摘要：【关键词】 Mechanism 6-((2-(Dimethylamino)ethyl)amino)-3-hydroxy-7H-indeno(2,1-c)-quinolin-7-one dihydrochloride (TAS-103) is a quinoline derivative that displays antitumor activity in murine a...

摘要：【关键词】 Direct Streptozotocin (STZ) is a diabetogenic agent extensively used to induce diabetes and to study complications including diabetic peripheral neuropathy (DPN)。[Abstract/Free Full...

摘要：【关键词】 Novel KCNQ2 (Kv7。 In the present study, we have identified the compound N-(6-chloro-pyridin-3-yl)-3,4-difluoro-benzamide (ICA-27243) as a selective activator of the neuronal M curre...

摘要：【关键词】 Modulation Dehydroepiandrosterone (DHEA), a C19 human adrenal steroid, activates peroxisome proliferator-activated receptor (PPAR) in vivo but does not ligand-activate PPAR in transi...

摘要：【关键词】 Atomic The GABAA receptor is a chloride-selective ligand-gated ion channel of the Cys-loop superfamily。 Barrera NP, Herbert P, Henderson RM, Martin IL, and Edw...

摘要：【关键词】 State- Ranolazine is an antianginal agent that targets a number of ion channels in the heart, including cardiac voltage-gated Na+ channels。 However, ranolazine block of muscle and n...

摘要：【关键词】 Breast Breast cancer resistance protein (BCRP) is most abundantly expressed in the apical membrane of placental syncytiotrophoblasts, suggesting that it may protect the fetus by impe...

摘要：【关键词】 Insulin-Like The initial event upon binding of insulin-like growth factor 1 to the insulin-like growth factor type-I receptor (IGF-1R) is auto-phosphorylation of tyrosine residues wi...

摘要：【关键词】 Novel Aberrant gene expression is one of the driving forces for cancer progression and is considered an ideal target for chemical intervention。 High-Throughput Compound Screening。M...

摘要：It is interesting that a structurally distinct PAM, N-{4-Chloro-2-[(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)methyl]phenyl}-2-hydroxybenzamide (CPPHA), does not to bind to the MPEP site。 Three disti...

摘要：【关键词】 Identification Steroidogenic factor SF-1, a constitutively active nuclear hormone receptor, is essential to the development of adrenal and gonadal glands and acts as a shaping factor...

摘要：【关键词】 Identification The retinoid-related orphan receptors (RORs) and liver X receptors (LXRs) were postulated to have distinct functions。 RORs play a role in tissue development and circa...

摘要：Lipid action at the nAChR thus involves more than a simple modulation of the equilibrium between resting and desensitized states。 Drug action at the nAChR and possibly other neurotransmitter recep...

摘要：【关键词】 Plasticity Adaptations to long-term morphine treatment resulting in tolerance are protective by counteracting the consequences of sustained opioid receptor activation。[Med...

摘要：【关键词】 Intracellular A novel mechanism for antagonism of the human chemokine receptors CCR4 and CCR5 has been discovered with a series of small-molecule compounds that seems to interact wit...

摘要：【关键词】 Progesterone Breast cancer resistance protein (BCRP) plays a significant role in drug disposition and in conferring multidrug resistance in cancer cells。-estradiol and progesterone ...

摘要：【关键词】 Telomeric Telomere repeat binding factor 2 (TRF2) has been increasingly recognized to be involved in DNA damage response and telomere maintenance。 Our previous report found that sal...

摘要：【关键词】 Chelation Anthracyclines are effective anticancer agents。 However, their use is limited by cardiotoxicity, an effect linked to their ability to chelate iron and to perturb iron meta...

摘要：【关键词】 Relationship Cocaine exerts its stimulatory effect by inhibiting the dopamine transporter (DAT)。 We observed a close relationship between the decrease in potencies of inhibitors at ...

摘要：【关键词】 Molecular In addition to being an important receptor in leukocyte activation and mobilization, CCR5 is the essential coreceptor for human immunodeficiency virus (HIV)。 A large numbe...

摘要：【关键词】 Activity Excess formation of nitric oxide and superoxide by-products (peroxynitrite, reactive oxygen, and reactive nitrogen species) attenuates cholinergic transmission potentially h...

摘要：Mutational inactivation of tumor suppressor tuberous sclerosis complex 2 (TSC2) in LAM constitutively activates the mammalian target of rapamycin (mTOR)/p70 S6 kinase 1 (S6K1) signaling pathway and...

摘要：【关键词】 Dioxin-Mediated Regulation of genes targeted by the ligand-activated aryl hydrocarbon receptor (AhR) has been shown to be controlled by calcium (Ca2+) changes induced by AhR agonists...

摘要：【关键词】 Small-Molecule 95% iodide influx in HT-29 cells in response to multiple calcium-elevating agonists, including thapsigargin, without inhibition of calcium elevation, calcium-calmodulin...

摘要：【关键词】 Inverse Despite the importance of 5-hydroxytryptamine (5-HT)2C (serotonin) receptors in the control of depressive states, actions of antidepressants at these receptors remain poorly ...

摘要：【关键词】 Inhibition Sodium cyanide-induced chemical hypoxia triggers a series of biochemical alterations leading to apoptosis in many cell types, including T cells。 Inhibition of iNOS blocks...

摘要：【关键词】 Na+/Ca2+ Exchanger The proteins NCX1, NCX2, and NCX3 expressed on the plasma membrane of neurons play a crucial role in ionic regulation because they are the major bidirectional syst...

摘要：【关键词】 Cell-Based Compounds that bind to microtubules (MTs) and alter their dynamics are highly sought as a result of the clinical success of paclitaxel and docetaxel。 Biochemical Corp。 Q...

摘要：【关键词】 Factor-B Pharmacological activators of peroxisome proliferator-activated receptor- (PPAR) inhibit growth of non-small-cell lung cancer (NSCLC) cell lines in vitro and in xenograft mo...

摘要：【关键词】 Three-Dimensional After the identification of a new lead bisphenol compound that had good topoisomerase II (EC 5。 The bisphenols represent a new structural class of topoisomerase II...

摘要：【关键词】 Derlin-1 The endoplasmic reticulum-associated degradation (ERAD), the main quality control pathway of the cell, is crucial for the elimination of unfolded or misfolded proteins。 Dis...

摘要：【关键词】 Caveolin The targeting of ion channels to cholesterol-rich membrane microdomains has emerged as a novel mechanism of ion channel localization。 Caveolin is not required for cell surf...

摘要：【关键词】 Potent 10,000 highly toxic abasic sites generated in the genome of each cell every day。 Inhibition of Ape1 using siRNA or the expression of a dominant-negative form of the protein ha...

摘要：【关键词】 Identification Substrate inhibition is a characteristic feature of many cytosolic sulfotransferases。 The differences between the complex structures of SULT2A1/DHEA and SULT2A1/PAP o...

摘要：【关键词】 2-[2-(3,4-Dichloro-phenyl)-2 Long and short QT syndromes associated with loss and gain of human ether-a-go-go-related gene (hERG) channel activity, respectively, can cause life-threa...

摘要：【关键词】 Activation Post-transplant diabetes is an untoward effect often observed under immunosuppressive therapy with cyclosporin A。 Immunoprecipitation and ex Vivo in Vitro Kinase Assay。 ...

摘要：【关键词】 Ginsenoside We have demonstrated previously that the 20(S) but not the 20(R) form of ginsenoside Rg3 inhibited K+ currents flowing through Kv1。4) channels expressed in Xenopus laevi...

摘要：【关键词】 Antitumor Squamous cell carcinoma of the head and neck (SCCHN) is one of the most common malignancies worldwide, with low 5-year survival rates。 Current strategies that block epider...

摘要：【关键词】 Progesterone The breast cancer resistance protein (BCRP。 845) now conclusively demonstrating that progesterone acts via the progesterone A and B receptors to regulate BCRP expressio...

摘要：【关键词】 Distinctions Abuse of psychostimulants such as cocaine and amphetamines has a tremendous social and economic impact。 The breaking and stabilization of salt bridges between these cha...