Potentiation of GPCR signaling by ATP and sugar monophosphates [0.03%]
ATP和单糖一磷酸盐通过激活腺苷酸环化酶和调节G蛋白γ亚基正向调控GPCR信号转导
Sam R J Hoare
Sam R J Hoare
Allosteric potentiation of G protein-coupled receptor (GPCR) signaling provides new opportunities for therapeutic discovery. Recently, the laboratory of Peter Chidiac has reported strong allosteric potentiation of numerous GPCRs by extracel...
Danicopan: complement factor D inhibitor for paroxysmal nocturnal hemoglobinuria [0.03%]
丹尼波普安：阵发性夜间血红蛋白尿的补体因子D抑制剂
Ekaterina Umnyakova,Alexander J Lander,Daniel Ricklin
Ekaterina Umnyakova
Qiang Zhu,Xiaoming Chen,Xiaotao Duan et al.
Qiang Zhu et al.
Glycans are complex sugar modifications found on cell surfaces that play crucial roles in biological processes. Glycosylation patterns are aberrantly altered in the tumor microenvironment (TME), which helps cancer cells escape immune survei...
Hongyan Jing,Xi Zhang,Linghua Meng
Hongyan Jing
SWI/SNF chromatin remodeling complexes are essential epigenetic regulators that control chromatin accessibility and transcriptional programs. Alterations in SWI/SNF components are common across a wide spectrum of human cancers, driving tumo...
Taoqian Zhao,Achi Haider,Steven H Liang
Taoqian Zhao
Therapeutic potential of targeting macrophages and microglia in glioblastoma [0.03%]
靶向胶质母细胞瘤巨噬细胞和小胶质细胞的治疗潜力
Fei Zhou,Pritha Mukherjee,Jinming Mu et al.
Fei Zhou et al.
Glioblastoma (GBM) is a highly aggressive and lethal form of brain tumor in human adults that resists standard of care (SOC) and immunotherapy. Tumor-associated macrophages and microglia (TAMs) represent the most abundant cell population wi...
Kian Noorman van der Dussen,Willem Jespers
Kian Noorman van der Dussen
G proteins, members of the GTPase superfamily, are central mediators of signal transduction downstream of G protein-coupled receptors (GPCRs). Despite their critical roles in normal physiology and the high intrinsic affinity for endogenous ...
Simone Giovannuzzi,Claudiu T Supuran
Simone Giovannuzzi
Human carbonic anhydrases (hCAs) are a superfamily of metalloenzymes with considerable, though yet poorly exploited therapeutic potential. They were primarily implicated in ocular and renal diseases and are targeted by antiglaucoma and diur...
Ren-Lei Ji,Zhe Wang,Jean J Zhao
Ren-Lei Ji
Biased G-protein-coupled receptor (GPCR) signaling is reshaping drug discovery by enabling pathway-selective drug action. Recent work by Motso et al. identified GPCR kinase 2 (GRK2) as a non-canonical transducer, independent of G proteins o...
David L Roman
David L Roman
In most drug discovery efforts targeting regulator of G-protein signaling (RGS) proteins, inhibiting their activity is the end-goal. A recent article by Aryal et al. presents a novel strategy to stabilize RGS2 by blocking its degradation vi...