T
Tianfeng Xu
Researcher at Guangzhou Institutes of Biomedicine and Health
Publications - 30
Citations - 885
Tianfeng Xu is an academic researcher from Guangzhou Institutes of Biomedicine and Health. The author has contributed to research in topics: Chemistry & Medicine. The author has an hindex of 11, co-authored 19 publications receiving 550 citations. Previous affiliations of Tianfeng Xu include University of Michigan & Chinese Academy of Sciences.
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Journal ArticleDOI
Discovery of ARD-69 as a Highly Potent Proteolysis Targeting Chimera (PROTAC) Degrader of Androgen Receptor (AR) for the Treatment of Prostate Cancer.
Xin Han,Chao Wang,Chong Qin,Weiguo Xiang,Ester Fernandez-Salas,Chao Yie Yang,Mi Wang,Lijie Zhao,Tianfeng Xu,Krishnapriya Chinnaswamy,James Delproposto,Jeanne A. Stuckey,Shaomeng Wang +12 more
TL;DR: The discovery of highly potent PROTAC degraders of androgen receptor (AR), as exemplified by compound 34 (ARD-69), capable of reducing the AR protein level by >95% in these prostate cancer cell lines and effectively suppressing AR-regulated gene expression may ultimately lead to a new therapy for AR+, castration-resistant prostate cancer.
Journal ArticleDOI
Discovery of Highly Potent and Efficient PROTAC Degraders of Androgen Receptor (AR) by Employing Weak Binding Affinity VHL E3 Ligase Ligands.
Xin Han,Lijie Zhao,Weiguo Xiang,Chong Qin,Bukeyan Miao,Tianfeng Xu,Mi Wang,Chao Yie Yang,Krishnapriya Chinnaswamy,Jeanne A. Stuckey,Shaomeng Wang +10 more
TL;DR: This study resulted in the discovery of 11 (ARD-266), which effectively induces degradation of AR protein in AR-positive (AR+) LNCaP, VCaP, and 22Rv1 prostate cancer cell lines with DC50 values of 0.2-1 nM and effectively reduces AR-regulated gene expression suppression.
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Copper-catalyzed tandem reactions of 1-(2-iodoary)-2-yn-1-ones with isocyanides for the synthesis of 4-oxo-indeno[1,2-b]pyrroles.
TL;DR: A novel copper-catalyzed tandem reaction of 1-(2-iodoaryl)-2-yn-1-ones with isocyanides is described, which leads to efficient formation of 4-oxo-indeno[1,2-b]pyrroles.
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Design, Synthesis, and Biological Evaluation of Novel Conformationally Constrained Inhibitors Targeting Epidermal Growth Factor Receptor Threonine790 → Methionine790 Mutant
Chang Shaohua,Lianwen Zhang,Lianwen Zhang,Shilin Xu,Jinfeng Luo,Xiaoyun Lu,Zhang Zhang,Tianfeng Xu,Yingxue Liu,Zhengchao Tu,Yong Xu,Xiaomei Ren,Meiyu Geng,Jian Ding,Duanqing Pei,Ke Ding +15 more
TL;DR: A series of 2-oxo-3,4-dihydropyrimido[4,5-d]pyrimidinyl derivatives as novel EGFR inhibitors inhibited the enzymatic activities of wild-type and mutated EGFRs and displayed promising anticancer efficacy in a human NSCLC (H1975) xenograft nude mouse model.
Journal ArticleDOI
Design of the First-in-Class, Highly Potent Irreversible Inhibitor Targeting the Menin-MLL Protein-Protein Interaction.
Shilin Xu,Angelo Aguilar,Tianfeng Xu,Ke Zheng,Liyue Huang,Jeanne A. Stuckey,Krishnapriya Chinnaswamy,Denzil Bernard,Ester Fernandez-Salas,Liu Liu,Mi Wang,Donna McEachern,Sally Przybranowski,Caroline Foster,Shaomeng Wang +14 more
TL;DR: This study demonstrates that irreversible inhibition of menin may be a promising therapeutic strategy for MLL leukemia.