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Journal: ERK inhibits osteoclast differentiation in RAW 264.7 cells through the osteoprotegerin-mediated autophagy. (Pubmed Central) - Mar 3, 2025
ERK inhibitors activated the Akt/mammalian target of the rapamycin (mTOR) signaling pathway while inhibiting unc-51-like autophagy activating kinase 1 (ULK1)...Therefore, ERK inhibition promoted OC differentiation by downregulating OPG-mediated inhibition of osteoclastogenesis and autophagy in RAW 264.7 cells. These findings highlight ERK's complex role in OC differentiation and suggest that understanding ERK's dual impact on OC differentiation can provide insights into novel treatment strategies for bone-related disorders.
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Discovery of DCC-3116. A selective, first-in-class ULK inhibitor for cancer therapy (Hybrid; Room 355 (Ernest N. Morial Convention Center)) - Mar 12, 2024 - Abstract #ACSSp2024ACS_Sp_10084;
We disclose herein the development of DCC-3116, a potent and selective inhibitor of ULK1/2 and report on its promising preclinical activity in a series of in vitro and in vivo studies. DCC-3116 is currently in Phase 1 clinical development in combination with RTK pathway inhibitors in patients with advanced or metastatic solid tumors with mutations in the pathway.
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