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br Drugs with documented pro apoptotic effects on
2024-06-13
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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br Results br Discussion br STAR Methods br
2024-06-13
Results Discussion STAR★Methods Author Contributions Acknowledgments We thank Angela Walker for assistance with the manuscript; Junlin Liu, Xiangxiang Gu, Na Chen, Lu Xue, and the BV Core Facility of iHuman Institute for their support; scientists and colleagues at Amgen Inc., Zhulun W
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In a missense mutation at
2024-06-13
In 1989, a missense mutation at codon 102 of the PRNP gene was first reported to be associated with GSS and, in 1991, the same mutation was also found in affected members of the “H” family (Hsiao et al., 1989; Kretzschmar et al., 1991). By 1995, the pedigree of the “H” family included 221 family mem
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SU6668 The association of male gender with increased atheros
2024-06-13
The association of male gender with increased atherosclerosis has stimulated interest in the role of androgen signalling in this condition. Androgens act (Fig. 2) by direct activation of androgen receptor (AR), a nuclear receptor that acts as a ligand-regulated transcription factor (Gao et al., 2005
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In the largest postmortem study
2024-06-13
In the largest postmortem study of 3618 autopsied individuals, almost 75% of the individuals without Aβ pathology already harbored cortical NFT pathology mostly confined to the medial temporal regions (Murray et al., 2015). In Braak's study of 2366 autopsied individuals (Braak and Del Tredici, 2014)
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pimaricin synthesis br Role of AMPK in inflammation signalin
2024-06-13
Role of AMPK in inflammation signaling Pro-inflammatory cytokines, such as interleukin (IL)-6 and tumor necrosis factor-α (TNF-α), activate Ikβ kinase (IKKβ), which phosphorylates IκBα, triggering the degradation of proteasomal IκB. This liberates active nuclear factor kB (NF-kB) to translocate i
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br Discussion AhR is a receptor that binds to
2024-06-13
Discussion AhR is a receptor that binds to a great variety of lipophilic compounds, in particular those containing at least one aromatic ring (Abel and Haarmann-Stemmann, 2010, Guyot et al., 2013, Hahn, 2002). The main known function of this receptor is to induce the metabolism of these compounds
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br Adenosine and tumor microenvironment In the majority
2024-06-13
Adenosine and tumor microenvironment In the majority of carcinogenic processes a proinflammatory state is generated [36], [37]. In addition, a tumor hypoxic environment is generally due to inadequate perfusion of oxygen to the tumor [38]. Immunomodulators are molecules that regulate the immune r
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G actin has a molecular weight of kD
2024-06-13
G-actin has a molecular weight of 42 kD and dimensions about 55 × 55 × 35 Å3. It consists of 375 amino acids arranged into two individual domains (Alberts et al., 2014). A central cleft bisects the protein into two aforementioned domains which surround a deep cleft containing ATP or ADP and a tightl
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The first suggestions that the cleaved intracellular domain
2024-06-13
The first suggestions that the cleaved intracellular domain of APP, AICD, might transit to the nucleus and hence selectively regulate gene transcription arose from analogies with the Notch receptor signalling system where similar intra-membrane proteolysis occurs [84], [85] and it was later confirme
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It is already established in the
2024-06-12
It is already established in the literature that products synthesized by 5-LO, such as lipoxin A4, can activate PPARγ in a setting of experimental stroke [43]. Interestingly, experiments using 5-LO knockout mice in an endotoxemia model to mimic septic conditions, demonstrated reduced multiple organ
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Another significant group of reductase inhibitors is the ste
2024-06-12
Another significant group of 5α-reductase inhibitors is the steroidal 3-carboxylic Bax channel blocker derivatives (relevant examples in Fig. 5), which were designed to mimic the putative enzyme-bound enolate intermediate. This was achieved by introducing sp2-hybridized centers at C3 and C4 and an
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Optimization of the B ring specifically
2024-06-12
Optimization of the B-ring specifically targeted preventing the oxidation of the ring system (). As described above, the 4-position of the phenyl ring provides the appropriate vector towards bulk solvent. - and -linked substitutions at the 4-position of the B-ring from the 4-fluoro-nitrophenyl inter
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Chk1 and MK2 Inhibitors set australia The consensus amino ac
2024-06-12
The consensus amino Chk1 and MK2 Inhibitors set australia recognition sequence for p38α substrates is (Ser/Thr)Pro (Cuadrado and Nebreda, 2010), typically assisted by upstream docking motifs (Remenyi et al, 2005, Sharrocks et al, 2000). P450c17 has 32 Ser and 25 Thr residues, of which only Thr 341 a
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Ryoichi et al modified potent clinical candidate VX with
2024-06-12
Ryoichi et al. modified potent clinical candidate VX-680 (6) with 3-cyano-6-(5-methyl-3-pyrazolamino)pyridine as Aurora kinase inhibitor. Substituted cyano pyridine derivative (7) inhibited proliferation of HCT-116 cells with an IC50 value of 115 nM. It showed tumor inhibition in mice model at a dos
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