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br Results and discussion br Conclusions
2021-12-14

Results and discussion Conclusions As described above, the SAR study based on compound 1 led to the identification of compound 4 as an ideal inhibitor. An enzyme level investigation showed that 4 is a more potent and selective FGFRs tyrosine kinase inhibitor than is Ponatinib. In addition, the
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This excellent tolerability is especially interesting in the
2021-12-14

This excellent tolerability is especially interesting in the light of the fact that intravenous administration of liposomal ponatinib was predicted to yield much higher plasma concentrations as compared to the orally administered free drug. In addition, liposomal drug dose in absolute numbers was te
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In conclusion the present study shows that the endothelin sy
2021-12-13

In conclusion, the present study shows that the endothelin system is of importance in the cardiopulmonary vascular pathophysiology of porcine endotoxin shock. In this model, combination of a selective endothelin ETA and a selective endothelin ETB receptor antagonist markedly improved pulmonary circu
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Oxytocin synthesis The selection of mutations in vivo with a
2021-12-13

The selection of mutations in vivo with antivirals is a complex process involving, among other things, the frequency of a given mutation prior to treatment, the effect of that mutation on viral protein function, and the interplay of a given mutation pattern with host immune mechanisms. Investigation
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SGCs tightly ensheath the soma of DRG neurons
2021-12-13

SGCs tightly ensheath the soma of DRG neurons (Costa and Moreira, 2015, Hanani, 2005, Takeda et al., 2009). Intimate associations between SGCs and neurons facilitate bidirectional regulation of SGC function and neuronal excitability. After nerve injury, neuronal hyperexcitability can result in SGC a
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NEIL interacts with many DNA replication
2021-12-13

NEIL1 interacts with many DNA replication proteins including flap-endonuclease 1 (FEN-1), proliferating cell nuclear antigen (PCNA), and Werner RecQ helicase (WRN) through its disordered C-terminal part. One study showed that in in vitro condition, NEIL1 binds to the damaged Kaempferol-3-rutinoside
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br Introduction Glycoproteins represent a staggeringly small
2021-12-13

Introduction Glycoproteins represent a staggeringly small fraction of proteins analyzed by high-resolution techniques despite high concentrations at the cell surface and critical roles in many human diseases. Though one-half or more of all human proteins are predicted to contain a carbohydrate ch
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Importance of glucokinase in glucose homeostasis and a
2021-12-13

Importance of glucokinase in glucose homeostasis and a possibility to change its activity using the activators define the scientific interest in the development of new allosteric activators of GK (Liu et al., 2012, Pfefferkorn et al., 2011, Waring et al., 2013, Behera et al., 2015). Activation of gl
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Tubastatin A receptor br Introduction Hepatocyte injury init
2021-12-13

Introduction Hepatocyte injury initiates and facilitates inflammation in the course of liver disease progression. Thus, understanding the regulatory basis for sensing and responding to damage-associated inflammatory processes in the liver’s parenchymal cells is a primary issue in liver pathophysi
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Since we were able to reach
2021-12-13

Since we were able to reach low micromolar to sub-micromolar potency in both compound series (6 and 7), we were also keen on assessing the preliminary ADME profile (particularly with respect to plasma and liver microsomal stability) of the most active compounds from these series. As it is evident fr
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FGF signals can be transduced
2021-12-13

FGF signals can be transduced to the signaling cascades of RAS-MAPK or PI3K-AKT through FRS2 and GRB2, to the pathways of PKC or PKD via PLCγ and DAG, and to Ca2+-releasing cascade via PLCγ and IP3, finally affecting cellular proliferation, cellular survival, and angiogenesis [48]. By increasing syn
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br Acknowledgement This research was supported by Basic Scie
2021-12-13

Acknowledgement This research was supported by Basic Science Research Program through the National Research Foundation of Korea funded by the Ministry of Education, Science and Technology (NRF-2016R1A2B4012818). Oral Dihydroeponemycin is the most popular administration route due to good patie
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Based on the aforementioned findings variations of the
2021-12-13

Based on the aforementioned findings, variations of the imidazole heterocycle present in the endogenous ligand histamine (1) led to 2-(thiazol-2-yl)ethanamine (2-TEA, 2) and later to 2-(3-bromophenyl)histamine or 2-(3-(trifluoromethyl)phenyl)histamine (3) (Fig. 3). Interestingly, 2-TEA demonstrated
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Betahistine N methyl pyridyl ethylamine is a well known dual
2021-12-10

Betahistine (N-methyl-2-(2-pyridyl)ethylamine) is a well-known dual H1 HG-10-102-01 sale agonist/H3 receptor antagonist with structural resemblance to histamine. Though it has been approved long before the discovery of H3R to treat disorders of vestibular function as Menières-Disease, the evidence
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To promote biomimetic growth of HAp Li
2021-12-10

To promote biomimetic growth of HAp, Li et al. [20] developed a technique to modify cellulose nanofibers using P2O5. It was ascertained that the negative phosphate groups bonded with Ca2+ through coordination bonds and subsequently guided the growth of the Ca–P crystals throughout the scaffolds. Sim
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