Publications by authors named "Ross McLennan"
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.
Targeted protein degradation offers an alternative modality to classical inhibition and holds the promise of addressing previously undruggable targets to provide novel therapeutic options for patients. Heterobifunctional molecules co-recruit a target protein and an E3 ligase, resulting in ubiquitylation and proteosome-dependent degradation of the target. In the clinic, the oral route of administration is the option of choice but has only been achieved so far by CRBN- recruiting bifunctional degrader molecules.
View Article and Find Full Text PDFArticle Synopsis
- A highly selective Lewis base-catalyzed reaction is introduced, allowing for the efficient synthesis of oxazolidin-4-ones through a [3+2] cycloaddition involving ammonium enolates and oxaziridines.
- The use of enantioenriched oxaziridine creates a matched/mismatched effect with the catalyst, enabling the production of either syn- or anti-stereodefined compounds with high selectivity and yield.
- The resulting oxazolidin-4-one products can be further modified into valuable functionalized building blocks in organic synthesis.