A5020947516- Liver Disease Diagnosis and Treatment
- Liver Diseases and Immunity
- Herpesvirus Infections and Treatments
- Virus-based gene therapy research
- Monoclonal and Polyclonal Antibodies Research
- Synthesis and biological activity
- Liver Disease and Transplantation
- Endoplasmic Reticulum Stress and Disease
- Retinoids in leukemia and cellular processes
- Animal Virus Infections Studies
- Synthesis and Characterization of Heterocyclic Compounds
- Peptidase Inhibition and Analysis
- Inflammatory mediators and NSAID effects
- Hepatocellular Carcinoma Treatment and Prognosis
- Neuropeptides and Animal Physiology
- Gene expression and cancer classification
- Radiomics and Machine Learning in Medical Imaging
- Polyomavirus and related diseases
- Proteoglycans and glycosaminoglycans research
- Systemic Sclerosis and Related Diseases
- Neuroendocrine Tumor Research Advances
- Synthesis and Reactions of Organic Compounds
- Helicobacter pylori-related gastroenterology studies
- Kruppel-like factors research
- Computational Drug Discovery Methods
Novartis (Switzerland)
2020-2024
Novartis Institutes for BioMedical Research
2022-2023
ETH Zurich
2011
Bayer (Switzerland)
2010
Pliva (Croatia)
2004
The multimodal activities of farnesoid X receptor (FXR) agonists make this class an attractive option to treat nonalcoholic steatohepatitis. safety and efficacy tropifexor, FXR agonist, in a randomized, multicenter, double-blind, three-part adaptive design, phase 2 study, patients with steatohepatitis were therefore assessed. In Parts A + B, 198 randomized receive tropifexor (10-90 μg) or placebo for 12 weeks. Part C, 152 140 µg, 200 µg (1:1:1) 48 primary endpoints tolerability end-of-study,...
Background and Aims: With distinct mechanisms of action, the combination tropifexor (TXR) cenicriviroc (CVC) may provide an effective treatment for NASH. This randomized, multicenter, double-blind, phase 2b study assessed safety efficacy TXR CVC combination, compared with respective monotherapies. Approach Results: Patients (N = 193) were randomized 1:1:1:1 to once-daily 140 μg (TXR ), 150 mg (CVC), + CVC), or 90 CVC) 48 weeks. The primary secondary end points histological improvement,...
Abstract Purpose To evaluate the safety and potential efficacy of LLF580, a genetically engineered variant human fibroblast growth factor-21, for triglyceride lowering, weight loss, hepatic fat reduction. Methods A multicenter, double-blind, parallel design trial in obese, mildly hypertriglyceridemic adults randomized (1:1) to LLF580 300 mg or placebo subcutaneously every 4 weeks 3 doses. Results Of 64 study participants, 61 (mean ± SD: age 45 11 years, 49% male, 80/15/5% Caucasian/African...
Bombesin is a peptide exhibiting high affinity for the gastrin-releasing receptor (GRPr), which highly overexpressed on prostate cancer cells. In present study, we developed an (18)F-labeled bombesin analog, (18)F-BAY 86-4367, currently being clinically tested use in PET of cancer.In vitro pharmacologic studies were performed to characterize nonradioactive ((19)F) standard analog binding and selectivity GRPr. The stability 86-4367 was determined murine human plasma. vivo, tumor-targeting...
The gastrin-releasing peptide receptor (GRPR) is overexpressed on a number of human tumors and has been targeted with radiolabeled bombesin analogues for the diagnosis therapy these cancers. Seven containing various linkers sequences were designed, synthesized, (18)F, characterized in vitro vivo as potential PET imaging agents. Binding studies displayed nanomolar binding affinities toward GRPR all synthesized analogues. Two high-affinity candidates 6b (K(i) = 0.7 nM) 7b 0.1 chosen further...
Non-alcoholic fatty liver disease (NAFLD) is the manifestation of metabolic syndrome with global prevalence reaching epidemic levels. Despite high burden in population only a small proportion those NAFLD will develop progressive disease, for which there currently no approved pharmacotherapy. Identifying who are at risk requires biopsy problematic. Firstly, invasive and therefore not appropriate use condition like that affects large population. Secondly, limited by sampling observer dependent...
Novel C-6 substituted pyrimidine derivatives are good substrates of herpes simplex virus type 1 thymidine kinase (HSV1-TK). Enzyme kinetic experiments showed that our lead compound, N-methyl DHBT (N-methyl-6-(1,3-dihydroxyisobutyl) thymine; N-Me DHBT), is phosphorylated at a similar rate compared to "gold standard" 9-[4-fluoro-3-(hydroxymethyl)butyl]guanine, FHBG, (K(m) = 10 ± 0.3 μM; k(cat) 0.036 0.015 sec(-1)). Additionally, it does not show cytotoxic properties on B16F1 cells up...
Abstract For see ChemInform in Full Text.
In multi-center randomized clinical trials imaging data can be diverse due to acquisition technology or scanning protocols. Models predicting future outcome of patients are impaired by this heterogeneity. Here, we propose a prediction method that cope with high number different sites and low samples per site. We cluster into pseudo-domains based on visual appearance scans, train pseudo-domain specific models. Results show they improve the accuracy for steatosis after 48 weeks from acquired...