The novel protein homeostatic modulator BTX306 is active in myeloma and overcomes bortezomib and lenalidomide resistance

新型蛋白质稳态调节剂 BTX306 在骨髓瘤中有效,并可克服硼替佐米和来那度胺的耐药性

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作者:Jianxuan Zou, Richard J Jones, Hua Wang, Isere Kuiatse, Fazal Shirazi, Elisabet E Manasanch, Hans C Lee, Robert Sullivan, Leah Fung, Normand Richard, Paul Erdman, Eduardo Torres, David Hecht, Imelda Lam, Brooke McElwee, Aparajita H Chourasia, Kyle W H Chan, Frank Mercurio, David I Stirling, Robert Z

Key messages

BTX306 has a unique thiophene-fused scaffold bearing phenylurea and glutarimide. BTX306 is more potent against myeloma cells than lenalidomide or pomalidomide. BTX306 overcomes myeloma cell resistance to lenalidomide or bortezomib in vitro. BTX306 is active against primary myeloma cells, and shows efficacy in vivo.

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