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In this study we designed
2024-02-18
In this study, we designed and synthesized two ALK PROTACs (degraders), 5 (MS4077) and 6 (MS4078), by linking ceritinib and pomalidomide [45] through two different linkers. Using human ALCL and NSCLC cells, we characterized both compounds in a battery of assays to demonstrate their effects on reduci
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TBB Interestingly hypoxia and an enhanced Warburg effect
2024-02-18
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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br Conclusions Triptans are HT B D F receptors agonists
2024-02-18
Conclusions Triptans are 5-HT1B/1D/(1F) receptors agonists and are considered as the gold standard for acute migraine treatment that have been proven effective. Unfortunately, they are contraindicated in patients with cardiovascular diseases due to their vasoconstrictor (side) effects (MaassenVan
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br Methodology In this paper mechanical properties of G
2024-02-18
Methodology In this paper, mechanical properties of G-actin are examined. To do so, three different external tensile loads are exerted to the protein. As illustrated in Fig. 1, Arp2/3 complex binds to the one sides of mother mdm2 p53 and leads to the growth of a new daughter filament at a distin
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br GMF Remodels Actin Networks
2024-02-18
GMF Remodels Actin Networks at the Leading Edge How are the conserved activities of GMF used in vivo to regulate branched hoechst networks (e.g., at sites of endocytosis and at the leading edge) (Figure 2A,B)? In animal cells, the regulatory effects of GMF on actin networks appear to govern lamel
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Molecular docking is widely used
2024-02-18
Molecular docking is widely used to predict the interaction between an enzyme and its inhibitors. This is a computational simulation approach that can be used as a tool to investigate the structure-activity relationship of ACE inhibitory peptides (Goodsell, 2009). It has been recently shown that ACE
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The synthetic route to M
2024-02-18
The synthetic route to M100907 developed by Rice was utilized, however, the chiral resolution was carried out at an earlier stage to provide the possibility of introducing different substituents onto the piperidinyl group. The conditions for this resolution were different from previously reported.
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br Introduction Melatonin N acetyl
2024-02-18
Introduction Melatonin (N-acetyl-5-methoxytryptamine) is a neurohormone which is mainly secreted from the pineal gland. Melatonin is a highly conserved molecule present not only in vertebrates but also in nonvertebrates such as bacteria, protists, fungi, macroalgae, and plants (Cecon et al., 2017
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Involvement of Adiponectin in the regulation
2024-02-14
Involvement of Adiponectin in the regulation of imatinib resistance in human CML cells has not been hitherto examined. Therefore, in this study, we first established imatinib-resistant K562 CML cells, and then evaluated the effect of Adiponectin in reversing imatinib resistance. The data presented h
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br Experimental section br Results and discussion br
2024-02-14
Experimental section Results and discussion Conclusions We present a simple, sensitive and selective assay of ADA activity and its inhibitor using the enzyme catalyzed reaction and the different interaction intensity of dye-labeled AD aptamer, aptamer/AD complex with GO. The as-proposed met
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The uterine muscle also changes to meet the
2024-02-10
The uterine muscle also changes to meet the demands of pregnancy. Over the course of pregnancy, the myometrium undergoes structural remodeling to accommodate a growing fetus, followed by a functional switch from quiescent to contractile characteristics for parturition. Studies on the mouse model ind
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For the TSH receptor signaling at the Golgi trans
2024-02-10
For the TSH receptor, signaling at the Golgi/trans-Golgi network appears required for both rapid effects of TSH − such as BMS 309403 synthesis depolymerization, which is implicated in thyroglobulin reuptake and, thus, thyroid hormone release − and late ones, such as those on gene transcription. Cont
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These mutations induce the gene
2024-02-09
These mutations induce the gene auto-activation in 10–40% of adenocarcinomas, triggering the EGFR-signaling pathway in the absence of ligand. That leads to an uncontrolled acceleration of cell proliferation, survival and anti-apoptotic signals (Couraud et al., 2012). The frequency of these mutations
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Aldose reductase AR is an NADPH dependent aldo keto reductas
2024-02-09
Aldose reductase (AR), is an NADPH-dependent aldo-keto reductase very well studied as a catalyst of glucose conversion to sorbitol in the polyol pathway [11], [12]. In the diabetic lens characterized by chronically high levels of glucose, AR is responsible for production of high levels of sorbitol a
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In summary the different types of interstitial
2024-02-09
In summary, the different types of interstitial cells found in the current study are illustrated in Fig. 7A (see legend for further details), which is suggestive of a heterogeneous complex network of interstitial cells communicating with each other. The possible signaling pathways involving this int
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