Fragment-Based Discovery of a Small-Molecule RhoGDI2 Ligand, HR3119, that Inhibits Cancer Cell Migration

Guanine nucleotide dissociation inhibitors (GDIs) proteins, including RhoGDI2, regulate the functions of Ras superfamily proteins that are known to be important cancer drug targets. Given the challenges in directly targeting Ras superfamily proteins with small molecules, targeting GDIs represents a...

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Váldodahkki:	Mingqing Liu (9356242) (author)
Eará dahkkit:	Shizhang Wan (22445332) (author), Shuangxi Guo (14304966) (author), Jiuyang Liu (5956922) (author), Wenqian Li (300451) (author), Lei Wang (6656) (author), Fudong Li (559033) (author), Jiahai Zhang (63883) (author), Xing Liu (221084) (author), Dan Liu (108669) (author), Xuebiao Yao (9931) (author), Jia Gao (221111) (author), Ke Ruan (520768) (author), Wei He (131453) (author)
Almmustuhtton:	2025
Fáttát:	Biophysics Biochemistry Pharmacology Biotechnology Immunology Cancer Infectious Diseases Chemical Sciences not elsewhere classified seen limited success micromolar affinity (< complex structure suggests rationally designed based 714 μm ). endogenous ligand rac1 work provides insights targeting gdis represents ras superfamily proteins early drug discovery chemistry starting points molecule rhogdi2 ligand hr3119 </ b based discovery 8 μm first ligand unique opportunity racemic mixture r </ preferentially bound phenotype studies nearly 100 k </ including rhogdi2 compound design >< sub >)-< b </ sub
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Fragment-Based Discovery of a Small-Molecule RhoGDI2 Ligand, HR3119, that Inhibits Cancer Cell Migration

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