Ionotropic and Metabotropic Mechanisms of Allosteric Modulation of α 7 Nicotinic Receptor Intracellular Calcium [0.03%]
α7烟碱受体胞内钙离子的别构调节的离子型和元基因组机制研究
Justin R King,Aman Ullah,Ellen Bak et al.
Justin R King et al.
The pharmacological targeting of the α7 nicotinic acetylcholine receptor (α7) is a promising strategy in the development of new drugs for neurologic diseases. Because α7 receptors regulate cellular calcium, we investigated how the protot...
GPR40-Mediated G α 12 Activation by Allosteric Full Agonists Highly Efficacious at Potentiating Glucose-Stimulated Insulin Secretion in Human Islets [0.03%]
allosteric全激动剂通过激活人类胰岛中GPR40的Gα12来高度有效地促进葡萄糖刺激的胰岛素分泌
Marie-Laure Rives,Brian Rady,Nadia Swanson et al.
Marie-Laure Rives et al.
GPR40 is a clinically validated molecular target for the treatment of diabetes. Many GPR40 agonists have been identified to date, with the partial agonist fasiglifam (TAK-875) reaching phase III clinical trials before its development was te...
Inhibition of CD45 Phosphatase Activity Induces Cell Cycle Arrest and Apoptosis of CD45+ Lymphoid Tumors Ex Vivo and In Vivo [0.03%]
抑制CD45磷酸酶活性诱发活体和离体实验中CD45+淋巴肿瘤细胞周期停止和凋亡
Michael Perron,H Uri Saragovi
Michael Perron
Src-family kinases (SFK) govern cellular proliferation of bone marrow-derived cells. SFKs are regulated by the protein tyrosine phosphatase enzymatic activity of CD45. All lymphoid cells express CD45, but only proliferating cells are depend...
Differential Pharmacology and Binding of mGlu2 Receptor Allosteric Modulators [0.03%]
mGlu2受体变构调节剂的药理学和结合差异性分析
Daniel E O&#x;Brien,Douglas M Shaw,Hyekyung P Cho et al.
Daniel E O&#x;Brien et al.
Allosteric modulation of metabotropic glutamate receptor 2 (mGlu2) has demonstrated efficacy in preclinical rodent models of several brain disorders, leading to industry and academic drug discovery efforts. Although the pharmacology and bin...
Mapping the Allosteric Action of Antagonists A740003 and A438079 Reveals a Role for the Left Flipper in Ligand Sensitivity at P2X7 Receptors [0.03%]
拮抗剂A740003和A438079的别构作用图谱揭示了P2X7受体上左翼状结构在配体敏感性中的作用
Rebecca C Allsopp,Sudad Dayl,Anfal Bin Dayel et al.
Rebecca C Allsopp et al.
P2X7 receptor (P2X7R) activation requires ∼100-fold higher concentrations of ATP than other P2X receptor (P2XR) subtypes. Such high levels are found during cellular stress, and P2X7Rs consequently contribute to a range of pathophysiologica...
Comparative Study
Molecular pharmacology. 2018 May;93(5):553-562. DOI:10.1124/mol.117.111021 2018
Cooperative Regulation of Intestinal UDP-Glucuronosyltransferases 1A8, -1A9, and 1A10 by CDX2 and HNF4 α Is Mediated by a Novel Composite Regulatory Element [0.03%]
CDX2和HNF4α通过一个新的复合型调控元件协同调节肠道UDP葡萄糖醛酸转移酶1A8、-1A9和-1A10
Nurul Mubarokah,Julie-Ann Hulin,Peter I Mackenzie et al.
Nurul Mubarokah et al.
The gastrointestinal tract expresses several UDP-glucuronosyltransferases (UGTs) that act as a first line of defense against dietary toxins and contribute to the metabolism of orally administered drugs. The expression of UGT1A8, UGT1A9, and...
The Novel C-terminal Truncated 90-kDa Isoform of Topoisomerase II α (TOP2 α/90) Is a Determinant of Etoposide Resistance in K562 Leukemia Cells via Heterodimerization with the TOP2 α/170 Isoform [0.03%]
拓扑异构酶IIα（TOP2α/90）的新截短型C端（170kDa形式）通过异二聚化决定K562白血病细胞的鬼臼毒素抗性
Ragu Kanagasabai,Soumendrakrishna Karmahapatra,Corey A Kientz et al.
Ragu Kanagasabai et al.
DNA topoisomerase IIα (170 kDa, TOP2α/170) is essential in proliferating cells by resolving DNA topological entanglements during chromosome condensation, replication, and segregation. We previously characterized a C-terminally truncated i...
"Selective" Class C G Protein-Coupled Receptor Modulators Are Neutral or Biased mGlu5 Allosteric Ligands [0.03%]
选择性G蛋白偶联受体调节剂是mGlu5的中立或偏向异构调节配体
Shane D Hellyer,Sabine Albold,Taide Wang et al.
Shane D Hellyer et al.
Numerous positive and negative allosteric modulators (PAMs and NAMs) of class C G protein-coupled receptors (GPCRs) have been developed as valuable preclinical pharmacologic tools and therapeutic agents. Although many class C GPCR allosteri...
Mary Vore
Mary Vore
Properties of Triheteromeric N-Methyl-d-Aspartate Receptors Containing Two Distinct GluN1 Isoforms [0.03%]
含有两种不同GluN1异构体的三聚N-甲基-D-天冬氨酸受体的特性
Feng Yi,Linda G Zachariassen,Katherine N Dorsett et al.
Feng Yi et al.
N-Methyl-d-aspartate (NMDA)-type glutamate receptors mediate excitatory synaptic transmission in the central nervous system and play critical roles in many neuronal processes. The physiologic roles of NMDA receptors are shaped by their func...