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Having established the structural requirements for
2024-07-09

Having established the structural requirements for potency in both the biochemical and biomarker (CRA) assays, we evaluated key compounds in the metabolic stability assay. Disappointingly, we found that all compounds had high intrinsic clearances in mouse microsomes. To ascertain whether the in vitr
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Concanamycin A br Autophagy inducers Macroautophagy is often
2024-07-09

Autophagy inducers Macroautophagy is often seen as a cellular process capable of increasing the fitness of Concanamycin A and overcome resistance to several forms of stress [9], [10]. As discussed above, it has been proposed by several authors that an effective strategy for enhancing sensitivity
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The canonical binding sites to which or
2024-07-08

The canonical XCT790 to which α2, α3, or α5 contribute are highly similar. Therefore, differences in ligand affinity will not be large even if a ligand makes optimal use of the small differences in the pockets. As a possible alternative approach to achieve separation of compound effects, ligands wit
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br Aromatase the key enzyme for estrogen formation in
2024-07-08

Aromatase: the key enzyme for estrogen formation in adipose tissue Estrogens are synthesized from androgens by aromatase, a member of the cytochrome P450 superfamily, which is the rate-limiting enzyme in estrogen biosynthesis (Santen et al, 2009, Simpson et al, 1994). At the cellular level, aroma
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protein kinase inhibitor br Implications for cancer ROS have
2024-07-08

Implications for cancer ROS have a long history of being involved in the development and progression of cancer and increased ROS level is considered as a hallmark of many tumors [76], [77]. Initially, it was thought that ROS would serve as chemical mutagens that would indiscriminately damage cell
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betaxolol br Roles of apelin and APJ
2024-07-08

Roles of apelin and APJ in cardiovascular diseases Therapeutic potential of apelin/APJ in cardiovascular diseases Since the apelin/APJ system plays a key role in the occurrence and development of cardiovascular diseases, it seems logical to presume that targeting this axis should be feasible a
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Several studies have explored the relationship between denta
2024-07-08

Several studies have explored the relationship between dental implants and MRONJ development. López-Cedrún JL et al. [13] reported that BRONJ developed after implant treatment in nine patients who were taking bisphosphonates orally. The mean interval between the initiation of treatment and the onset
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Cellular detoxification is an important process that helps r
2024-07-08

Cellular detoxification is an important process that helps remove excess oxidants from the cellular environment through endogenous antioxidants or other molecules capable of reduction. One of the key regulators of antioxidant production is the transcription factor, nuclear factor (erythroid-derived
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br Conclusion br Introduction The identification of Alzheime
2024-07-08

Conclusion Introduction The identification of Alzheimer's disease (AD) biomarkers and their ability to measure pathology antemortem has led to a fundamental reconsideration of the pathogenesis of AD. The importance of biomarkers was already reflected in revised diagnostic criteria proposed by
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We stimulated HNEpC cells with
2024-07-08

We stimulated HNEpC cells with LPS found that the secretion of inflammatory cytokines and the expression of AHR was increased significantly, and miR124 was reduced. It has been found that LPS as a foreign substance can bind to the TLR family of proteins to activate intracellular AHR signaling [[19],
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The relatively high concentration of HT used in
2024-07-08

The relatively high concentration of 5-HT used in this study (100 µM) is consistent with the concentrations used in other published ex vivo studies (Ropert and Guy, 1991, Passani et al., 1994, Shen and Andrade, 1998). In our paradigm 5-HT was focally applied at the surface of the slice via a fast pe
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Compound mg was purified as an amorphous
2024-07-06

Compound 3 (29 mg) was purified as an amorphous, colourless powder. Molecular formula C20H28O4 was established by HRESIMS (Fig. S11) and corroborated with 1H and 13C NMR spectroscopic data (Table 1). IR spectrum showed bands for hydroxyl (3433 cm−1) and carbonyl (1686 cm−1) groups. 13C NMR spectrum
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Osteoblasts have been thought to be the major
2024-07-06

Osteoblasts have been thought to be the major cell type that expresses RANKL (Suda et al., 1999) which is a ligand for osteoprotegerin (OPG) and which functions as a key factor for osteoclast differentiation and activation. Recently, Nakashima and his colleagues (Nakashima et al., 2011) demonstrated
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p-gp inhibitors The use of one or more of
2024-07-06

The use of one or more of psychotropic medications and hypnotics was associated with a higher risk of falls in the current study. Previous studies have also shown that these medications increase the risk of falls in the geriatric population.25, 26, 27, 28, 29, 30, 31 Clinicians should weigh the risk
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The link between HPV infection and neoplasia
2024-07-06

The link between HPV infection and neoplasia has been well established. HPV encodes two oncogenes (E6 and E7) that drive prostaglandin e2 progression by controlling the functions of tumor suppressor proteins p53 and Rb [7]. HPV is associated with more than 99% of cervical CESC cases [8]. CESC remai
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