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Game-changing pan-TEAD inhibitor for solid tumours

Drug Target Review

TEAD proteins are crucial for tumour progression and drug resistance, making them an attractive focus for therapeutic interventions. Leveraging AI-guided structure-based drug design, Insilico’s research and development team generated an impressive portfolio of over 6,000 molecules and identified three highly promising hit series.

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Metabolism of five membered nitrogen containing heterocycles

Metabolite Tales Blog

2 Figure 1 Not only does the carboxylic acid moiety of the infamous drug zomepirac undergo conjugation to an unstable acyl glucuronide, the pyrrole undergoes oxidative metabolism to an epoxide intermediate that can be trapped by glutathione (Figure 2). 2a Figure 2 Also reported are more complex “per-oxidative” oxidations.