Moira Cornell,Smita Yadav
Moira Cornell
Pseudokinases are enigmatic proteins that evolved such that they retained the evolutionarily conserved kinase-like fold but lost key residues required for substrate phosphorylation. Pseudokinases have unique functions ranging from altered e...
Loss of α-cell GRK2 modulates glucagon response and supports cardiac function [0.03%]
α细胞GRK2丢失调节胰高血糖素反应并支持心脏功能
Jonathan Snyder,Lilly Underwood,Chun-Sun Jiang et al.
Jonathan Snyder et al.
Pancreatic α-cells secrete glucagon to maintain glucose homeostasis, yet the molecular mechanisms regulating hormone release are understudied. G-protein coupled receptor kinases (GRKs) regulate receptor desensitization; however, their role...
Extracellular domain-dependent modulation of class B1 G-protein-coupled receptor signaling [0.03%]
依赖于细胞外结构域的C类G蛋白偶联受体信号转导的调节
Alex D White,Leah R Padgett,Francis S Willard
Alex D White
The class B1 subfamily of G-protein-coupled receptors (GPCRs) comprises 15 members that respond to endogenous peptides to regulate an array of important physiological processes. Activation by peptide ligands is considered to follow a 2-step...
Meredith A Skiba
Meredith A Skiba
Once considered tools to aid structural studies, single-domain antibodies (nanobodies) have emerged as a new class of G protein-coupled receptor (GPCR) ligands. Aided by camelid immunization and advances in synthetic nanobody library develo...
Differential impacts of exon 1-associated and exon 11-associated variants of the rat mu opioid receptor gene, Oprm1, on buprenorphine- and morphine-induced analgesia and respiratory depression in male rats [0.03%]
大鼠μ阿片受体基因(Oprm1)外显子1相关变异和外显子11相关变异对雄性大鼠布托菲诺和吗啡诱导痛觉缺失及呼吸抑制的差异影响
Tiffany Zhang,Jin Xu,Valerie P Le Rouzic et al.
Tiffany Zhang et al.
Buprenorphine has long been recognized as a mu opioid agonist with a distinctive and intricate pharmacological profile. It is a partial agonist at the mu opioid receptor, an antagonist at the kappa and delta opioid receptors, and an agonist...
Cepharanthine, a valuable sanative alternative for hepatocellular carcinoma through regulating Hippo-Yes-associated protein signal transduction [0.03%]
喜马拉雅独参汤通过调节Hippo-YAP信号通路对肝癌的治疗作用
Kejun Hu,Yukai Zhao,Xinyu Fu et al.
Kejun Hu et al.
Hepatocellular carcinoma (HCC) stands as a prevalent form of primary liver cancer, distinguished by challenging diagnosis and grim prognoses. Its global mortality rate is on the rise, compounded by the insensitivity of patients with HCC to ...
UCM-A86 is a selective positive allosteric modulator of GluN1/GluN3 NMDA receptors [0.03%]
UCM-A86是一种选择性的GluN1/GluN3型N-甲基-D天冬氨酸受体正向变构调节剂
Avery J Benton,Mia R Johns,Emil Diamant et al.
Avery J Benton et al.
NMDA receptors are ionotropic glutamate receptors that mediate excitatory neurotransmission in the central nervous system where they play critical roles in normal and pathological brain functions and neurodevelopment. Glutamate/glycine-acti...
Cannabinoid receptor 2 activating antibodies: A promising therapeutic strategy for macrophage-driven fibro-inflammatory diseases [0.03%]
激活大麻素受体2的抗体：巨噬细胞驱动的纤维炎症性疾病的潜在治疗策略
Raghavender Reddy Gopireddy,Dipankar Bhattacharya,Swastik Sen et al.
Raghavender Reddy Gopireddy et al.
Fibrotic diseases, often fueled by chronic inflammation, represent a major unmet medical need. A critical driver of this process is the activation of macrophages, which secrete pro-inflammatory cytokines and chemokines, leading to immune ce...
A subunit-selective negative allosteric modulator of GluN1/GluN3A glycine-activated receptor [0.03%]
选择性甘氨酸激活的GluN1/GluN3A NMDA受体变构抑制剂
Leon Jacobs,TrangKimberly T Nguyen,Adam McCallum et al.
Leon Jacobs et al.
The ionotropic glutamate N-methyl-d-aspartate (NMDA) receptor gene family includes 7 homologous subunits (GluN1, GluN2A-D, and GluN3A-B). The coassembly of GluN1 and GluN2 form the well-studied NMDA receptor, which requires binding of both ...
Sadikshya Aryal,John J G Tesmer,Carmen W Dessauer et al.
Sadikshya Aryal et al.
Membrane-bound adenylyl cyclases (ACs) function as vital enzymes that convert external signals into intracellular responses through the second messenger cAMP. Traditionally viewed as monomers, ACs are now recognized to form oligomers, intro...