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The two competitive bivalent GlxI inhibitors polyBHG
2022-07-16
The two competitive bivalent GlxI inhibitors polyBHG2-62 (=1nM) and polyBHG2-54 (=0.3nM) () were designed based on the transition-state analog -(-bromophenyl--hydroxycarbamoyl) glutathione (BHG) by an examination of the X-ray crystal structure of human GlxI in complex with one CHG at each active sit
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br Materials and methods br Results br
2022-07-16
Materials and methods Results Discussion The glucose transporter GLUT1 can be acutely activated or inhibited in L929 fibroblast Chromocarb by a wide variety of reagents or nutrient conditions [[9], [10], [11], [12],36,50]. This abrupt change in the activity of GLUT1 occurs within minutes an
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iwp2 The mammalian AMPA receptor protein
2022-07-16
The mammalian AMPA receptor protein family comprises four subunits, termed GluR-A through GluR-D (or GluR1 through GluR4), which form hetero-tetrameric receptor complexes Dingledine et al. 1999, Rosenmund et al. 1998. These subunits possess distinctive intracellular C-terminal domains that can be gr
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As glucagon stimulated hepatic glucose production is
2022-07-16
As glucagon-stimulated hepatic 4a 5 2 3.25 a production is a key component of the normal response to hypoglycemia, the potential of a GCGr antagonist to delay or prevent recovery from a hypoglycemic state is a critical safety issue that must be addressed. Studies of the effects on time to recovery f
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br Regulation of the GLI code by non HH
2022-07-16
Regulation of the GLI code by non-HH signals and by the oncogenic load The GLI code may be seen as the essential parameter to regulate canonical HH output. Its regulation first appeared to be strictly dependent on the presence of specific levels of HH ligands. Indeed, GLI1 transcription is so far
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Contradictory results have been described
2022-07-16
Contradictory results have been described regarding the role of the Shh pathway during vertebrate skeletal myogenesis. Different studies have shown that Shh can increase or inhibit myoblasts proliferation and terminal muscle differentiation, depending on the experimental model [[1], [2], [3], [4], [
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The eradication of agonist activity in compound
2022-07-16
The eradication of agonist activity in compound was also confirmed in the ex vivo growth hormone (GH) release experiment conducted in isolated primary rat pituitary RI-1 as shown in . Compound did not produce any noticeable GH secretion at up to 10μM concentration. It could also antagonize the st
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The role of cell to cell interactions
2022-07-16
The role of cell-to-cell interactions in coordinating the cells’ behaviour to ensure an appropriate anterior pituitary hormone response is receiving increasing attention. Anterior pituitary bcl-2 family interact with neighbouring cells through junctional complexes. As their name implies, the comple
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So far only few studies report about GAL in the
2022-07-16
So far only few studies report about GAL in the visual system: GAL has been detected in the cornea of rat (Jones and Marfurt, 1998), mouse (Henken and Martin, 1992) and pig (Stone et al., 1988), and in the uvea of rat (Strömberg et al., 1987), pig (Stone et al., 1988) and cat (Grimes et al., 1994),
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There are multiple docking platforms
2022-07-16
There are multiple docking platforms suitable for use with nucleic STF 083010 receptors. These include: DOCK v4-6 (UCSF) [[68], [69], [70]], AutoDock (Scripps) [71], AutoDock Vina (Scripps) [72], GOLD (Cambridge Crystallographic Data Centre) [73], Surflex-DOCK (BioPharmics) [74], Glide (Schrӧdinger
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For our test subjects we
2022-07-16
For our test subjects, we used established high fat diet–induced obese (eDIO) male mices T2DM models. The establishment of eDIO mice was accomplished with a 60% high fat diet ad libitum over a 14 week period (initiated at 6 weeks of age). Compared with regularly-dieted mice, the eDIO ones weigh sign
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Together the epigenetic interplay revealed in this study ena
2022-07-15
Together, the epigenetic interplay revealed in this study enabled us to expand the therapeutic potential of EZH2is from hematological malignances to solid tumors. In solid tumors, EZH2i-driven transcriptional changes are shown to be dispensable of H3K27me-regulated transcriptional network. Instead,
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br Conclusion We have demonstrated that
2022-07-15
Conclusion We have demonstrated that ETB receptors negatively regulate the expression of AT1 receptors in renal proximal tubule gemsa from WKY rats but not in SHRs. Short-term activation of the ETB receptor increases AT1 receptor phosphorylation in WKY cells but decreases it in SHR cells. We conc
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Obesity may be associated with allergic
2022-07-15
Obesity may be associated with allergic diseases (including atopy, asthma, and allergic rhinitis) in children.9, 10, 11 Furthermore, body mass index (BMI) may be associated with bronchial hyper-responsiveness.9, 12 Nevertheless, the relationship between histamine skin reactivity and BMI is poorly un
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The newest histamine receptor to be discovered
2022-07-15
The newest histamine receptor to be discovered is the H4 receptor, which was identified in humans and cloned in 2000 (Thurmond, 2010). Genetically, the H4 receptor is closely related to the H3 receptor, but is restricted to ASC-J9 receptor within the spleen, intestines and thymus, and to immune cell
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