Publications by authors named "D Moustakas"

Artificial intelligence is rapidly changing our world at an exponential rate and its transformative power has extensively reached important sectors like healthcare. In the fight against cancer, AI proved to be a novel and powerful tool, offering new hope for prevention and early detection. In this review, we will comprehensively explore the medical applications of AI, including early cancer detection through pathological and imaging analysis, risk stratification, patient triage, and the development of personalized prevention approaches.

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Background: Sovateltide (IRL-1620), an endothelin B receptor agonist, has previously demonstrated neuroprotective and neuroregenerative effects in animal models of acute ischemic stroke. Recently, clinical trials indicated that it could also be effective in humans with stroke. Here, we systematically investigate whether IRL-1620 may be used for the treatment of ischemia-induced brain injury.

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Fibroblast growth factor receptor (FGFR) kinase inhibitors have been shown to be effective in the treatment of intrahepatic cholangiocarcinoma and other advanced solid tumors harboring alterations, but the toxicity of these drugs frequently leads to dose reduction or interruption of treatment such that maximum efficacy cannot be achieved. The most common adverse effects are hyperphosphatemia caused by FGFR1 inhibition and diarrhea due to FGFR4 inhibition, as current therapies are not selective among the FGFRs. Designing selective inhibitors has proved difficult with conventional approaches because the orthosteric sites of FGFR family members are observed to be highly similar in X-ray structures.

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Article Synopsis
  • - The COVID Moonshot was a collaborative, open-science effort focused on finding a new drug to inhibit the SARS-CoV-2 main protease, which is crucial for the virus's survival.
  • - Researchers developed a novel noncovalent, nonpeptidic inhibitor that stands out from existing drugs targeting the same protease, employing advanced techniques like machine learning and high-throughput structural biology.
  • - Over 18,000 compound designs, 490 ligand-bound x-ray structures, and extensive assay data were generated and shared openly, creating a comprehensive and accessible knowledge base for future drug discovery efforts against coronaviruses.
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  • * RLY-4008 is a next-generation FGFR2 inhibitor that shows high selectivity over FGFR1 and FGFR4, effectively targeting both primary changes and resistance mutations seen in tumors.
  • * Early clinical trials indicate that RLY-4008 can successfully induce tumor regression without significant toxicities from other FGFR isoforms, highlighting its potential as a promising treatment for FGFR2-driven cancers.
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