Emma Gebauer,Markus A Seeliger
Emma Gebauer
In this issue of Cell Chemical Biology, Chakraborty et al.1 employ a deep mutational screening analysis of 3,500 single point mutations in every residue in Src kinase's catalytic domain to determine which residues are critical for conferrin...
Cellular reprogramming by protein degradation: The next frontier in cancer immunotherapy [0.03%]
通过蛋白降解的细胞重编程:癌症免疫治疗的下一片疆土
Erik Ehinger,Anjana Rao
Erik Ehinger
In this issue of Cell Chemical Biology, Lane et al.1 introduce a transgene-based system to express fusion proteins that recruit transcription factors to E3 ligases. This approach expands the target repertoire for engineered cell therapies a...
Deguang Liang,Xuejun Jiang
Deguang Liang
In this issue of Cell Chemical Biology, Rodencal et al.1 report that cell-cycle arrest by p53 stabilizers or CDK4/6 inhibitors (CDK4/6i) can lead to phospholipid remodeling and hence sensitize cancer cells to GPX4 inhibitor (GPX4i)-triggere...
Meet the authors: Cydney N. Johnson, Shyra Wilde, Elaine Tuomanen, and Jason W. Rosch [0.03%]
作者简介:Cydney N. Johnson, Shyra Wilde, Elaine Tuomanen 和 Jason W. Rosch
Cydney N Johnson,Shyra Wilde,Elaine Tuomanen et al.
Cydney N Johnson et al.
In an interview with Samantha Nelson, a scientific editor for Cell Chemical Biology, the authors of the review entitled "Convergent impact of vaccination and antibiotic pressures on pneumococcal populations" share their perspectives on life...
Identification of differential biological activity and synergy between the PARP inhibitor rucaparib and its major metabolite [0.03%]
PARP抑制剂鲁卡帕利及其主要代谢物的生物活性差异和协同作用的识别
Huabin Hu,Carme Serra,Wenjie Zhang et al.
Huabin Hu et al.
The (poly)pharmacology of drug metabolites is seldom comprehensively characterized in drug discovery. However, some drug metabolites can reach high plasma concentrations and display in vivo activity. Here, we use computational and experimen...
The cyclimids: Degron-inspired cereblon binders for targeted protein degradation [0.03%]
环基酰亚胺类化合物:受Degron启发的cereblon结合物用于靶向蛋白质降解
Saki Ichikawa,N Connor Payne,Wenqing Xu et al.
Saki Ichikawa et al.
Cereblon (CRBN) is an E3 ligase substrate adapter widely exploited for targeted protein degradation (TPD) strategies. However, achieving efficient and selective target degradation is a preeminent challenge with ligands that engage CRBN. Her...
Anti-tumor immunotherapy using engineered bacterial outer membrane vesicles fused to lysosome-targeting chimeras mediated by transferrin receptor [0.03%]
通过转铁蛋白受体介导的工程细菌外膜囊泡与溶酶体靶向嵌合体融合的抗肿瘤免疫疗法
Ling-Yan Su,Yang Tian,Qiang Zheng et al.
Ling-Yan Su et al.
The lysosome-targeting chimera (LYTAC) approach has shown promise for the targeted degradation of secreted and membrane proteins via lysosomes. However, there have been challenges in design, development, and targeting. Here, we have designe...
Identification and characterization of a potent and selective HUNK inhibitor for treatment of HER2+ breast cancer [0.03%]
HER2阳性乳腺癌治疗中强力且特异的HUNK抑制剂的鉴定与特征分析
Tinslee Dilday,Melissa Abt,Nicole Ramos-Solís et al.
Tinslee Dilday et al.
Human epidermal growth factor receptor 2 (HER2)-targeted agents have proven to be effective, however, the development of resistance to these agents has become an obstacle in treating HER2+ breast cancer. Evidence implicates HUNK as an anti-...
Beyond antibiotic resistance: The whiB7 transcription factor coordinates an adaptive response to alanine starvation in mycobacteria [0.03%]
超越抗生素耐药性:whiB7转录因子协调分枝杆菌对丙氨酸饥饿的适应性反应
Nicholas C Poulton,Michael A DeJesus,Vanisha Munsamy-Govender et al.
Nicholas C Poulton et al.
Pathogenic mycobacteria are a significant cause of morbidity and mortality worldwide. The conserved whiB7 stress response reduces the effectiveness of antibiotic therapy by activating several intrinsic antibiotic resistance mechanisms. Desp...
PARP trapping is governed by the PARP inhibitor dissociation rate constant [0.03%]
PARP捕获由PARP抑制剂解离速率常数控制
Angelica A Gopal,Bianca Fernandez,Justin Delano et al.
Angelica A Gopal et al.
Poly(ADP-ribose) polymerase (PARP) inhibitors (PARPi) are a class of cancer drugs that enzymatically inhibit PARP activity at sites of DNA damage. Yet, PARPi function mainly by trapping PARP1 onto DNA with a wide range of potency among the ...