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Regarding the HT B receptors
2024-07-17

Regarding the 5-HT1B receptors, they act as terminal receptors and are involved in the presynaptic regulation of the release of 5-HT. But at spinal level these receptors are principally situated post-synaptically (Sari, 2004). The ability of autoreceptors to regulate extracellular levels of 5-HT dur
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br The cytochrome P enzyme hydroxylase lyase P
2024-07-17

The cytochrome P450 enzyme 17α-hydroxylase/17,20-lyase (P450) is involved in the production of the C containing androgen precursors from the C containing steroids such as the pregnanes and progestins (). Steroids such as androstenedione (AD) and dehydroepiandrosterone (DHEA) are therefore synthesi
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At present drugs that specifically inhibit YAP
2024-07-17

At present, drugs that specifically inhibit YAP activity are not available. In fact, verteporfin, which was originally described as a specific inhibitor of YAP-TEAD interaction, has been recently shown to exert its activity through selective induction of proteotoxicity rather than through YAP inhibi
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The ATX LPA signaling axis
2024-07-17

The ATX–LPA signaling “axis” [5] has been implicated in a perplexing variety of physiological and pathophysiological processes, including vascular and neural development [5], [26], [27], [28], [29], tumor progression and metastasis [30], [31], lymphocyte trafficking [22], bone development [32], neur
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br Acknowledgements We thank Dr Stefan Schulte Merker
2024-07-17

Acknowledgements We thank Dr. Stefan Schulte-Merker and his group members at the Hubrecht Institute (Utrecht, the Netherlands) for their invaluable support of the zebrafish studies. Our work is supported by grants from the Dutch Cancer Society (KWF) and the Netherlands Organisation for Scientific
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br Methods br Results br Discussion
2024-07-17

Methods Results Discussion Autotaxin has been shown to have effects on major cell types implicated in OA, notably chondrocytes, osteoblasts, osteoclasts, and synoviocytes, through its enzymatic product LPA [20]. However, a paucity of research exists on the involvement of autotaxin in OA. Fi
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Aurora kinases were initially identified
2024-07-17

Aurora kinases were initially identified as protein kinases essential for error-free chromosome segregation during mitosis and meiosis. Aurora A appears to control premetaphase events, such as bipolar spindle assembly 3, 4, with Aurora B and C directing metaphase and postmetaphase events, including
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From an historical perspective ligands for GPCRs
2024-07-17

From an historical perspective, ligands for GPCRs (adrenaline, serotonin, hexokinase regulation or morphine, to name a few) have been identified before their receptor counterparts, at a time when the concept of receptor itself was controversial [15]. Although many cognate receptors for endogenous l
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br Conflict of interest br Introduction
2024-07-17

Conflict of interest Introduction Platelets are anucleate blood cells essential for hemostasis and wound healing; tight regulation of platelet numbers is crucial for human health. Platelets are synthesized and released from bone marrow megakaryocytes into the circulation where they remain for
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AP was originally described as
2024-07-17

AP-1 was originally described as a heterodimer of the bZIP proteins c-Jun and c-Fos. The experiments described here showed that stimulation of TRPV1 channels induced the expression of both of these classical constituents of AP-1. The essential role of both proteins was analyzed in a series of experi
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br Model Fig demonstrates the block scheme of main
2024-07-17

Model Fig. 1 demonstrates the block-scheme of main interactions between variables of the model under investigation. These interactions are described below in details and are expressed in mathematical form as well, where all variables are the functions of space and time coordinates, r and t, which
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br Conclusions br Declarations br Introduction The classical
2024-07-17

Conclusions Declarations Introduction The classical term of endocrine disruption includes any agent that interferes with the action of hormones within the human body; these agents are therefore named endocrine disruptors. Among these agents, that are mainly environmental chemicals (pollutan
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Immunohistochemistry Hearts from young and aged mice
2024-07-17

Immunohistochemistry: Hearts from young and aged mice were collected at the indicated times, fixed overnight in 10% formalin, and embedded in paraffin. Serial 5-μm heart sections from each group were analyzed. Samples were stained with H&E for routine histologic examination. Immunohistochemical stai
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AAT enzyme activity was readily detected in
2024-07-17

AAT enzyme activity was readily detected in crude cell-free extracts obtained from berry tissues of all accessions but displayed different substrate selectivities (Fig. 2). Cell-free extracts derived from ‘Muscat Hamburg’ berries showed the highest AAT activity with all alcoholic substrates tested,
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Alectinib is a second generation ALK
2024-07-17

Alectinib is a second generation ALK antagonist that is built upon a 9-ethyl-6, 6-dimethyl-11-oxo benzo[b]carbazole scaffold (Fig. 5C) [58]. This drug is effective against the ALK L1196M gatekeeper mutation along with C1156Y and F1174L mutations [7]. The 11-oxo group of the drug forms a PRT-060318
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