17187-79-0Relevant academic research and scientific papers
LIGNANS FROM JUNIPERUS THURIFERA
Feliciano, Arturo San,Medarde, Manuel,Lopez, Jose L.,Puebla, Pilar,Corral, Jose M. Miguel Del,Barrero, Alejandro F.
, p. 2863 - 2866 (1989)
The isolation and identification of two new natural lignans, (-)epi-podorhizol and deoxypicropodophyllotoxin, and 12 known lignans from a hexane extract of Juniperus thurifera is described.Key Word Index - Juniperus thurifera; Cupressaceae; deoxypicropodophyllotoxin; (-)epi-podorhizol; lignans.
Affinity-Driven Covalent Modulator of the Glyceraldehyde-3-Phosphate Dehydrogenase (GAPDH) Cascade
Chern, Jeffy,Lu, Chun-Ping,Fang, Zhanxiong,Chang, Ching-Ming,Hua, Kuo-Feng,Chen, Yi-Ting,Ng, Cheng Yang,Chen, Yi-Lin Sophia,Lam, Yulin,Wu, Shih-Hsiung
supporting information, p. 7040 - 7045 (2018/05/29)
Traditional medicines provide a fertile ground to explore potent lead compounds, yet their transformation into modern drugs is fraught with challenges in deciphering the target that is mechanistically valid for its biological activity. Herein we reveal that (Z)-(+)-isochaihulactone (1) exhibited significant inhibition against multiple-drug-resistant (MDR) cancer cell lines and mice xenografts. NMR spectroscopy showed that 1 resisted an off-target thiolate, thus indicating that 1 was a target covalent inhibitor (TCI). By identifying the pharmacophore of 1 (α,β-unsaturated moiety), a probe derived from 1 was designed and synthesized for TCI-oriented activity-based proteome profiling. By MS/MS and computer-guided molecular biology approaches, an affinity-driven Michael addition of the noncatalytic C247 residue of GAPDH was found to control the “ON/OFF” switch of apoptosis through non-canonically nuclear GAPDH translocation, which bypasses the common apoptosis-resistant route of MDR cancers.
