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Extensive pharmacological and structural analysis
2022-04-09
Extensive pharmacological and structural analysis shows GCGR antibody REMD-477 competitively blocks GLC binding to the GCGR with 30-pM binding affinity, and can fully inhibit the receptor activity at low nanomolar concentrations in Oleandrin 14, 17, 20. Functionally identical to REMD-477, REMD2.59
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In conclusion this is the first
2022-04-09
In conclusion, this is the first study performed in acute limbic seizure models that shows the ability of DAG to dose-dependently attenuate pilocarpine-induced seizures, albeit at a higher concentration as ghrelin (Portelli et al., 2012b). We also establish that DAG's anticonvulsant mechanism of act
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One important discovery of our study is the identification o
2022-04-09
One important discovery of our study is the identification of a pharmacological mechanism for the macrolide antibiotic erythromycin (EM) in promoting joint health. EM is a commonly used antibiotic that directly binds bacterial ribosomes to inhibit protein synthesis [66]. Although EM-like macrolide U
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Because of its role in the cleavage of
2022-04-09
Because of its role in the cleavage of Aβ and the fact that many genetic forms of AD are caused by mutations in the enzyme, GS has long been a target for drug development, though previous clinical trials of Semagacestat, a GS inhibitor, have failed due to an increase in skin cancer, and a decrease i
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Comparison of dlGALRs deduced amino acid
2022-04-09
Comparison of dlGALRs deduced amino Cyclosporin A sale sequences with that of human GALRs demonstrate that the GALR1 ortholog sequences have diverged less than those of GALR2. Since often duplicate genes undergo divergent evolution through sub-functionalization, loss or gain of new functions (Princ
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As mentioned earlier two different
2022-04-09
As mentioned earlier two different isoforms of TFE3 [16] have been reported viz. the full length (TFE3L) and smaller (TFE3S) without exon 1&2. TFE3S lacks an N-terminal acidic activation domain which is present in TFE3L hence is a dominant negative form of TFE3L [51]. This dominant negative feature
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Recently some researchers working in China Pharmaceutical Un
2022-04-09
Recently, some researchers working in China Pharmaceutical University developed novel FFA1 agonists some of which were found to be efficacious in the management of type 2 diabetes and with low toxicity. For instance, Zheng et al. [48] in their in vivo study using experimental animals, reported that
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Several small molecules such as erastin and RSL
2022-04-09
Several small molecules, such as erastin and RSL3, are reported to induce ferroptosis in both normal and cancer D609 [21,22]. We confirmed that erastin-induced growth inhibition is an ideal ferroptosis model for cardiomyocytes. The erastin inhibits the growth of H9c2 cells in a Fe-dependent manner,
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Mitochondria are also involved in other modalities of progra
2022-04-09
Mitochondria are also involved in other modalities of programmed cell death, particularly apoptosis. Intriguingly, the roles of mitochondria in apoptosis and ferroptosis are fundamentally different. In mitochondria-mediated apoptosis, the mitochondrion serves as a reservoir, storing apoptosis-regula
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Defining the cooperation between molecular pathways
2022-04-09
Defining the cooperation between molecular pathways within highly complex biological systems, such as those between immune cell networks and target tissues is certainly a hard task. Recently, there are many investigations in the pathogenesis of renal graft rejection, one of the most evident investig
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The primary or in transit
2022-04-09
The primary or in-transit site of metastasis for many cancers, including melanoma, are nearby sentinel lymph nodes (LNs) [6]. As such, sentinel LN biopsy is a common procedure to diagnose and stage melanoma progression [7,8]. Sentinel LNs are often the primary site of metastasis due to tumor cell-st
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gtpase inhibitor MicroRNAs miRNAs are endogenous small RNA m
2022-04-09
MicroRNAs (miRNAs) are endogenous small RNA molecules 20–25 nucleotides in length; they regulate multiple genes by binding to target mRNAs, thereby controlling the stability and translation of protein coding mRNAs (Esteller, 2011, Guo et al., 2010). It has been established that gtpase inhibitor of
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The synthesis of substituted pyrimidinone carboxamides is
2022-04-09
The synthesis of 2-substituted pyrimidinone carboxamides – is outlined in , . Treatment of readily accessible nitriles with N-methylhydroxylamine hydrochloride in the presence of atm kinase inhibitor provided the adducts , which were subsequently reacted with diethyl acetylenedicarboxylate to affo
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br Role of catecholamines in HIV associated neuroinflammatio
2022-04-09
Role of catecholamines in HIV-associated neuroinflammation Concluding remarks However, more research is needed to determine the precise mechanisms responsible for the immunomodulatory effects of catecholamines, including the involvement of specific receptors and signaling pathways in immune ce
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Dysregulation of catecholaminergic neurotransmission particu
2022-04-09
Dysregulation of catecholaminergic neurotransmission, particularly the dopaminergic system, has long been correlated with the development of neuroinflammation and HAND. Studies specifically examining role of catecholamines in HIV pathogenesis, particularly focused on NeuroHIV, are relatively few. Ho
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