52 Result(s)
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Article
Synthesis of novel spin-labeled podophyllotoxin derivatives as potential antineoplastic agents: Part XXV
A series of novel spin-labeled 4β-[(4-substituted)-1,2,3-triazol-1-yl]podophyllotoxin derivatives (17a–h) were firstly designed and synthesized with significant regioselectivity by employing Cu(I) catalyzed click...
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Article
Sigma 1 receptor activation regulates brain-derived neurotrophic factor through NR2A-CaMKIV-TORC1 pathway to rescue the impairment of learning and memory induced by brain ischaemia/reperfusion
Sigma-1 receptor (Sig-1R) agonists showed anti-amnesic properties in Alzheimer’s disease models and anti-inflammatory properties in cerebrum ischaemia models. The agonist of Sig-1R was reported to up-regulate ...
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Article
High throughput screening technologies for ion channels
Ion channels are involved in a variety of fundamental physiological processes, and their malfunction causes numerous human diseases. Therefore, ion channels represent a class of attractive drug targets and a c...
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Article
Biochemical features of the adhesion G protein-coupled receptor CD97 related to its auto-proteolysis and HeLa cell attachment activities
CD97 belongs to the adhesion GPCR family characterized by a long ECD linked to the 7TM via a GPCR proteolytic site (GPS) and plays important roles in modulating cell migration and invasion. CD97 (EGF1-5) is a ...
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Article
Impact of Drug Treatment at Neonatal Ages on Variability of Drug Metabolism and Drug-Drug Interactions in Adult Life
As the number of patients taking more than one medication concurrently continues to increase, predicting and preventing drug-drug interactions (DDIs) are now more important than ever. Administration of one dru...
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Article
In vitro assessment of the glucose-lowering effects of berberrubine-9-O-β-D-glucuronide, an active metabolite of berberrubine
Berberrubine (BRB) is the primary metabolite of berberine (BBR) that has shown a stronger glucose-lowering effect than BBR in vivo. On the other hand, BRB is quickly and extensively metabolized into berberrubine-...
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Article
Chemokine CXCL13 activates p38 MAPK in the trigeminal ganglion after infraorbital nerve injury
Recent data demonstrated that chemokine CXCL13 mediates neuroinflammation and contributes to the maintenance of neuropathic pain after nerve injury in the spinal cord. Pro-nociceptive chemokines activate mitog...
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Article
Serum Copeptin Predicts Severity and Recurrent Stroke in Ischemic Stroke Patients
Several studies investigated the prognostic role of copeptin in stroke. The aim of this study is to assess copeptin levels in serum, and investigate their associations with risk of recurrent stroke in a 1-year...
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Chapter
Vanillin
Vanillin is extracted from gastrodin and has been used in the treatment of epilepsy. Vanillin is known as one of the first synthetic spices. It can be used as intermediate for the synthesis of a variety of dru...
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Chapter
Bergapten
Bergapten is extracted from the roots, stems, and leaves of bergamot, of which has a photosensitive activity. It has a significant effect on the treatment of various skin diseases. But, there is no clinical re...
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Article
Genetic Variations Associated with Anti-Tuberculosis Drug-Induced Liver Injury
In order to combat the development of drug resistance, the clinical treatment of tuberculosis requires the combined use of several anti-tuberculosis (anti-TB) drugs, including isoniazid and rifampicin. Combina...
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Article
Profiling and targeting of cellular mitochondrial bioenergetics: inhibition of human gastric cancer cell growth by carnosine
l-Carnosine (β-alanyl-l-histidine) is a naturally occurring dipeptide distributed in various organs of mammalians. We previously showed that carnosine inhibited proliferation of human gastric cancer cells through...
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Article
Identification of PRDX6 as a regulator of ferroptosis
Ferroptosis is a newly characterized iron-dependent form of nonapoptotic regulated cell death triggered by lipid reactive oxygen species (LOOH). The dysregulation of ferroptosis is highly related to cancer, an...
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Article
A novel compound AB38b attenuates oxidative stress and ECM protein accumulation in kidneys of diabetic mice through modulation of Keap1/Nrf2 signaling
Extracellular matrix (ECM) deposition following reactive oxygen species (ROS) overproduction has a key role in diabetic nephropathy (DN), thus, antioxidant therapy is considered as a promising strategy for tre...
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Article
MDL-800, an allosteric activator of SIRT6, suppresses proliferation and enhances EGFR-TKIs therapy in non-small cell lung cancer
Sirtuin 6 (SIRT6), a member of the sirtuin family, is a nicotinamide adenine dinucleotide (NAD+)-dependent deacetylase that is involved in various physiological and pathological processes. SIRT6 is generally down...
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Article
Activation of unfolded protein response overcomes Ibrutinib resistance in diffuse large B-cell lymphoma
Diffuse large B-cell lymphoma (DLBCL) is the most widespread type of non-Hodgkin lymphoma (NHL). As the most aggressive form of the DLBCL, the activated B-cell-like (ABC) subtype is often resistant to standard...
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Article
Bis-isatin derivatives: design, synthesis, and biological activity evaluation as potent dimeric DJ-1 inhibitors
The PARK7 gene (encode DJ-1 protein) was first discovered as an oncogene and later found to be a causative gene for autosomal recessive early onset Parkinson’s disease. DJ-1 has been proposed as a potential thera...
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Article
The C terminus of DJ-1 determines its homodimerization, MGO detoxification activity and suppression of ferroptosis
DJ-1 is a multifunctional protein associated with cancers and autosomal early-onset Parkinson disease. Besides the well-documented antioxidative stress activity, recent studies show that DJ-1 has deglycation e...
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Article
Downregulation of c-Myc expression confers sensitivity to CHK1 inhibitors in hematologic malignancies
Checkpoint kinase 1 inhibitors (CHK1i) have shown impressive single-agent efficacy in treatment of certain tumors, as monotherapy or potentiators of chemotherapy in clinical trials, but the sensitive tumor typ...
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Article
mTOR regulates cocaine-induced behavioural sensitization through the SynDIG1–GluA2 interaction in the nucleus accumbens
Behavioral sensitization is a progressive increase in locomotor or stereotypic behaviours in response to drugs. It is believed to contribute to the reinforcing properties of drugs and to play an important role...
