Side-by-Side Comparison of Different Thiol Bioconjugation Strategies for the Chemoselective Radiolabeling of Human Serum Albumin with Zirconium-89 [0.03%]
用于人血清白蛋白放射性标记的不同的硫醇生物连接策略的对比研究
Julia Kronberger,Barbora Neuzilova,Anja Federa et al.
Julia Kronberger et al.
Different bioconjugation strategies are available for the cysteine (Cys)-specific functionalization of proteins with different payloads, including imaging probes and (pro-)-drugs. Most commonly applied linkers include maleimides (mal); howe...
Advancements in Technologies Targeting Horizontal Gene TransferRoutes to Control Drug Resistance Evolution [0.03%]
针对水平基因转移的技术攻关——控制药物抗性进化的途径
Samuel Chetachukwu Adegoke,Md Adnan Karim,Maurelio Cabo Jr et al.
Samuel Chetachukwu Adegoke et al.
The global rise of multidrug-resistant (MDR) bacteria poses a major public health crisis, threatening the effectiveness of modern medicine. Traditional antibiotic development struggles to keep pace with bacterial evolution, largely due to t...
Proton Transfer Mechanisms in the MmpL3 Transporter of Mycobacterium tuberculosis Studied by Computer Simulations [0.03%]
计算机模拟研究结核分枝杆菌MmpL3转运蛋白中的质子转移机制
Yong-Sok Lee,Sergio A Hassan,Darrell E Hurt
Yong-Sok Lee
The mycobacterial membrane exporter MmpL3 transports trehalose monomycolates (TMM) from the cytosol to the outer membrane of Mycobacterium tuberculosis, making it a potential drug target. Proton influx is believed to drive TMM efflux, sugge...
Carborane Hydrophobic Tags Drive Selective Degradation of Endogenous KRASG12C via HSP70-Ubiquitin-Proteasome Pathway [0.03%]
碳硼烷疏水标记物通过HSP70-泛素-蛋白酶体途径驱动内源性KRASG12C的选择性降解
Yujie Shao,Kazuki Miura,Hiroyuki Nakamura
Yujie Shao
Persistent activation of the Kirsten rat sarcoma viral oncogene homologue (KRAS)G12C mutation sustains oncogenic signaling, and covalent inhibitors often yield incomplete pathway suppression or resistance. Herein, we developed hydrophobic-t...
Encapsulation of Exosomal Volatile Organic Compounds for Modulating the NF-κB Pathway in Monocytes [0.03%]
外泌体挥发性有机化合物的封装在单核细胞中调节NF-κB通路中的作用
Dina Hashoul,Rand Shibel,Haya Dahamshy-Silawi et al.
Dina Hashoul et al.
Cytokines communicate and coordinate immunity, allowing the immune cells to understand one another. Aside from cytokines, a wide variety of molecules modify immune cell behavior and immune responses. We present a study of volatile organic c...
Combining Topography and Chemistry toward Polydopamine Antibacterial Surfaces [0.03%]
结合拓扑和化学制备聚多巴胺抗菌表面
Leonardo Moscolari,Simona Tomaselli,Francesco Galeotti et al.
Leonardo Moscolari et al.
Microporous antibacterial surfaces offer a promising route for preventing bacterial adhesion and biofilm formation, yet their fabrication often involves complex and energy consuming processes. In this work, we present a sustainable strategy...
Discovery of N‑Acylhydrazone Derivatives as ROCK Inhibitors: A Journey from Virtual Screening and Structure-Based De Novo Design to the Identification of ROCK2 Selective Inhibitors and Beyond [0.03%]
ROCK抑制剂的发现：从虚拟筛选和基于结构的从头设计，到选择性ROCK2抑制剂及其他成果
Pedro de Sena Murteira Pinheiro,Lucas Silva Franco,Raysa Magali Pillpe-Meza et al.
Pedro de Sena Murteira Pinheiro et al.
Rho-associated coiled-coil containing kinases (ROCK1 and ROCK2) are central regulators of actin cytoskeleton organization and cell contractility under physiological conditions. Dysregulation of ROCK signaling contributes to aberrant cell mi...
Christian M Matter,Amedeo Caflisch
Christian M Matter
Transformers are machine learning models originally developed to translate between natural languages. Recently, a transformer model was trained on knowledge of medicinal chemistry, i.e., matched molecular pairs of nearly a million bioactive...
Pyrazolylpyrimidinamines Decorated via Petasis Reaction as Small-Molecule Activators of the RNA-Degrading Ribonuclease IRE1α [0.03%]
通过Petasis反应装饰的吡唑基嘧啶胺类小分子活化RNA降解内切酶IRE1α
Amrutha K Avathan Veettil,Yang Liu,Leon Wagner et al.
Amrutha K Avathan Veettil et al.
The multicomponent Petasis boron-Mannich reaction (PR) enables the generation of functionalized amines that are of biological interest. Here, we demonstrated that a series of pyrazolylpyrimidinamines decorated via PR are new small-molecule ...
Discovery of Small-Molecule Antagonists of PHF1 and 19 Demonstrates the Ligandability of PRC2 Accessory Proteins [0.03%]
小分子PHF1和PHF19拮抗剂的发现展示了PRC2辅助蛋白的配体结合能力
Isabelle E Amick,Rebecca L Johnson,Jiuyang Liu et al.
Isabelle E Amick et al.
PHF1 and PHF19 are key accessory components of polycomb repressive complex 2 (PRC2) which is responsible for trimethylation at histone H3 lysine 27, ultimately leading to gene repression. PHF1 and 19 are known for their methyl-lysine reader...