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In the late s Solvay Pharmaceuticals discontinued the Phase
2023-12-21
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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Actin is capable of polymerizing
2023-12-21
Actin is capable of polymerizing spontaneously. However, this process is relatively slow and kinetically unfavorable in cells. Formation of Cy3 carboxylic acid (non-sulfonated) dimers and trimers, which can easily disassemble due to their instability, is a rate-determining step in actin polymerizati
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In summary this study reveals that the stability
2023-12-21
In summary, this study reveals that the stability of rapsyn is critically dependent on HSP90β, highlighting a novel function of HSP90β in NMJ formation and maintenance. It also identifies a mechanism in agrin signaling for AChR clustering, i.e., by upregulating the interaction between HSP90β and rap
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We used the lead compound C to demonstrate
2023-12-20
We used the lead compound C4 to demonstrate that small molecule ACL inhibitors can recapitulate ACL knockdown (KD) in modulation of cancer stemness. We have shown previously that ACL KD reduced the CSC population in multiple cancer cell lines. The E-snail cells are an established CSC model system.
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155 8 The leaves of Bambusa nutans B vulgaris B textilis McC
2023-12-20
The leaves of Bambusa nutans, B. vulgaris, B. textilis McClure, B. vulgaris var. vittata, and Dendrocalamus oldhami are reported as promising natural alternatives to synthetic antioxidants as functional food ingredients (Tripathi et al., 2015). Luo et al. (2015), identified two novel flavonoids name
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Autophagy Compound Library N terminally extended antigenic p
2023-12-20
N-terminally extended antigenic peptide precursors that survive cytosolic degradation and enter the ER, need to be further processed by ERAP1 and/or ERAP2, in order to acquire the right length required for MHCI binding. ERAP1 (ERAAP in mouse) is an IFN-γ-inducible, metalloaminopeptidase that trims N
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br Materials and methods br Results br Discussion Knowledge
2023-12-20
Materials and methods Results Discussion Knowledge of the molecular basis of an inherited genetic disease is crucial for understanding the disease pathology and, ultimately, for therapeutic design. Several recent reports have stressed the need for physical characterization of disease-associ
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Cryptochlorogenic acid br Acetaldehyde One of the most commo
2023-12-20
Acetaldehyde One of the most common environmental aldehydes is acetaldehyde (CH2CHO). Acetaldehyde, which is highly volatile, has been classified as a Group I human carcinogen by the International Agency for Research on Cancer [30]. Aldehydes can form DNA adducts, including ring-open forms of cro
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Targeted disruption of the Akt gene in mice
2023-12-20
Targeted disruption of the Akt1 gene in mice induces a growth retardation phenotype [4,19]. Akt2 KO mice reveal mild growth retardation and insulin resistance [4,20,21]. Akt1/2 double KO (DKO) mice display severe growth deficiency and die shortly after birth. These mice exhibit impaired bone and ski
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Within the PARP family TIPARP is most evolutionarily conserv
2023-12-20
Within the PARP family, TIPARP is most evolutionarily conserved with PARP12 (ARTD12) and PARP13 (ARTD13) [27,28,41]. All three proteins contain at least one RNA-type CCCH zinc finger domain, a poly-ADP-ribose binding WWE domain and a PARP catalytic domain (Fig. 1). PARP13 is catalytically inactive,
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The putative physiological meaning of epinephrine related
2023-12-20
The putative physiological meaning of epinephrine-related hepatic drug transporter regulation remains to be established. It is nevertheless noteworthy that the catecholamine rather decreases expression of sinusoidal SLC transporters like NTCP, OAT2, OAT7, OCT1, OATP1B1 and OATP2B1 whereas those of c
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Voluminous literature about the neuroendocrine
2023-12-20
Voluminous literature about the neuroendocrine mechanism of reproduction and energy regulation has emerged from studies involving mammalian species. The avian infundibular nucleus (equivalent structure to the mammalian arcuate nucleus) consists of two neuronal populations, one of which expresses neu
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2 nbdg br Actin cytoskeleton in protrusion Pushing force dri
2023-12-20
Actin cytoskeleton in protrusion Pushing force driving membrane protrusion is generated by polymerizing 2 nbdg filaments organized either into branched networks or parallel bundles. Branched networks are assembled through Arp2/3 complex-dependent actin nucleation and drive protrusion of lamellip
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The subdivision of HT receptors
2023-12-19
The subdivision of 5-HT receptors started in the 1950s by Gaddum and colleagues, when they realised that in the guinea pig ileum, the effects of 5-HT could be blocked in part by morphine (M), and in part by dibenzyline (D). Gaddum and Picarelli proposed two receptor classes, 5-HT M and 5-HT D (1957)
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In humans the major LOs are subdivided
2023-12-19
In humans, the major LOs are subdivided by their positional specificity into 5-(ALOX5), 12-(ALOX12) and 15-LO (ALOX15) (Kuhn et al., 2015). 5-LO is the key enzyme for LT biosynthesis and mainly found in mature cells from myeloid origin, including neutrophil, eosinophil and basophil granulocytes, mon
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