Bridget K Wagner,Mishtu Dey
Bridget K Wagner
Vanessa A Gutzeit,Amanda Acosta-Ruiz,Hermany Munguba et al.
Vanessa A Gutzeit et al.
Despite the power of photopharmacology for interrogating signaling proteins, many photopharmacological systems are limited by their efficiency, speed, or spectral properties. Here, we screen a library of azobenzene photoswitches and identif...
Scribble sub-cellular localization modulates recruitment of YES1 to regulate YAP1 phosphorylation [0.03%]
scribble亚细胞定位调控YES1招募以调节YAP1磷酸化
Dongyu Zhao,Zhangyuan Yin,Matthew B Soellner et al.
Dongyu Zhao et al.
The multi-domain scaffolding protein Scribble (Scrib) regulates cell polarity and growth signaling at cell-cell junctions. In epithelial cancers, Scrib mislocalization and overexpression paradoxically transform Scrib from a basolateral tumo...
Thermal proteome profiling identifies the membrane-bound purinergic receptor P2X4 as a target of the autophagy inhibitor indophagolin [0.03%]
热蛋白组分析鉴定出自主噬抑制剂吲哚酚林的作用靶点为膜结合嘌呤受体P2X4
Marjorie A Carnero Corrales,Sarah Zinken,Georgios Konstantinidis et al.
Marjorie A Carnero Corrales et al.
Signaling pathways are frequently activated through signal-receiving membrane proteins, and the discovery of small molecules targeting these receptors may yield insights into their biology. However, due to their intrinsic properties, membra...
Y box binding protein 1 inhibition as a targeted therapy for ovarian cancer [0.03%]
卵癌靶向治疗的新策略——Y盒结合蛋白1抑制作用
Dhanir Tailor,Angel Resendez,Fernando Jose Garcia-Marques et al.
Dhanir Tailor et al.
Y box binding protein 1 (YB-1) is a multifunctional protein associated with tumor progression and the emergence of treatment resistance (TR). Here, we report an azopodophyllotoxin small molecule, SU056, that potently inhibits tumor growth a...
HER2-targeted antibody-drug conjugate induces host immunity against cancer stem cells [0.03%]
抗HER2抗体药物缀合物可诱导机体针对癌症干细胞的免疫反应
Leiming Xia,Lu Wen,You Qin et al.
Leiming Xia et al.
We previously tested HER2-targeted antibody-drug conjugates (ADCs) in immunocompromised (SCID) mice, precluding evaluation of host immunity, impact on cancer stem cells (CSCs), and potential benefit when combined with PD-L1 blockade. In thi...
A potent and selective PARP14 inhibitor decreases protumor macrophage gene expression and elicits inflammatory responses in tumor explants [0.03%]
高效的PARP14抑制剂可降低促肿瘤巨噬细胞基因表达并诱发体外培养肿瘤组织的炎症反应
Laurie B Schenkel,Jennifer R Molina,Kerren K Swinger et al.
Laurie B Schenkel et al.
PARP14 has been implicated by genetic knockout studies to promote protumor macrophage polarization and suppress the antitumor inflammatory response due to its role in modulating interleukin-4 (IL-4) and interferon-γ signaling pathways. Her...
Multiple unbiased approaches identify oxidosqualene cyclase as the molecular target of a promising anti-leishmanial [0.03%]
多种无偏见的方法识别出氧化角鲨烯环化酶是具有前景的抗利什曼原生动物药物的作用靶点
Luciana S Paradela,Richard J Wall,Sandra Carvalho et al.
Luciana S Paradela et al.
Phenotypic screening identified a benzothiophene compound with activity against Leishmania donovani, the causative agent of visceral leishmaniasis. Using multiple orthogonal approaches, oxidosqualene cyclase (OSC), a key enzyme of sterol bi...
A synthetic small molecule stalls pre-mRNA splicing by promoting an early-stage U2AF2-RNA complex [0.03%]
一种合成的小分子通过促进早期阶段的U2AF2-RNA复合物来抑制前mRNA剪接
Rakesh Chatrikhi,Callen F Feeney,Mary J Pulvino et al.
Rakesh Chatrikhi et al.
Dysregulated pre-mRNA splicing is an emerging Achilles heel of cancers and myelodysplasias. To expand the currently limited portfolio of small-molecule drug leads, we screened for chemical modulators of the U2AF complex, which nucleates spl...
In-depth characterization of ubiquitin turnover in mammalian cells by fluorescence tracking [0.03%]
利用荧光追踪技术对哺乳动物细胞泛素周转的深入研究
Anna A Kudriaeva,Ido Livneh,Mikhail S Baranov et al.
Anna A Kudriaeva et al.
Despite almost 40 years having passed from the initial discovery of ubiquitin (Ub), fundamental questions related to its intracellular metabolism are still enigmatic. Here we utilized fluorescent tracking for monitoring ubiquitin turnover i...