Thursday, July 11, 2024

PH-binding motifs as a platform for drug design: Lessons from protease-activated receptors

Inside activation of EGFR by PAR as indicated by Tyr-phosphorylation, potently inhibited by Pc(4-4). Credit: Oncoscience (2024). DOI: 10.18632/oncoscience.599 A new editorial paper was published in Oncoscience, titled “PH-binding motifs as a platform for drug design: Lessons from protease-activated receptors; PARs.” While targeted cancer therapy is greatly dependent on specific oncogenic pathways or conferred by genetic alterations, it remains challenging and somewhat disappointing. The high level of failure relies on the interplay between the dose for desired therapy versus toxicity, namely the therapeutic index. Furthermore, one should take into consideration Read More

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