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The Nagoya Heart Study enrolled patients with hypertension a
2024-08-19
The Nagoya Heart Study enrolled patients with hypertension and type 2 diabetes or impaired SMER 3 tolerance (12). Patients were randomized to valsartan- or amlodipine-based regimens with a BP target of ≤130/80 mmHg. The primary outcome was a composite of sudden cardiac death, myocardial infarction,
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What is the mechanism by which
2024-08-19
What is the mechanism by which Wnt7a-Fz7 signaling enhances AMPAR localization and synaptic strength? Following induction of LTP, the number of AMPARs rapidly increases at extrasynaptic sites (Makino and Malinow, 2009, Yang et al., 2008a) through PKA-dependent phosphorylation of GluA1 at S845 (He et
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br cDNA cloning gene structure and chromosomal
2024-08-19
cDNA cloning, gene structure and chromosomal localization The cDNA for the leukocyte-type 12S-lipoxygenase was first cloned from porcine leukocytes [9], and later from mouse [10], [11], rat [12], [13], bovine [14] and rabbit [15] sources. The cDNA for the platelet-type 12S-lipoxygenase cDNA has b
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Interestingly hypoxia and an enhanced Warburg effect ultimat
2024-08-17
Interestingly, hypoxia and an enhanced Warburg effect ultimately lead to increased lactate production. The accumulation of lactate results in an acidic tumor microenvironment, which induces local inflammation. Lactate also promotes the polarization of macrophages that express immunosuppressive argin
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Liaohe River situates in the southwestern part of
2024-08-17
Liaohe River situates in the southwestern part of Northeast China and flows through Liaoning Province. Due to the rapid urbanization and industrialization, Liaohe River has become one of the most polluted rivers in China. Multitudinous organic pollutants that can induce toxicity to organisms such as
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Thus far clinical data indicate
2024-08-17
Thus far, clinical data indicate that IDO1 inhibitors have manageable toxicity, albeit with a relatively short period of treatment in a small number of patients. KYN is a pluripotent mediator and key intermediate for the synthesis of a host of downstream KP metabolites that are implicated in inflamm
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A selected set of these new derivatives was then
2024-08-17
A selected set of these new derivatives was then used for functional assays at the human A1AR showing, as expected, an antagonist profile with IC50 values at nanomolar level. The same molecules showed also to be efficacious as nanomolar antagonists in a functional assay aimed at analyzing their abil
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In the late s Solvay Pharmaceuticals
2024-08-17
In the late ‘90s, Solvay Pharmaceuticals discontinued the Phase 2 development of a promising potent and highly selective A1AR antagonist based on the pyrrolopyrimidine scaffold, SLV320 [43] (2, Chart 1, also named derenofylline; Ki hA1AR = 1 nM), for the treatment of acute heart failure [24]. In the
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The role of DHT in
2024-08-17
The role of DHT in early teleost embryogenesis is not entirely clear or established, however additional studies that treat fish embryos to DHT or to specific srd5a inhibitors at critical stages of development (i.e. prior to sex differentiation) will shed light on the early functions of this androgen
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The present study indicates elevated ATX
2024-08-17
The present study indicates elevated ATX activity as a highly sensitive and specific biomarker to differentiate ICP from other pregnancy-related liver disorders or pruritic dermatoses. In Protease Inhibitor Library sale to the current gold standard for diagnosis, total fasting serum bile salt level
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The synthesis of compounds in which the ethyl
2024-08-17
The synthesis of compounds in which the ethyl linker has been modified to the carbamate and urea derivatives , and is shown in . Thus the diamine was reacted with glycolic RGDfK to give the alcohol followed by Mitsunobu reaction with phthalimide to give . Deprotection with hydrazine gave the am
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The Type A series contains of the confirmed
2024-08-17
The Type-A series contains 6 of the 11 confirmed hits, making it a highly attractive lead template. Seven (7) out of 8 Type-A series of 3-substituted-2-furoic acids are highly active (84–100% inhibition) at the high concentration of 100μM. We could deduce some interesting, albeit preliminary structu
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How does the ATM to ATR
2024-08-17
How does the ATM-to-ATR switch occur at DSBs? The progressive attenuation of ATM activation could be attributed to the loss of DNA structures that activate ATM, or to the generation of DNA structures that interfere with ATM activation. Our finding that SSOs do not directly affect the binding of puri
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APJ receptor expression is altered in various cardiovascular
2024-08-17
APJ receptor expression is altered in various cardiovascular diseases, and both increases as well as decreases in APJ receptor expression have been reported. A decrease in mRNA and protein levels of APJ receptors was observed in patients with ischemic heart disease or idiopathic dilated cardiomyopat
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Thiazole heterocycles constitute an interesting class
2024-08-16
Thiazole heterocycles constitute an interesting class of molecules, which exhibit a broad spectrum of biological activity, including antifungal properties [[16], [17], [18], [19]]. Encouraged by our previous study that describes the activity of hydrazine-thiazole derivatives against C. gattii and C.
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