Mixed Lineage Kinase Suppression in Triple-Negative Breast Cancer: Identification of a Dual Inhibitor Targeting MLK3 and NAMPT [0.03%]
三阴性乳腺癌中混合谱系激酶的抑制作用：鉴定同时靶向MLK3和NAMPT的双重抑制剂
Ganga Reddy Velma,Sandeep Kumar,Piush Srivastava et al.
Ganga Reddy Velma et al.
Triple-negative breast cancer (TNBC) is aggressive and lacks targeted therapeutic options. Mixed lineage kinase 3 (MLK3) plays a key role in TNBC progression. To enhance the therapeutic impact of MLK3 inhibition in TNBC, a novel MLK3 inhibi...
Design, Synthesis, and Pharmacological Evaluation of cGAS/HDAC Dual Inhibitors for Treatment of Autoimmune Diseases [0.03%]
用于自身免疫疾病治疗的cGAS/HDAC双靶点抑制剂的设计、合成及药理学评价
Zihua Zhou,Mingjie Chen,Shuyue Lei et al.
Zihua Zhou et al.
cGAS overactivation is linked to various inflammatory and autoimmune diseases. Recent studies identify HDACs as critical regulators of cGAS, suggesting that dual cGAS/HDAC inhibition could be a novel therapeutic strategy. Herein, we report ...
Discovery of an Indole-Based p53-Y220C Reactivator with In Vivo Antitumor Activity via Structure-Guided Design [0.03%]
基于结构的药物设计发现一种能够激活p53Y220C突变体的吲哚类化合物及其抗肿瘤活性研究
Yule Ma,Xiaoning Zhu,Jiahao Yuan et al.
Yule Ma et al.
The oncogenic Y220C mutation destabilizes the p53 DNA-binding domain by creating a druggable surface crevice. Although the clinical advancement of PC14586 validates this target, the scarcity of structurally distinct correctors limits explor...
Correction to "Discovery of a New Four-Leaf Clover-Like Ligand as a Potent c-MYC Transcription Inhibitor Specifically Targeting the Promoter G-Quadruplex" [0.03%]
“四叶草配体的发现及其作为c-MYC转录抑制剂靶向启动子G-四链体的作用”一文的更正通知
Ming-Hao Hu,Yu-Qing Wang,Ze-Yi Yu et al.
Ming-Hao Hu et al.
Published Erratum
Journal of medicinal chemistry. 2026 Jun 10. DOI:10.1021/acs.jmedchem.6c01754 2026
Revisiting 2-Substituted-4(1 H)-Quinolones for Targeting the Plasmodium falciparum Cytochrome bc1 Complex [0.03%]
研究2位取代的4(1H)喹诺酮类化合物靶向恶性疟原虫cytochrome bc1复合体
Sovitj Pou,Katherine M Liebman,Rolf W Winter et al.
Sovitj Pou et al.
Quinolones substituted at the 2- and 3-positions with biaryl and diphenylether groups have been investigated for their antimalarial potential. ELQ-300, with a 3-position diphenyl ether, is at an advanced stage of preclinical development. He...
Gold(I)-Loaded Nanomedicine for Liver Cancer: A Closed-Loop Strategy Integrating Ferritinophagy-Driven Ferroptosis and Immunotherapy [0.03%]
基于铁死亡及免疫疗法的闭合环路策略封金基载药纳米体系用于肝癌治疗
Yejin Zhu,Yifei Li,Yuming Jiang et al.
Yejin Zhu et al.
The clinical translation of gold(I) pharmacophores for liver cancer is hindered by rapid deactivation, poor tumor selectivity, and off-target toxicity. To address these limitations, we engineered a tumor-targeting bovine serum albumin (BSA)...
Development and Preclinical Evaluation of 68Ga-Labeled B7-H3-Specific Bicyclic Peptides as Immuno-PET Tracers for Oncology [0.03%]
用于癌症免疫-PET显像的放射性68Ga标记B7-H3特异性双环肽 tracer 的开发和临床前评估
Fengsheng Zhang,Jindian Li,Dongliang Wang et al.
Fengsheng Zhang et al.
B7-H3 (CD276) is an emerging target for cancer theranostics, highlighting the need for imaging probes capable of noninvasively quantifying B7-H3 expression in tumors. Here, we developed three 68Ga-labeled B7-H3-targeting bicyclic peptide tr...
Structure-Based Design and Optimization of Novel PHGDH Inhibitors for Overcoming Erlotinib-Resistant Lung Cancer [0.03%]
基于结构的PHGDH抑制剂设计与优化用于克服肺癌吉非替尼耐药性
Xingmei Wu,Shuai Tang,Yiyang Yan et al.
Xingmei Wu et al.
Phosphoglycerate dehydrogenase (PHGDH), a key regulator in the serine biosynthesis pathway, is aberrantly expressed in various cancers, making it an attractive therapeutic target. In this study, we designed and synthesized a series of PHGDH...
All-Hydrocarbon Stapling and Amino Acid Substitution-Modified Antimicrobial Peptide Feleucin-K3 Analogs Enhanced the Stability and Optimized the Therapeutic Index against Multidrug-Resistant Bacteria [0.03%]
全碳氢化合物稳定和氨基酸替代优化抗菌肽Feleucin-K3衍生物对抗多重耐药细菌的治疗指数
Bei Gao,Yue Jia,Tiantian Yan et al.
Bei Gao et al.
Our previous research found that the poor stability of the antimicrobial peptide Feleucin-K3 (FK3) had limited its transition into clinical application. Herein, we developed a series of FK3 derivatives stapled by all-hydrocarbon and thioeth...
Dual SYK-HDAC Inhibitor Elicits Striking Efficacy against Acute Myeloid Leukemia: Rational Design, Synthesis, and Biological Evaluation [0.03%]
一种针对急性髓系白血病的双效SYK-HDAC抑制剂：理性设计、合成及生物活性评估
Anshul Mishra,Wen-Bin Yang,Tsu-Shao Liu et al.
Anshul Mishra et al.
An integrated transcriptomic and survival analysis led to the identification of SYK and HDAC isoforms as age- and FLT3-dependent prognostic markers in acute myeloid leukemia (AML). Driven by the aforementioned, our research group employed a...