Proviral integration site for Moloney murine leukemia virus (PIM) kinase family (PIM1, PIM2, and PIM3) comprises constitutively active serine/threonine kinases that function as proto-oncogenic and immune-inflammatory signaling nodes. In cancer, PIM kinases promote tumor growth, therapeutic resistance, and immune microe...
Qing-Yan Li, Q. Qiu, Lin Ding et al.· European journal of medicina...· 0 citations
USP1, a deubiquitinating enzyme critical for DNA damage repair, represents a promising therapeutic target for cancers. In this study, we employed scaffold hopping to design and synthesize a series of 1H-pyrrolo[3,2-c]pyridine-based USP1 inhibitors. Among these, the lead compound 38a displayed robust enzymatic and cellu...
Tao Yang, Xue Cui, Qing-Yan Li et al.· Journal of Medicinal Chemist...· 0 citations
(R)-A17, a novel, highly selective PARP1 inhibitor featuring a unique tricyclic scaffold, is developed and established as a promising candidate and the design strategy for the next-generation PARP1-targeted therapy is validated.
Zhongning Guo, Rongrong Sun, Lin-Yu Yang et al.· Journal of Medicinal Chemist...· 0 citations
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