• AhR was proven to participate in carcinogenesis

  2024-02-22

  

  AhR was proven to participate in carcinogenesis. Its high expression was demonstrated in a variety of tumors, i.e. pancreatic, prostate, urinary tract, lung and papillary thyroid carcinoma (Safe et al., 2013, Mian et al., 2014). However, cell line studies showed variable AhR levels/responses. AhR kn

• A high throughput small molecule ACK biochemical inhibition

  2024-02-22

  

  A high-throughput small molecule ACK1 biochemical inhibition screen was performed in-house and led to the identification of 1μM inhibitor furanopyrimidine (). Further binding studies found MLN0128 to be both ATP-competitive and reversible. Early structure-activity relationship (SAR) work was perf

• br Materials and methods br Results br Discussion Prostate

  2024-02-22

  

  Materials and methods Results Discussion Prostate cancer represents an ideal candidate for chemoprevention because of its high incidence and long latency to clinically significant disease [17]. The precancerous lesion PIN may also be a suitable target for ablation in chemoprevention strateg

• NLX a k a F or befiradol exhibits

  2024-02-22

  

  NLX-112 (a.k.a. F13640 or befiradol), exhibits nanomolar affinity at 5-HT1A receptors, and, in Bexarotene to the 5-HT1A receptor agonists listed above, it presents exceptional selectivity and high efficacy at these receptors (Colpaert et al., 2002, Newman-Tancredi et al., 2017). Additionally, it ha

• A rational approach for the design

  2024-02-22

  

  A rational approach for the design of new steroid compounds as possible competitive inhibitors of CYP17 include chemical modification at C17 of the enzyme's natural substrates, pregnenolone (1) and progesterone (2), introducing groups with moderate to strong dipole properties at C20, such as oxime a

• Introduction An association of elevated branched chain amino

  2024-02-22

  

  Introduction An association of elevated branched-chain LY83583 (BCAA—Leu, Val, Ile) with obesity and insulin resistance was first reported nearly 50 years ago (Felig et al., 1969). With the advent of metabolomics technologies, it has since become apparent that the association of BCAA and related me

• br Material and methods br Results br Discussion T D

  2024-02-22

  

  Material and methods Results Discussion T2D is a substantial threat to global human health [31]. Obesity-associated chronic low-grade inflammation promotes insulin resistance and T2D [32]. In obese individuals, the production of numerous inflammatory molecules including IL-6 and TNF-a is up

• TLX may promote survival and

  2024-02-22

  

  TLX may promote survival and prevent apoptosis in NB (-)-Huperzine A [12]. Here, we ask whether the survival-promoting effects of TLX are mediated by Apoptosis Signal-regulating Kinase-1 (ASK1, MAP3K5). ASK1 is a member of the Mitogen-Activated Protein (MAP) kinase family and it preferentially acti

• NO is an important mediator for maintaining bone

  2024-02-22

  

  NO is an important mediator for maintaining bone integrity since it plays a role in the bone remodeling process. It was shown that mechanical strain and shear stress induce NO synthesis in osteoblasts and osteocytes (van't Hof & Stuart, 2001). It was reported that mechanical loading influences its a

• br Introduction The apelin receptor angiotensin receptor lik

  2024-02-22

  

  Introduction The apelin receptor (angiotensin receptor-like 1, APJ) is a seven transmembrane receptor (7TMR) that belongs to the class A peptidergic G protein-coupled receptors (GPCR) superfamily [1]. The endogenous ligands of APJ are the different isoforms of apelin (namely apelin-13, −17, and −

• Insulin is the central hormone

  2024-02-21

  

  Insulin is the central hormone involved in the control of glucose and lipid metabolism. Other nonmetabolic effects of insulin are intensively studied as well. Activation of insulin receptor not only promotes glucose uptake, protein synthesis, and inhibits lipid metabolism, but also is crucial for re

• Thus far a tight coupling has been

  2024-02-21

  

  Thus far, a tight coupling has been observed between mAbs that target aggregated Aβ and the occurrence of ARIA. If ARIA-E is caused by increased trafficking to and clearance of fibrillar Aβ from cerebral vessels (20), mAbs could be designed with conformationally specific epitopes selective for solub

• Treatment of RAW cells with AP exosomes

  2024-02-21

  

  Treatment of RAW264.7 faah inhibitors with AP(+)-exosomes caused an increase in their phagocytic activity. In the presence of amastatin, phagocytic activity was not completely suppressed, suggesting that at least two components were responsible for the activity; one of which is aminopeptidase(s). W

• A large number of aldose reductase inhibitors have been

  2024-02-21

  

  A large number of aldose reductase inhibitors have been prepared synthetically, and a limited number of them are therapeutically used. However, none of them is satisfactory. Here, Cannabis extracts with high content of non-psychotropic phytocannabinoids CBD/CBDA or CBG/CBGA showed statistically sign

• The most widely recognized effects of adenosine are

  2024-02-21

  

  The most widely recognized effects of adenosine are operated through inhibiting A1R, one of the most abundant G protein-coupled receptors in Istaroxime hydrochloride tissue [53]. A1R are located presynaptically, postsynaptically and nonsynaptically [54]. Effect of adenosine in neuronal circuits of

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