A covalent inhibitor targeting Cys16 on RhoA in colorectal cancer [0.03%]
一种靶向结直肠癌RhoA蛋白半胱氨酸16的共价抑制剂
Tin-Yan Koo,Jason Ying Ki Li,Nga-Sze Lee et al.
Tin-Yan Koo et al.
RhoA is a key cancer driver and potential colorectal cancer (CRC) therapy target but remains undrugged clinically. Using activity-based protein profiling (ABPP) and mass spectrometry (MS), we identified CL16, a covalent inhibitor targeting ...
A base editor facilitates simultaneous purine and pyrimidine substitutions for ex vivo and in vivo mutagenesis screens [0.03%]
一种碱基编辑器可同时实现嘌呤和嘧啶的替换用于体外和体内诱变筛选
Zhiyong He,Yuyang Xie,Honglin Huang et al.
Zhiyong He et al.
Genetic mutations are closely linked to human diseases, yet the relationship between many mutations and their corresponding phenotypes remains poorly understood. Furthermore, tools to study the connection between nucleotide variations and p...
Pharmacologic interrogation of USP28 cellular function in p53 signaling [0.03%]
探究USP28的药理功能在p53信号转导中的作用
Ariana S Bratt,Susan Kilgas,Maria I Tarazona Guzman et al.
Ariana S Bratt et al.
Deubiquitinating enzymes (DUBs) are crucial regulators of ubiquitin signaling and protein degradation that remain incompletely understood in part due to the lack of high-quality chemical probes. To address this challenge, we developed CAS-0...
Raffaella De Pace,Saikat Ghosh,Chad D Williamson et al.
Raffaella De Pace et al.
Endolysosomes are dynamic organelles that undergo movement along the cytoskeleton, fusion, fission, and tubulation during their lifetime. These processes are regulated by complex molecular machineries, including the structurally related het...
Inhibiting cancer metastasis with water-solubilized membrane receptor CXCR4QTY-Fc as a molecular trap [0.03%]
用水溶性膜受体CXCR4QTY-Fc抑制癌症转移作为分子陷阱
Changfa Sun,Shilei Hao,Lili Wang et al.
Changfa Sun et al.
The CXCR4/CXCL12 axis is vital for tumor metastasis and immune evasion in various cancers. However, developing effective inhibitors is challenging due to complex intracellular interactions and limitations of soluble receptor drugs targeting...
Engineering affinity-matured variants of an anti-polysialic acid monoclonal antibody with superior cytotoxicity-mediating potency [0.03%]
工程亲和成熟技术获得一类抗聚唾液酸单克隆抗体毒性的变异体
Weiyao Wang,Mehman Bunyatov,Deana Moffat et al.
Weiyao Wang et al.
Monoclonal antibodies (mAbs) that specifically recognize cell surface glycans associated with cancer and infectious disease hold tremendous value for basic research and clinical applications. However, high-quality anti-glycan mAbs with suff...
Targeting the MYC oncogene with a selective bi-steric mTORC1 inhibitor elicits tumor regression in MYC-driven cancers [0.03%]
一种选择性双作用mTORC1抑制剂通过靶向MYC原癌基因诱导由MYC驱动的癌症消退
Wadie D Mahauad-Fernandez,Yu Chi Yang,Ian Lai et al.
Wadie D Mahauad-Fernandez et al.
The MYC oncogene is causally involved in the pathogenesis of most human cancers. The mTORC1 complex regulates MYC translation through 4EBP1 and S6K. However, agents that selectively target mTORC1 (without affecting mTORC2) have so far faile...
Robust antitumor treatment driven by lock-and-key biorecognition of dynamic cyclic diselenide-guided chiral prodrug self-assembly [0.03%]
动态环状二硒化物引导的手性前药自组装的锁钥生物识别引起的稳健抗肿瘤治疗
Yixin Sun,Baoyuan Zhang,Jiayao Wang et al.
Yixin Sun et al.
Designing highly selective nanomedicines with precise recognition of biological interfaces for efficient cancer therapy represents a tremendous challenge. Inspired by the inherent chirality and enantioselectivity of organisms, we constructe...
An adjuvant database for preclinical evaluation of vaccines and immunotherapeutics [0.03%]
疫苗和免疫疗法的临床前评估辅助数据库
Yayoi Natsume-Kitatani,Kouji Kobiyama,Yoshinobu Igarashi et al.
Yayoi Natsume-Kitatani et al.
Adjuvants are immunostimulators used to enhance vaccine efficacy against infectious diseases. However, current methods for evaluating their efficacy and safety are limited, hindering large-scale screening. To address this, we developed a pr...
A method for the detection and enrichment of endogenous cereblon substrates [0.03%]
一种内源性环孢菌素底物的检测和浓缩方法
Hannah C Lloyd,Yuli Li,N Connor Payne et al.
Hannah C Lloyd et al.
C-terminal cyclic imides are posttranslational modifications (PTMs) on proteins that are recognized and removed by the E3 ligase substrate adapter cereblon (CRBN). Despite the observation of these modifications across the proteome by mass s...