Sunvozertinib (Zegfrovy): an oral EGFR inhibitor that irreversibly targets exon20ins in NSCLC [0.03%]
sunvozertinib（泽弗鲁替尼）：一种不可逆靶向NSCLC患者EGFR exon20插入突变的口服抑制剂
Xiaoshuang Niu,Wenshan Zhao,Bin Yu
Xiaoshuang Niu
Yuxi Wang,Cuiyu Guo,Weimin Li
Yuxi Wang
Antibody-drug conjugates (ADCs) offer a promising approach for targeted cancer treatment. Progress, however, is constrained by the combinatorial complexity of design, toxicity and side effects, and variable clinical benefit across indicatio...
Ningyang Xu,Edwin Legall,Roger H Johnson et al.
Ningyang Xu et al.
Biased signaling by G protein-coupled receptors (GPCRs) occurs when ligands selectively activate G proteins or β-arrestins, offering therapeutic potential with fewer side effects. In class A GPCRs, which include the targets of approximatel...
Pierre-André Lafon,Laurent Prézeau,Jean-Philippe Pin et al.
Pierre-André Lafon et al.
Camelid-derived nanobodies offer a promising alternative to conventional antibodies for the treatment of brain disorders. Their current development in models of schizophrenia or Alzheimer's disease highlights their strong therapeutic potent...
Discovering next-generation dopamine transporter drugs with lower abuse potential [0.03%]
发现具有较低滥用倾向的下一代多巴胺转运体药物
Ding Luo,Zerong Liu,Weiwei Xue
Ding Luo
Many traditional psychostimulants used to treat neuropsychiatric disorders by targeting the dopamine transporter (DAT) exhibit a high potential of abuse. This necessitates the development of next-generation drugs with improved safety. Disco...
Targeting BRD4 bromodomains and beyond: exploring new therapeutic frontiers [0.03%]
靶向BRD4溴结构域及其它：探索新的治疗前沿方向
Wenju Zhang,Yumei Li,Ming-Ming Zhou et al.
Wenju Zhang et al.
Bromodomain-containing protein 4 (BRD4) is a key transcriptional regulator in the bromodomain and extraterminal (BET) family. It promotes cancer and inflammation by binding to chromatin through its bromodomains. Although bromodomain inhibit...
Next-generation isoform-selective fibroblast growth factor receptor inhibitors [0.03%]
下一代同种型选择性成纤维细胞生长因子受体抑制剂
Lingfeng Chen
Lingfeng Chen
Dysregulated fibroblast growth factor receptor (FGFR) signaling - driven by amplifications, mutations, or fusions - represents a clinically validated oncogenic driver across diverse malignancies. Pan-FGFR-selective inhibitors (erdafitinib, ...
WEE-family kinases in cancer: synthetic lethal interactions and drug discovery [0.03%]
wee-家族激酶在癌症中的作用：合成致死相互作用和药物发现
Chaofan Wang,Xiaoyun Lu
Chaofan Wang
The WEE-family kinases, WEE1 and PKMYT1, play critical roles in regulating the G2/M cell cycle checkpoint to maintain genomic stability. Cancer cells with DNA damage response (DDR) deficiencies become heavily reliant on WEE1 and PKMYT1 to a...
Targeting SARM1: from inhibition for neuroprotection to activation for neuroablation [0.03%]
靶向SARM1：从抑制神经保护到激活神经消融
Peter Arthur-Farraj,Andrea Loreto
Peter Arthur-Farraj
Sterile alpha and TIR motif-containing protein 1 (SARM1),is a central enzyme that drives programmed axon degeneration and has gathered significant interest as a therapeutic target. Despite preclinical development of inhibitory therapeutic a...
Dennis-Dominik Rosmus,Bahareh Ajami
Dennis-Dominik Rosmus
Neurodegeneration arises from malfunctional intercellular interactions within the central nervous system (CNS). In a recent study, Frosch et al. identified a microglia-neuron enzyme delivery system the dysfunction of which drives Sandhoff d...