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LX7101 HCL In this study we designed and
2023-10-24
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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Introduction Epinephrine is an endocrine hormone mainly prod
2023-10-24
Introduction Epinephrine is an endocrine hormone mainly produced by adrenal medulla in response to stress (Tank and Lee Wong, 2015). This catecholamine exerts various major physiological effects, concerning notably the cardiovascular system, the respiratory system and the endocrine system, through
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K03861 br Adenosine receptors and innate immunity Monocytes
2023-10-24
Adenosine receptors and innate immunity Monocytes and macrophages. All four adenosine receptor subtypes are expressed on monocytes and macrophages, and their levels and function undergo significant changes during the maturation of macrophages from monocytes. Indeed, quiescent monocytes are charac
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In the late s Solvay Pharmaceuticals discontinued the Phase
2023-10-24
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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br Acknowledgments We thank the anonymous reviewers for thei
2023-10-23
Acknowledgments We thank the anonymous reviewers for their constructive comments on the manuscript, and also thank Dr. Hans-U. Dahms for his comments on the manuscript. This work was supported by a grant from the National Research Foundation (2009-0071218) funded to Young-Mi Lee. This work was al
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br Materials and methods br Results Bilateral microinjection
2023-10-23
Materials and methods Results Bilateral microinjections (n = 6) of 10 mM ACh (300–500 pmol) and 5 mM physostigmine (150–250 pmol) at the two selected caudal NTS sites caused within 1 min significant increases in respiratory frequency (from 54.5 ± 1.7 to 70.9 ± 4.1 breaths/min; +30.8 ± 7.0%; P
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The gene SRD A encodes the
2023-10-23
The gene SRD5A2 encodes the 5-α-reductase enzyme, which converts testosterone into dihydrotestosterone. Although dihydrotestosterone levels are considerably lower than testosterone, dihydrotestosterone has a five-fold stronger binding capacity to the androgen receptor and, thereby, a considerably mo
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The MOB and AOB are important in ungulates Keller
2023-10-23
The MOB and AOB are important in ungulates (Keller and Levy, 2012, Sanchez-Andrade and Kendrick, 2009), which rely heavily on odorant information for social interactions (Baum and Cherry, 2015, Keller and Levy, 2012, Osada et al., 2014, Villagran and Ungerfeld, 2013). The release of GABA and glutama
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br Materials and methods br Results br Discussion
2023-10-23
Materials and methods Results Discussion Japanese encephalitis caused by JEV is characterized by fura 2 receptor neuron death. However, the underlying mechanism is not fully understood. We and other researchers have demonstrated that JEV induces apoptosis by ER stress-mediated IRE1/JNK and
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Although the role of apelin
2023-10-23
Although the role of apelin and APJ receptor in cardiovascular functions has been well-elucidated, little is known for the effect of the central apelinergic system on gastrointestinal (GI) functions. In mice, it has been found previously that central exogenous apelin-13 decreased gastric emptying (G
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TLRs play a key role
2023-10-23
TLRs play a key role in pathogen recognition and early response. In our study, we showed an increase of TLR2 mRNA and protein expression after BMECs were stimulated by S. aureus, as seen for BMECs in a previous study [25]. Although most studies describe TLR4 as a primary receptor for Gram-negative b
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Women are usually at risk of
2023-10-23
Women are usually at risk of sleep deprivation or restriction during pregnancy, especially in the third trimester of gestation, due to the pregnancy-associated anatomic, physiological and hormonal changes (Pien and Schwab, 2004). However, several major G007-LK developmental events, such as the neur
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The G R mutation is
2023-10-23
The G1202R mutation is located at the solvent front of the ALK kinase domain adjacent to the inhibitor's binding pocket. Although barely reported in the setting of crizotinib resistance, it has emerged as the most refractory mutation to both the first- and second-generation ALK inhibitors. The large
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Although several ARIs have reached various phases of
2023-10-23
Although several ARIs have reached various phases of clinical experimentation however most of them have been withdrawn either due to an insufficient bioavailability, their poor efficacy or adverse side effects. Currently Epalrestat is in clinical use for the treatment of diabetic neuropathy. The sid
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AZD0156 To verify whether circulating APN could protect cogn
2023-10-23
To verify whether circulating APN could protect cognitive function during aging, we detected the alterations in circulating adipoenctin levels in aging rats. Our results suggested that circulating APN levels reduced with age. Kawasumi et al’s study results are consistent with ours. They concluded th
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