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br Author contributions br Transparency
2022-05-11
Author contributions Transparency document Acknowledgments The financial contributions of the Marie-Curie Action: BIOCONTROL, contract number MCRTN – 33439, the Agence Nationale de la Recherche (projects membraneDNP 12-BSV5-0012, MemPepSyn 14-CE34-0001-01, InMembrane 15-CE11-0017-01 and the
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The current lack of effective treatments for
2022-05-11
The current lack of effective treatments for primary or metastatic UM leaves a large therapeutic gap for patients and clinicians underscoring an urgent need for the identification of additional pharmacological targets for therapeutic intervention. As YAP-targeting strategies have remained elusive th
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Finally the optimized leads and were tested
2022-05-11
Finally, the optimized leads (−)- and (−)- were tested in rat model of CIPN (3 and 30 mg/kg, po, qd, administered for 7 days) and the results have been shown in . Under acute set up, after single oral administration at 30 mg/kg, both the compounds exerted significant improvement of the NP condition
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The structures of KDM A revealed a
2022-05-10
The structures of KDM4A revealed a Cys-His Zn(II) binding site that is close to the substrate binding spot, which bioinformatic analyses indicated was not present in any other histone demethylase subfamily. Therefore, an alternative method to inhibit the KDM4 family (95) would be to use compounds th
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In mammalian cells Motins have been identified as
2022-05-10
In mammalian cells, Motins have been identified as a key link between F-actin and Hippo pathway regulation, as knockdown of all three Motins increased Yap activity even in the presence of cytoskeletal disruption [105]. Motins can physically associate with F-actin but this association is blocked by p
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salicin synthesis While the binding of HK to VDAC is
2022-05-10
While the binding of HK1 to VDAC1 is strong and continuous, the binding of HK2 to VDAC1 is much weaker, and alternates between a cytoplasmic and a mitochondrial-bound states (John et al., 2011). This dynamic process is regulated by the metabolic and energetic requirements of the salicin synthesis an
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One of the possibilities of
2022-05-10
One of the possibilities of HO-1 targeting is gene therapy. So far, the majority of preclinical studies have focused on recombinant adeno-associated viral (rAAV) vectors as DNA carriers. They not only provide stable, long-term transgene expression in non-dividing 3-isomangostin synthesis but also ha
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Similarly towards the acylsulfamoyl benzoxaboroles the boron
2022-05-10
Similarly, towards the 5-acylsulfamoyl benzoxaboroles, the boronate intermediate was prepared according to , while the boronate , an intermediate towards 4-acylsulfamoyl benzoxaboroles, was prepared according to . The sulfonamides and used in the synthesis were made from the starting sulfonyl chl
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cucurbitacin For further understanding of the interaction
2022-05-10
For further understanding of the interaction between these inhibitors and proteins (BRafV600E and HDAC1) for guiding the SAR, compound 10e, the most potent compound of this series, was chosen as a representative for docking into the BRafV600E (PDB code: 1UWJ) and HDAC1 (PDB code: 1C3R), revealing ex
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Introduction Hepatocellular carcinoma HCC is
2022-05-10
Introduction Hepatocellular carcinoma (HCC) is the fifth most lethal malignant tumor worldwide and is the second leading cause of cancer-related death [1]. For HCC patients, (+)-MK 801 virus (HBV) infection is the important causative risk factor in Asia-Pacific regions [[2], [3], [4]]. In China, m
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br S proteins and HBV induced autophagy
2022-05-10
S proteins and HBV-induced autophagy HBV surface proteins (S proteins or HBs) are reported to trigger HBV-induced autophagy by inducing ER stress and UPR in host retinoic acid receptor [22]. HBx and HBV-induced autophagy HBx is a multifunctional viral protein. It can regulate virus replicati
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Introduction Soluble guanylyl cyclase sGC is
2022-05-10
Introduction Soluble guanylyl cyclase (sGC) is a key protein in the regulation of multiple physiological functions in mammalian physiology [1,2]. Upon stimulation by nitric oxide (NO) [3], sGC generates cyclic guanosine monophosphate (cGMP) from guanosine-5′ triphosphate and activates protein kinas
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br Author contributions br Conflict
2022-05-10
Author contributions Conflict of interest Acknowledgments We appreciate technical support of the Research Support Center at the Graduate School of Medical Sciences of the Kyushu University. This study was supported by the Uehara Memorial Foundation and a KAKENHI grant from the Ministry of E
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To effectively evaluate prospective mechanisms by
2022-05-10
To effectively evaluate prospective mechanisms by which chronic HIV infection induces pulmonary fibrotic changes in humans, we confirmed that predisposition to fibrotic change in older individuals could be mimicked in a mouse model. Hydroxyproline is a nonessential amino mma f required for the synt
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Our exploration of Domain focused on the
2022-05-10
Our exploration of Domain 1 focused on the role of the carbonyl linker in (). We found that replacement of this group by a methylene unit as in or direct attachment of the thiophene ring to the central aromatic core as in did not significantly impact potency. The thiophene ring in could be repla
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