N- Acyl Amino Acids (Elmiric Acids): Endogenous Signaling Molecules with Therapeutic Potential [0.03%]
N-酰基氨基酸（elmiric酸）：具有治疗潜力的内源性信号分子
Sumner H Burstein
Sumner H Burstein
The subject of N-acyl amino acid conjugates has been rapidly growing in recent years, especially with regard to their analgesic and anti-inflammatory actions. The field comprises a large family of lipid signaling molecules whose importance ...
Correction to "Novel Small Molecule JP-153 Targets the Src-FAK-Paxillin Signaling Complex to Inhibit VEGF-Induced Retinal Angiogenesis" [0.03%]
关于“新型小分子JP-153靶向Src-FAK-Paxillin信号复合物以抑制VEGF诱导的视网膜新生血管形成”的更正通知
Published Erratum
Molecular pharmacology. 2017 Dec;92(6):627. DOI:10.1124/mol.116.105031err 2017
Peter O Oladimeji,Taosheng Chen
Peter O Oladimeji
Pregnane X receptor (PXR) is a nuclear receptor considered to be a master xenobiotic receptor that coordinately regulates the expression of genes encoding drug-metabolizing enzymes and drug transporters to essentially detoxify and eliminate...
Desensitization and Tolerance of Mu Opioid Receptors on Pontine Kölliker-Fuse Neurons [0.03%]
作用于脑桥Kölliker-Fuse核的μ阿片受体的脱敏和耐受性
Erica S Levitt,John T Williams
Erica S Levitt
Acute desensitization of mu opioid receptors is thought to be an initial step in the development of tolerance to opioids. Given the resistance of the respiratory system to develop tolerance, desensitization of neurons in the Kölliker-Fuse ...
The X-Ray Crystal Structure of the Human Mono-Oxygenase Cytochrome P450 3A5-Ritonavir Complex Reveals Active Site Differences between P450s 3A4 and 3A5 [0.03%]
人单加氧酶细胞色素P450 3A5-ritonavir复介的X射线晶体结构揭示了P450s 3A4和3A5的作用位点差异
Mei-Hui Hsu,Uzen Savas,Eric F Johnson
Mei-Hui Hsu
The contributions of cytochrome P450 3A5 to the metabolic clearance of marketed drugs is unclear, but its probable role is to augment the metabolism of several drugs that are largely cleared by P450 3A4. Selective metabolism by 3A4 is often...
Structural Determinants Influencing the Potency and Selectivity of Indazole-Paroxetine Hybrid G Protein-Coupled Receptor Kinase 2 Inhibitors [0.03%]
影响吲达唑帕罗西杂合G蛋白偶联受体激酶2抑制剂活性和选择性的结构决定因素
Renee Bouley,Helen V Waldschmidt,M Claire Cato et al.
Renee Bouley et al.
G protein-coupled receptor kinases (GRKs) phosphorylate activated receptors to promote arrestin binding, decoupling from heterotrimeric G proteins, and internalization. GRK2 and GRK5 are overexpressed in the failing heart and thus have beco...
Relationship between DNA Methylation in the 5' CpG Island of the SLC47A1 (Multidrug and Toxin Extrusion Protein MATE1) Gene and Interindividual Variability in MATE1 Expression in the Human Liver [0.03%]
人肝SLC47A1（多药和毒素外排蛋白MATE1）基因5' CpG岛甲基化与个体间MATE1表达差异相关性研究
Toshihiro Tanaka,Takeshi Hirota,Ichiro Ieiri
Toshihiro Tanaka
Multidrug and toxin extrusion protein 1 (MATE1), which is encoded by solute carrier 47A1 (SLC47A1), mediates the excretion of organic cations into bile and urine. Some genetic variants in human MATE1 altered its transport function in in vit...
Evaluation of the Selectivity and Cysteine Dependence of Inhibitors across the Regulator of G Protein-Signaling Family [0.03%]
评估_Regulator_of_G_protein_信号家族抑制剂的选择性和半胱氨酸依赖性
Michael P Hayes,Christopher R Bodle,David L Roman
Michael P Hayes
Since their discovery more than 20 years ago, regulators of G protein-signaling (RGS) proteins have received considerable attention as potential drug targets because of their ability to modulate Gα activity. Efforts to identify small molec...