Inhibition of a lower potency target drives the anticancer activity of a clinical p38 inhibitor [0.03%]
一款临床p38抑制剂的抗癌作用由抑制效力较低的靶点驱动
Debanjan Bhattacharjee,Jaweria Bakar,Surbhi P Chitnis et al.
Debanjan Bhattacharjee et al.
The small-molecule drug ralimetinib was developed as an inhibitor of the p38α mitogen-activated protein kinase, and it has advanced to phase 2 clinical trials in oncology. Here, we demonstrate that ralimetinib resembles EGFR-targeting drug...
In vivo bioluminescence imaging of labile iron in xenograft models and liver using FeAL-1, an iron-activatable form of D-luciferin [0.03%]
利用铁激活型D-荧光素FeAL-1在移植瘤模型和肝脏中进行体内.labile.铁的生物发光成像研究
Ryan L Gonciarz,Honglin Jiang,Linh Tram et al.
Ryan L Gonciarz et al.
Dysregulated iron homeostasis underlies diverse pathologies, from ischemia-reperfusion injury to epithelial-mesenchymal transition and drug-tolerant "persister" cancer cell states. Here, we introduce ferrous iron-activatable luciferin-1 (Fe...
An N terminomics toolbox combining 2-pyridinecarboxaldehyde probes and click chemistry for profiling protease specificity [0.03%]
一种结合2-吡啶甲醛探针和点击化学的N末端组学工具箱用于谱绘蛋白酶特异性
Haley N Bridge,William Leiter,Clara L Frazier et al.
Haley N Bridge et al.
Proteomic profiling of protease-generated N termini provides key insights into protease function and specificity. However, current technologies have sequence limitations or require specialized synthetic reagents for N-terminal peptide isola...
Targeting RNA with synthetic oligonucleotides: Clinical success invites new challenges [0.03%]
靶向RNA的合成寡核苷酸疗法：临床成功带来新挑战
Cristina R Hofman,David R Corey
Cristina R Hofman
Synthetic antisense oligonucleotides (ASOs) and duplex RNAs (dsRNAs) are an increasingly successful strategy for drug development. After a slow start, the pace of success has accelerated since the approval of Spinraza (nusinersen) in 2016 w...
Linqi Cheng,Yixian Wang,Yiming Guo et al.
Linqi Cheng et al.
Recent years have seen a remarkable growth in the field of protein-based medical treatments. Nevertheless, concerns have arisen regarding the cytotoxicity limitations, low affinity, potential immunogenicity, low stability, and challenges to...
A machine learning and live-cell imaging tool kit uncovers small molecules induced phospholipidosis [0.03%]
一个机器学习和活细胞成像工具包发现了诱导磷脂osis的小分子
Huabin Hu,Amelie Tjaden,Stefan Knapp et al.
Huabin Hu et al.
Drug-induced phospholipidosis (DIPL), characterized by excessive accumulation of phospholipids in lysosomes, can lead to clinical adverse effects. It may also alter phenotypic responses in functional studies using chemical probes. Therefore...
Targeting METTL3 reprograms the tumor microenvironment to improve cancer immunotherapy [0.03%]
靶向METTL3重编程肿瘤微环境以改善癌症免疫治疗
Haisheng Yu,Jing Liu,Xia Bu et al.
Haisheng Yu et al.
The tumor microenvironment (TME) is a heterogeneous ecosystem containing cancer cells, immune cells, stromal cells, cytokines, and chemokines which together govern tumor progression and response to immunotherapies. Methyltransferase-like 3 ...
Kivanç Birsoy,Navdeep S Chandel,Sarah-Maria Fendt et al.
Kivanç Birsoy et al.
Over the past decade or two, targeting metabolism has been effective in the treatment of many diseases and disorders, particularly cancer. In a metabolism focus issue in Cell Chemical Biology, this Voices piece asks researchers from a range...
Glutamine availability unleashes dendritic cells' anti-tumor power [0.03%]
谷氨酰胺通过解除代谢限制激发树突状细胞的抗肿瘤能力
Mauro Corrado,Christian Frezza
Mauro Corrado
Metabolic competition within the tumor microenvironment (TME) shapes the efficacy of anticancer immunity. In the August 3rd issue of Nature, Guo et al.1 show that glutamine is an intercellular metabolic checkpoint between cancer and immune ...
Repurposing SGLT2 inhibitors for autoimmune diseases? YES, WE MAY! [0.03%]
SGLT2抑制剂有望用于自身免疫性疾病吗？是的，可能！
Michelangelo Certo,Jennifer Niven,Claudio Mauro
Michelangelo Certo
T cells play a key role in driving autoimmunity, with alterations in metabolism powering their effector function. In the July 11 issue of Cell Metabolism, Jenkins et al.1 describe how a type 2 diabetes drug, canagliflozin, can be repurposed...