PPARβ/δ contributes to the antidiabetic effect and the increase in GDF15 caused by metformin [0.03%]
过氧化物酶体增殖激活受体β/δ介导二甲双胍的抗糖尿病作用及其诱导GDF15表达的作用
Javier Jurado-Aguilar,Emma Barroso,Patricia Rada et al.
Javier Jurado-Aguilar et al.
Metformin, the most prescribed drug for the treatment of type 2 diabetes mellitus, increases the circulating levels of the metabolic regulator growth differentiation factor 15 (GDF15) via transcriptional regulation, with the kidneys being r...
β-Hydroxybutyrate improves glymphatic system function and alleviates cerebral edema in mice after ischemic stroke [0.03%]
β-羟丁酸改善缺血性卒后小鼠的脑淋巴系统功能并缓解脑水肿
Ming-Jia Yu,Rui-Qi Xiong,Jing-Wen Wu et al.
Ming-Jia Yu et al.
Cerebral edema is a severe complication following ischemic stroke. Recent studies have highlighted the crucial role of the glymphatic system (GS) in the clearance of water and macromolecules. GS dysfunction involving the disorders of AQP4 p...
G protein-dependent dopamine D2 receptor signaling mediates cocaine-primed reinstatement [0.03%]
G蛋白依赖型多巴胺D2受体信号介导可卡因触发的复吸
Hai-Bo Li,Yong-Hui Liu,Hai Liu et al.
Hai-Bo Li et al.
The high relapse rate of drugs is currently a therapeutic dilemma in the treatment of substance use disorder (SUD). Emerging evidence from preclinical animal models demonstrates that pretreatment with selective dopamine D2 receptor (D2R) an...
Secoemestrin C exerts rapid and prominent anti-breast cancer effect in triple-negative breast cancer by inducing SLX4 and YAP degradation [0.03%]
秒萼酯类化合物Secoemestrin C通过诱导SLX4和YAP降解快速显著地抑制三阴性乳腺癌的作用
Xiao-Jun Zhao,Yang Xu,Cong-Hui Zhang et al.
Xiao-Jun Zhao et al.
Mitochondrial DNA (mtDNA) mutations are the most common cause in aberrant mitochondrion-leading cancer, exploration of direct targeting mutated mtDNA still remains incomplete. Secoemestrin C (Sec C) is epitetrathiodioxopiperazine derived fr...
Benchmarking co-folding methods to predict the structures of covalent protein-ligand complexes [0.03%]
评估预测共价蛋白质-配体复合物结构的协同折叠方法
Tong-Han Zhang,Jin-Tao Zhu,Zhi-Xian Huang et al.
Tong-Han Zhang et al.
Targeted covalent inhibitors (TCIs) are emerging as a new modality in drug discovery because of their strong binding affinity and prolonged target engagement. However, the rational design of TCIs remains a significant challenge and is hinde...
Sigma-1 receptor positive allosteric modulator promotes neuronal survival and improves cognitive deficits in AD mice via sigma-1 receptor/ERK pathway [0.03%]
σ-1受体正向变构调节剂促进AD小鼠神经元存活及认知功能的改善并通过σ-1受体/ERK通路实现上述作用
Xiao-Yu Wang,Wen-Shu Zhou,Uma Gaur et al.
Xiao-Yu Wang et al.
The sigma-1 receptor is an important new therapeutic drug target for Alzheimer's disease (AD). Here, we reported that SOMCL-668, a novel selective and potent sigma-1 receptor allosteric modulator, is neuroprotective in AD both in vitro and ...
Sophocarpine alleviates chronic itch in mouse atopic dermatitis by inhibiting spinal astrocyte reactivity and pro-inflammatory signaling [0.03%]
Sophocarpine通过抑制星形胶质细胞活化和促炎信号转导缓解小鼠特应性皮炎慢性瘙痒
Meng-Ping Lou,Xin-Yi Gao,He-Ting Yan et al.
Meng-Ping Lou et al.
Chronic itch is a debilitating symptom of atopic dermatitis (AD). Current therapeutic approaches for managing this condition include topical and systemic pharmacological agents with inconsistent efficacy and potential adverse effects. Sopho...
Targeting RSK2 enhances the efficacy of IGF1R inhibitor against triple-negative breast cancer via antagonizing IGF1/IGF1R signaling mediated by GATA3-IGFBP5 pathway [0.03%]
靶向RSK2通过GATA3-IGFBP5途径拮抗IGF1/IGF1R信号增强胰岛素样生长因子1受体抑制剂对三阴性乳腺癌的治疗效果
Tian-Jiao Shan,Lan-Ya Li,Xiao-Ya Wan et al.
Tian-Jiao Shan et al.
Targeting the IGF1 system holds promise as a therapeutic approach for breast cancer. However, the intricate nature of IGF1 signaling and suboptimal drug combinations have resulted in limited clinical success. This study demonstrates that si...
Clozapine impaired the hypoglycemic effect of metformin by inhibiting hepatic organic cation transporter 1 (OCT1) [0.03%]
氯氮平通过抑制肝脏阳离子转运蛋白1(OCT1)削弱二甲双胍的降糖作用
Wen-Han Wu,Yi-Dong Dai,Wen-Ke Feng et al.
Wen-Han Wu et al.
Atypical antipsychotics often cause hyperglycemia, with clozapine showing the highest risk. Metformin is a first-line medication for managing diabetes or prediabetes and is often used to control clozapine-induced hyperglycemia. Clinical stu...
β-Sitosterol ameliorates metabolic dysfunction-associated steatohepatitis by targeting the RAC1/mTOR/TFEB axis thus activating lipophagy-lysosomal pathway [0.03%]
通过靶向RAC1/mTOR/TFEB轴激活脂噬-溶酶体途径从而改善代谢功能障碍相关steatohepatitisβ-谷固醇的作用
Yang Wang,Yi Sun,Chang-Yuan Wang et al.
Yang Wang et al.
Metabolic dysfunction-associated steatohepatitis (MASH), an inflammatory subtype of metabolic dysfunction-associated fatty liver disease (MAFLD), drives hepatic dysfunction and poses a significant health burden. Lipophagy dysfunction disrup...