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Our observation that squalestatin caused only small differen
2023-08-11

Our observation that squalestatin caused only small differences in the production of Aβ40 and Aβ42 was in contrast to prior reports of the effects of other cholesterol synthesis inhibitors. This may be due to using squalestatin, a more specific cholesterol synthesis inhibitor that does not affect is
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Although AMPK is a negative regulator of bioenergetic reprog
2023-08-11

Although AMPK is a negative regulator of bioenergetic reprogramming in cancer cells, little is known about the role of AMPK in immunometabolism in sepsis. Our current study indicates that AMPKα dysfunction enhances PKM2-dependent aerobic glycolysis, which results in HMGB1 release in macrophages and
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Although only Leu CysAP IRAP Herbest et al Keller
2023-08-11

Although only Leu/CysAP (IRAP) (Herbest et al., 1997, Keller, 2004) and DPPIV (Alponti and Silveira, 2010, Kirino et al., 2009) had been identified and studied in adipocytes, our kinetic analysis suggested the highest physiological significance for AspAP (highest affinity) and APM and PSA (highest e
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To understand the kinase selectivity
2023-08-11

To understand the kinase selectivity profile of this series, Furosemide , as a representative analog from this series, was profiled against 216 purified protein kinases representing the tyrosine and serine/threonine kinase families using an in-house Caliper EZ Reader mobility shift assay. Assays we
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Based on the observation that
2023-08-11

Based on the observation that antipsychotic drugs increase 5-HT1A–D2 heteromerization level (Łukasiewicz et al., 2016), we set out to compare the effect of paroxetine to that of risperidone. Paroxetine, a potent SSRI, is very effective in the treatment of depression and anxiety disorders, e.g., gene
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Finasteride was the first steroidal reductase
2023-08-11

Finasteride (13) was the first steroidal 5α-reductase inhibitor approved by the US Food and Drug Administration (FDA) in 1992 for treatment of BPH. In fact, long term clinical studies with this drug demonstrated a sustained reduction of the prostatic specific antigen and an overall improvement in BH
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At present drugs that specifically inhibit YAP activity
2023-08-11

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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br Funding br Ethics br Conflict of interest br
2023-08-11

Funding Ethics Conflict of interest Acknowledgements Introduction Hepatic fibrosis occurs in response to different etiologies of chronic liver injury, which is mainly accompanied by pathological Cytochalasin J of excessive extracellular matrix (ECM) of the liver, as the common reacti
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rad001 br Introduction Human esophageal carcinoma is one
2023-08-11

Introduction Human esophageal carcinoma is one of the most frequently diagnosed cancers, ranked as the eighth leading causes of cancer-related mortality worldwide. Esophagus squamous cell carcinoma (ESCC) is the most common histological type of esophageal carcinomas, especially with a higher inci
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Our previous studies and others have identified
2023-08-10

Our previous studies and others have identified that the inhalational anesthetic isoflurane induces neuronal apoptosis via [Ca2+]i overload through the opening of synaptic voltage-dependent calcium channels (VDCCs) and the excessive Ca2+ release from the endoplasmic reticulum (Zhao et al., 2011; Zha
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br Drugs with documented pro apoptotic effects on
2023-08-10

Drugs with documented pro-apoptotic effects on platelets More than 200 drugs are reported to cause thrombocytopenia [5,42]. The concept of platelet apoptosis is relatively new and was only recently evaluated in the context of drug-induced thrombocytopenia [43]. Table 2 lists the drugs presently k
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F is an orotomide a
2023-08-10

F901318 is an orotomide, a novel class of antifungals, which inhibits pyridine biosynthesis by blocking dihydroorotate dehydrogenase (URA1) activity [137]. Although this pathway is conserved in humans, human URA1 is only 20% identical to its fungal homolog and it is inhibited 2000-fold less effectiv
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br Results A total of respondents completed the survey respo
2023-08-10

Results A total of 126 respondents completed the survey (68.5% response rate), with at least 65% response rate from each of the four represented sectors (denominators represent the total constituent body of the organization or the total attendees of the meeting): PUC 24 out of 37 (65%), SPUNZA 33
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This unsuspected antagonistic interaction of androgen with
2023-08-10

This unsuspected antagonistic interaction of androgen with OXER1 could therefore explain the effect of plant derived compounds with this ligand-receptor system. For example, wedelolactone, a coumestan found in Eclipta alba (false daisy) and in Wedelia calendulacea that is the major component of ecl
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ERAP has been crystallized in two different conformations
2023-08-10

ERAP1 has been crystallized in two different conformations, wherein the C-terminal domain IV is either closely interacting with domains I/II and enclosing the active site (termed ‘closed’), or is rotated away in a hinge motion which exposes the active site (‘open’). This large motion correlates with
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