Publications by authors named "A M Gollner"
Article Synopsis
- Mutations in the KRAS protein are common in cancer, with a notable example being the G12C mutation, which has targeted treatments.
- Researchers developed a novel small molecule that can degrade many KRAS mutations, demonstrating more effective and lasting effects compared to traditional inhibition.
- Their findings showed that this approach not only effectively kills cancer cells with KRAS mutations but also spares normal cells, leading to reduction in tumors in animal models.
Article Synopsis
- * MDM2-p53 antagonists can restore p53 activity but have dose-limiting toxicities such as thrombocytopenia and neutropenia; to reduce these side effects, less frequent dosing is being explored with drugs like brigimadlin.
- * Brigimadlin, a new MDM2-p53 antagonist, has shown promise in preclinical models by effectively restoring p53 function and inhibiting tumor growth in cancers with TP53 mutations, supporting its further testing in cancer
Background: The diagnosis of cardiac amyloidosis can be established non-invasively by scintigraphy using bone-avid tracers, but visual assessment is subjective and can lead to misdiagnosis. We aimed to develop and validate an artificial intelligence (AI) system for standardised and reliable screening of cardiac amyloidosis-suggestive uptake and assess its prognostic value, using a multinational database of Tc-scintigraphy data across multiple tracers and scanners.
Methods: In this retrospective, international, multicentre, cross-tracer development and validation study, 16 241 patients with 19 401 scans were included from nine centres: one hospital in Austria (consecutive recruitment Jan 4, 2010, to Aug 19, 2020), five hospital sites in London, UK (consecutive recruitment Oct 1, 2014, to Sept 29, 2022), two centres in China (selected scans from Jan 1, 2021, to Oct 31, 2022), and one centre in Italy (selected scans from Jan 1, 2011, to May 23, 2023).
Herein we report a method for the synthesis of indazoles from readily available 2-aminomethyl-phenylamines via N-N bond-forming oxidative cyclization. Inspired by indazole formation initially observed as a side product by N. Coskun et al.
View Article and Find Full Text PDFIn this study, a one-pot synthesis via photoinduced C(sp)-C(sp) coupling followed by amide formation to access proteolysis targeting chimeras (PROTACs) was developed. The described protocol was studied on cereblon (CRBN)-based E3-ligase binders and (+)-JQ-1, a bromodomain inhibitor, to generate BET (bromodomain and extra terminal domain) targeting protein degraders. The generated PROTACs were profiled in vitro and tested for their degradation ability with several potent candidates identified.
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