesis and biological activity
- Advanced biosensing and bioanalysis techniques
- Alcohol Consumption and Health Effects
- Heat shock proteins research
- Chronic Lymphocytic Leukemia Research
- Vitamin C and Antioxidants Research
Constellation Pharmaceuticals (United States)
2024
Morpho (United States)
2024
Silicon Therapeutics (United States)
2019-2022
Pfizer (United States)
2015
National Institutes of Health
1997-2001
National Cancer Institute
1997-2001
Queen's University
2000
Southern Research Institute
1998
University of Alabama at Birmingham
1998
Sanford Burnham Prebys Medical Discovery Institute
1998
Retinoids, particularly all- trans -retinoic acid (RA), are potent regulators of cell differentiation, proliferation, and apoptosis. The role -RA during development in the maintenance adult tissues has been well established. control levels cells is regulated by balance between its biosynthesis catabolism to inactive metabolites. cytochrome P450 enzyme P450RAI (herein renamed P450RAI-1) partially responsible for this inactivation -RA. In report, we describe identification, molecular cloning,...
Retinoids are potent regulators of cell proliferation, differentiation, and morphogenesis important therapeutic agents in oncology dermatology. The gene regulatory activity endogenous retinoids is effected primarily by retinoic acid isomers (all-trans 9-cis) that synthesized from retinaldehyde precursors a broad range tissues act as ligands for nuclear receptors. catabolism all-trans-retinoic (atRA) an mechanism controlling RA levels tissues. We have previously identified two cytochrome...
Abstract Recurrent somatic mutations in the BRG1/BRM-associated factor (BAF) chromatin remodeling complex subunit ARID1A occur frequently advanced urothelial, endometrial, and ovarian clear cell carcinomas, creating an alternative state that may be exploited therapeutically. The histone methyltransferase EZH2 has been previously identified as targetable vulnerability context of mutations. In this study, we describe discovery tulmimetostat, orally available, clinical stage inhibitor, it...
Long chain fatty acids have recently emerged as critical signaling molecules in neuronal, cardiovascular, and renal processes, yet little is presently known about the precise mechanisms controlling their tissue distribution bioactivation. We identified a novel cytochrome P450, CYP2U1, which may play an important role modulating arachidonic acid pathway. Northern blot real-time PCR analysis demonstrated that CYP2U1 transcripts were most abundant thymus brain (cerebellum), indicating specific...
Abstract 1α,25‐Dihydroxyvitamin D 3 (1,25D ) displays potent antiproliferative activity in a variety of tumor model systems and is currently under investigation clinical trials cancer. Studies were initiated to explore its potential nonsmall cell lung cancer (NSCLC), as effective approaches the treatment that disease are needed. In evaluating factors may affect NSCLC, authors found CYP24 (25‐hydroxyvitamin ‐24‐hydroxylase), enzyme catabolizes 1,25D , frequently expressed NSCLC lines but not...
Abstract The protein STING (stimulator of interferon genes) is a central regulator the innate immune system and plays an important role in antitumor immunity by inducing production cytokines such as type I (IFN). Activation stems from selective recognition endogenous cyclic dinucleotides (CDNs) large, polar, flexible binding site, thus posing challenges to design small molecule agonists with drug-like physicochemical properties. In this work we present SNX281, agonist that functions through...
We recently synthesized several conformationally constrained retinoic acid (RA) analogues [8-(2'-cyclohexen-1'-ylidene)-3,7-dimethyl-2,4,6-octatrienoic acids with different alkyl substituents at 2' (R1) and 3' (R2) positions on the cyclohexene ring] (Muccio et al. J. Med. Chem. 1996, 39, 3625) as cancer chemopreventive agents. UAB8 (R1 = Et; R2 iPr), which contains sufficient steric bulk terminal end of polyene chain to mimic trimethylcyclohexenyl ring RA, displayed biological properties...
Abstract The lectin jacalin is mitogenic for CD4 expressing T lymphocytes, interacts with the molecule, and inhibits HIV infection of CD4+ cells. In present study effect was tested on cells from monocyte/macrophage lineage that also express molecule. We used promyelomonocytic U937 differentiated towards monocytic/macrophage either a mixture two physiological agents, retinoic acid (RA) 1α,25-dihydroxyvitamin D3 (VD), or exogenous drug phorbol myristate acetate (PMA). resulting these...
Inhibition of hepatic efflux transporters (BSEP, MRP2) is one the important mechanisms in drug-induced liver injury and particular cholestasis. The inhibitory effect compounds on these two commonly delineated using inverted membrane vesicles from Sf9 insect cells overexpressing BSEP or MRP2 protein. However, due to lack bioactivation metabolism compound, expression functionality other sinusoidal uptake cell-free assay system, it difficult fully understand role a given transporter Therefore,...
<div>Abstract<p>Recurrent somatic mutations in the BRG1/BRM-associated factor (BAF) chromatin remodeling complex subunit ARID1A occur frequently advanced urothelial, endometrial, and ovarian clear cell carcinomas, creating an alternative state that may be exploited therapeutically. The histone methyltransferase EZH2 has been previously identified as targetable vulnerability context of mutations. In this study, we describe discovery tulmimetostat, orally available, clinical stage...
<p>Tulmimetostat mediated cancer cell phenotypic responses are increased in ARID1A LOF contexts.</p>