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Advancements in hit identification for membrane protein drug discovery

Drug Target Review

Advancements in screening technologies for small-molecule drug discovery including cellular assays, computational screening, and biophysics-based methods enhanced by structural biology breakthroughs have improved screening hit rates and facilitated the identification of drug candidates for previously undruggable targets.

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Target-directed cancer: protein-ligand interactions  

Drug Target Review

The mission of the CCDD is to discover novel small-molecule therapeutics for the treatment of cancer and progress them to hypothesis testing phase 1 clinical trials. We support the drug discovery projects of the CCDD with assay development and screening, biophysics, structural biology and recombinant protein production.

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Obstacles and innovations of macrocyclic drug development

Drug Target Review

Phase III trials for MK-0616 commenced in the second half of 2023. Phase 2b randomized trial of the oral PCSK9 inhibitor MK-0616. These drugs, including grazoprevir and vaniprevir, were the result of macrocyclisation of acyclic precursors. 8 Why are there not more macrocyclic drugs? Ballantyne CM, Banka P, Mendez G, et al.