RUVBL1/RUVBL2 ATPase Activity Drives PAQosome Maturation, DNA Replication and Radioresistance in Lung Cancer [0.03%]
RUVBL1/RUVBL2 ATP酶活性驱动肺癌PAQosome成熟、DNA复制和放射抵抗作用
Paul Yenerall,Amit K Das,Shan Wang et al.
Paul Yenerall et al.
RUVBL1 and RUVBL2 (collectively RUVBL1/2) are essential AAA+ ATPases that function as co-chaperones and have been implicated in cancer. Here we investigated the molecular and phenotypic role of RUVBL1/2 ATPase activity in non-small cell lun...
Mei Zeng,Yuan Xiong,Nozhat Safaee et al.
Mei Zeng et al.
KRAS is the most frequently mutated oncogene found in pancreatic, colorectal, and lung cancers. Although it has been challenging to identify targeted therapies for cancers harboring KRAS mutations, KRASG12C can be targeted by small-molecule...
Aptamers as Reversible Sorting Ligands for Preparation of Cells in Their Native State [0.03%]
适配子作为可逆分拣配体用于制备天然状态的细胞
Bethany Powell Gray,Martin D Requena,Michael D Nichols et al.
Bethany Powell Gray et al.
Although antibodies are routinely used to label and isolate a desired cell type from a more complex mixture of cells, via either fluorescence-activated cell sorting (FACS) or magnetic-activated cell sorting (MACS), such antibody labeling is...
Discovery of an AKT Degrader with Prolonged Inhibition of Downstream Signaling [0.03%]
一种长效抑制下游信号的AKT降解剂的发现
Inchul You,Emily C Erickson,Katherine A Donovan et al.
Inchul You et al.
The PI3K/AKT signaling cascade is one of the most commonly dysregulated pathways in cancer, with over half of tumors exhibiting aberrant AKT activation. Although potent small-molecule AKT inhibitors have entered clinical trials, robust and ...
Sunil Mathur,Adam J Fletcher,Emma Branigan et al.
Sunil Mathur et al.
Activity-based protein profiling is an invaluable technique for studying enzyme biology and facilitating the development of therapeutics. Ubiquitin E3 ligases (E3s) are one of the largest enzyme families and regulate a host of (patho)physio...
Marcus J C Long,Yi Zhao,Yimon Aye
Marcus J C Long
Ribonucleotide reductase (RNR) is an essential enzyme in DNA biogenesis and a target of several chemotherapeutics. Here, we investigate how anti-leukemic drugs (e.g., clofarabine [ClF]) that target one of the two subunits of RNR, RNR-α, af...
A Systems Chemoproteomic Analysis of Acyl-CoA/Protein Interaction Networks [0.03%]
酰基辅酶a/蛋白质互作网络的化学蛋白组学分析
Michaella J Levy,David C Montgomery,Mihaela E Sardiu et al.
Michaella J Levy et al.
Acyl-coenzyme A (CoA)/protein interactions are essential for life. Despite this importance, their global scope and selectivity remains undefined. Here, we describe CATNIP (CoA/AcetylTraNsferase Interaction Profiling), a chemoproteomic platf...
A Strategic Approach for Fluorescence Imaging of Membrane Proteins in a Native-like Environment [0.03%]
原生环境下膜蛋白荧光成像的战略方法研究
Jean-Marie Swiecicki,Jordan Tyler Santana,Barbara Imperiali
Jean-Marie Swiecicki
Biological membranes are complex barriers in which membrane proteins and thousands of lipidic species participate in structural and functional interactions. Developing a strategic approach that allows uniform labeling of membrane proteins w...
Degradation of Polycomb Repressive Complex 2 with an EED-Targeted Bivalent Chemical Degrader [0.03%]
一种靶向EED的双价化学降解剂对PRC2复合体的降解作用
Frances Potjewyd,Anne-Marie W Turner,Joshua Beri et al.
Frances Potjewyd et al.
Protein degradation via the use of bivalent chemical degraders provides an alternative strategy to block protein function and assess the biological roles of putative drug targets. This approach capitalizes on the advantages of small-molecul...
Combining Stage Specificity and Metabolomic Profiling to Advance Antimalarial Drug Discovery [0.03%]
结合分期特异性和代谢组学谱型促进抗疟新药发现
James M Murithi,Edward S Owen,Eva S Istvan et al.
James M Murithi et al.
We report detailed susceptibility profiling of asexual blood stages of the malaria parasite Plasmodium falciparum to clinical and experimental antimalarials, combined with metabolomic fingerprinting. Results revealed a variety of stage-spec...