Evaluation of Cereblon-Directing Warheads for the Development of Orally Bioavailable PROTACs
化学
生物利用度
药理学
医学
作者
Marisa Actis,Joel O. Cresser-Brown,Elizabeth A. Caine,Martin Steger,Anup Aggarwal,Anand Mayasundari,Nancy E. Murphy,Gintvile Valinciute,Yong Li,Xiang Fu,Lei Yang,Graham P. Marsh,G. Hughes,Burhan Karadogan,Dean Wheeler,Mark C. Norley,Freya Spain,Marjeta Urh,Martine F. Roussel,Björn Schwalb
comparative study with analogues containing alternative CRBN-directing warheads. Our study highlights the importance of considering warhead modifications when optimizing PROTACs for oral delivery.