ORCID Profile
0000-0002-3618-1208
Current Organisation
Bond University
Does something not look right? The information on this page has been harvested from data sources that may not be up to date. We continue to work with information providers to improve coverage and quality. To report an issue, use the Feedback Form.
Publisher: Elsevier BV
Date: 11-2014
DOI: 10.1016/J.BMCL.2014.09.036
Abstract: A versatile and high yielding synthesis of novel androgen receptor (AR) antagonists is presented. Using this methodology, six 1,4-substituted-1,2,3-triazole derived bicalutamide mimics were synthesised in five steps and in isolated overall yields from 41% to 85%. Evaluation of these compounds for their anti-proliferative properties against androgen dependent (LNCaP) and independent (PC-3) cells showed promising IC50 values of 34-45 μM and 29-151 μM, respectively. The data suggest that the latter compounds may be an excellent starting point for the development of prostate cancer therapeutics for both androgen dependent and independent forms of this disease. Docking of these compounds (each enantiomer) in silico into the T877A mutated androgen receptor, as possessed by LNCaP cells, was also undertaken.
Publisher: Elsevier BV
Date: 09-2014
DOI: 10.1016/J.EJMECH.2014.07.063
Abstract: A series of morpholine substituted amino acids (phenylalanine, leucine, lysine and glutamic acid) was synthesized. A fragment-based screening approach was then used to evaluate a series of small heterocycles, including morpholine, oxazoline, dihydro-1,3-oxazine, tetrahydro-1,3-oxazepine, thiazoline, tetrahydro-1,3-pyrimidine, tetrahydro-1,3-diazepine and hexahydro-1H-benzimidazole, as potential inhibitors of Glycogen Phosphorylase a. Thiazoline 7 displayed an improved potency (IC50 of 25 μM) and had good LE and LELP values, as compared to heterocycles 1, 5, 9-13 and 19 (IC50 values of 1.1 mM-23.9 mM). A docking study using the crystal structure of human liver Glycogen Phosphorylase, provided insight into the interactions of heterocycles 5, 7, 9-13 and 19 with Glycogen Phosphorylase.
Publisher: American Chemical Society (ACS)
Date: 10-09-2019
Publisher: Elsevier BV
Date: 06-2022
DOI: 10.1093/AJCN/NQAC035
Publisher: Elsevier BV
Date: 09-2023
Publisher: Elsevier BV
Date: 04-2021
Publisher: Elsevier BV
Date: 09-2023
Publisher: Oxford University Press (OUP)
Date: 23-01-2023
Abstract: Ginger (Zingiber officinale) has been investigated for its potentially therapeutic effect on a range of chronic conditions and symptoms in humans. However, a simplified and easily understandable examination of the mechanisms behind these effects is lacking and, in turn, hinders interpretation and translation to practice, and contributes to overall clinical heterogeneity confounding the results. Therefore, drawing on data from nonhuman trials, the objective for this narrative review was to comprehensively describe the current knowledge on the proposed mechanisms of action of ginger on conferring therapeutic health effects in humans. Mechanistic studies support the findings from human clinical trials that ginger may assist in improving symptoms and biomarkers of pain, metabolic chronic disease, and gastrointestinal conditions. Bioactive ginger compounds reduce inflammation, which contributes to pain promote vasodilation, which lowers blood pressure obstruct cholesterol production, which regulates blood lipid profile translocate glucose transporter type 4 molecules to plasma membranes to assist in glycemic control stimulate fatty acid breakdown to aid weight management and inhibit serotonin, muscarinic, and histaminergic receptor activation to reduce nausea and vomiting. Additional human trials are required to confirm the antimicrobial, neuroprotective, antineoplastic, and liver- and kidney-protecting effects of ginger. Interpretation of the mechanisms of action will help clinicians and researchers better understand how and for whom ginger may render therapeutic effects and highlight priority areas for future research.
Publisher: Elsevier BV
Date: 02-2017
Publisher: Elsevier BV
Date: 11-2016
DOI: 10.1016/J.JMGM.2016.10.008
Abstract: Gingerols and shogaols are the primary non-volatile actives within ginger (Zingiber officinale). These compounds have demonstrated in vitro to exert 5-HT
Publisher: Elsevier BV
Date: 05-2014
DOI: 10.1016/J.BMC.2014.03.018
Abstract: A range of 1,4-substituted-1,2,3-N-phenyltriazoles were synthesized and evaluated as non-steroidal androgen receptor (AR) antagonists. The motivation for this study was to replace the N-phenyl amide portion of small molecule antiandrogens with a 1,2,3-triazole and determine effects, if any, on biological activity. The synthetic methodology presented herein is robust, high yielding and extremely rapid. Using this methodology a series of 17 N-aryl triazoles were synthesized from commercially available starting materials in less than 3h. After preliminary biological screening at 20 and 40 μM, the most promising three compounds were found to display IC50 values of 40-50 μM against androgen dependent (LNCaP) cells and serve as a starting point for further structure-activity investigations. All compounds in this work were the focus of an in silico study to dock the compounds into the human androgen receptor ligand binding domain (hARLBD) and compare their predicted binding affinity with known antiandrogens. A comparison of receptor-ligand interactions for the wild type and T877A mutant AR revealed two novel polar interactions. One with Q738 of the wild type site and the second with the mutated A877 residue.
No related grants have been discovered for Anna Lohning.