STAT3 Differential Scanning Fluorimetry and Differential Scanning Light Scattering Assays: addressing a missing link in the characterization of STAT3 Inhibitor interactions

Publication date: Available online 17 July 2018Source: Journal of Pharmaceutical and Biomedical AnalysisAuthor(s): Matthieu Desroses, Sander Busker, Juan Astorga-Well, Sanaz Attarha, Iryna kolosenko, Roman Zubare, Thomas Helleday, Dan Grandér, Brent D.G. PageAbstractSTAT3 protein is an established target for the development of new cancer therapeutic agents. Despite lacking a traditional binding site for small molecule inhibitors, many STAT3 inhibitors have been identified and explored for their anti-cancer activity. Because STAT3 signaling is mediated by protein-protein interactions, indirect methods are often employed to determine if proposed STAT3 inhibitors bind to STAT3 protein. While established STAT3 inhibition assays (such as the fluorescence polarization assay, electrophoretic mobility shift assay and ELISAs) have been used to identify novel inhibitors of STAT3 signaling, methods that directly assess STAT3 protein-inhibitor interactions could facilitate the development of novel inhibitors. In this context, we herein report new STAT3 binding assays based on differential scanning fluorimetry (DSF) and differential scanning light scattering (DSLS) to characterize interactions between STAT3 protein and inhibitors. Several peptide and small molecule STAT3 inhibitors have been evaluated, and new insight into how these compounds may interact with STAT3 is provided.
Source: Journal of Pharmaceutical and Biomedical Analysis - Category: Drugs & Pharmacology Source Type: research

Related Links:

Abstract The combined immunotherapy of nivolumab and ipilimumab causes a variety of autoimmune-related adverse events (irAEs). The current report details a 70-year-old woman with clear cell renal cell carcinoma metastasis in the lung. Two weeks after two courses of treatment, the patient complained of headache, dizziness and nausea. Cerebrospinal fluid (CSF) analysis revealed an elevated protein level of 195 mg/dl and a significantly elevated white blood cell (WBC) count of 830/mm3 (lymphocytes, 825/mm3; neutrophils, 5/mm3). The results excluded malignancy and infection. The patient was diagnosed with aseptic meni...
Source: Clinical Lung Cancer - Category: Cancer & Oncology Authors: Tags: Mol Clin Oncol Source Type: research
Authors: Anttinen M PMID: 31701789 [PubMed - as supplied by publisher]
Source: Scandinavian Journal of Urology - Category: Urology & Nephrology Tags: Scand J Urol Source Type: research
Daria Riva Neurofibromatosis type-1 (NF1) is a monogenic tumor-predisposition syndrome creating a wide variety of cognitive and behavioral abnormalities, such as decrease in cognitive functioning, deficits in visuospatial processing, attention, and social functioning. NF1 patients are at risk to develop neurofibromas and other tumors, such as optic pathway gliomas and other tumors of the central nervous system. Few studies have investigated the impact of an additional diagnosis of brain tumor on the cognitive outcome of children with NF1, showing unclear results and without controlling by the effect of surgery, radio-...
Source: Cancers - Category: Cancer & Oncology Authors: Tags: Article Source Type: research
We report a case of a 47-year-old female known with metastatic papillary thyroid cancer. Her treatment history included total thyroidectomy and 3 previous radio ablations with a cumulative dose of 950 mCi of131I. On follow-up, her thyroglobulin levels had demonstrated a rising trend (from 3789.0 to 4240.0 ug/L) despite a123I whole-body scan demonstrating a reduction in tracer avid lesions. She was suspected of having radio-resistant disease. The patient underwent both18F-FDG and68Ga-PSMA PET/CT imaging with both scans demonstrating congruent lesions however with far greater intensity on the68Ga-PSMA study.
Source: Nuclear Medicine and Molecular Imaging - Category: Nuclear Medicine Source Type: research
ConclusionsWe suggest SPECT/CT as the primary modality of choice for the assessment of the ratio of diseased lung area. Both perfusion scan and SPECT/CT can be used for the prediction of postoperative lung function.
Source: Nuclear Medicine and Molecular Imaging - Category: Nuclear Medicine Source Type: research
Publication date: Available online 9 November 2019Source: Radiation Physics and ChemistryAuthor(s): Farahani Somayeh, Nader Riyahi Alam, Haghgoo Soheila, Shirazi Alireza, Geraily Ghazale, Gorji Ensiye, Kavousi NasibehAbstractOvercoming the tumor radioresistance along with protecting the adjacent normal tissues is considered as the ultimate goal of the radiation therapy. To achieve this goal, extensive studies have demonstrated the radiosensitization potential of the gold nanoparticles (AuNPs) during treatment with low-energy ionizing radiation due to their high-photoelectric absorption coefficient. Compared to the AuNPs, t...
Source: Radiation Physics and Chemistry - Category: Physics Source Type: research
Publication date: Available online 9 November 2019Source: Materials Today CommunicationsAuthor(s): Felipe Alves Batista, Sabryna Brena Cunha Fontele, Lubna Karine Beserra Santos, Livia Alves Filgueiras, Steffane Quaresma Nascimento, João Marcelo de Castro e Sousa, Juan Carlos Ramos Gonçalves, Anderson Nogueira MendesAbstractThe development of systems for transport and release of drugs, also known as Drug delivery system (DDS), and are being used as strategies to combat cancer. These systems can maintain drug delivery at therapeutic levels and protect it from premature degradation in the biological environment...
Source: Materials Today Communications - Category: Materials Science Source Type: research
CONCLUSION: Although MRIyT=2N0/TRG1-2 cannot predict all cases of a complete pathologic response, it can effectively predict a low rate of lymph node involvement and a better prognosis in patients who undergo total mesorectal excision. PMID: 31687781 [PubMed - as supplied by publisher]
Source: Surgical Technology International - Category: Surgery Tags: Surg Technol Int Source Type: research
In this study, A54 peptide was utilized to fabricate CK-loaded micelles (APD-CK) for liver targeting, using deoxycholic acid-O-carboxymethyl chitosan as the vehicle. The average particle size of APD-CK micelles was about 171.4 nm by dynamic light scattering in the hydrated state and their morphology were spherical with good dispersion. An in vitro release assay indicated pH-responsive and sustained release behavior through a mechanism of non-Fickian diffusion. Moreover, the in vitro cytotoxicity of the APD-CK micelles against HepG2 and Huh-7 cells was significantly stronger than that of CK up to 20 μg/mL. Enhance...
Source: Carbohydrate Polymers - Category: Biomedical Science Source Type: research
In this study, the sustained-release DOX-loaded implants were prepared by melt-molding method. The implants were characterized with regards to drug content uniformity, micromorphology and drug release profiles. Furthermore, differential scanning calorimetry (DSC) and Fourier transform infrared spectroscopy (FTIR) analyses were carried out to investigate the drug-excipient compatibility. To determine the local penetration of DOX in liver, the minipigs received intrahepatic implantation of DOX-loaded implants by abdominal surgery. UPLC-MS/MS method was used to detect the concentration of DOX in liver tissues. Our results sug...
Source: Drug Delivery - Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research
More News: Cancer | Cancer & Oncology | Drugs & Pharmacology | PET Scan