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Based on structure activity relationship of several SARM
2023-10-08
Based on structure activity relationship of several SARM templates, Ligand Pharmaceuticals chose LGD2226 as their first clinical candidate (Miner et al., 2007). Although LGD2226 demonstrated myo- and osteo-anabolic activity and maintenance of sexual function in various preclinical models, the develo
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YM 155 ERAP has been crystallized in two
2023-10-08
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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N terminally extended antigenic peptide precursors that surv
2023-10-08
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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PF-5274857 br Serine glycine and one carbon metabolism
2023-10-08
Serine/glycine and one-carbon metabolism Altered serine metabolism in tumors was noted nearly half a century ago, and elevated flux through the de novo serine synthesis pathway (SSP) is a common phenomenon in cancer PF-5274857 [43]. The SSP branches from glycolysis at the point of 3-phosphoglyce
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br Study approval br Author
2023-10-08
Study approval Author contributions Conflicts of interest Acknowledgements This work was supported by grants of the Youth Backbone Program (to Jianming Ying) of Cancer Hospital, CAMS, Beijing, Beijing Hope Run Special Fund of Cancer Foundation of China (LC2015A06) and the National Natura
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Growing evidence indicates that GRKs can exert different eff
2023-10-07
Growing evidence indicates that GRKs can exert different effects within the cell depending on the stimulus, cell type, and localization [97], [121]. In this sense, we were the first to demonstrate a mitochondrial localization for GRK2 [122], later confirmed by other investigators [123], establishing
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br Results br Discussion Members of the PfkB
2023-10-07
Results Discussion Members of the PfkB family of proteins, which exhibit AK activity, have only been found in the eukaryotic organisms in the past. Hence, the report of a PfkB family protein in MTub that exhibited AK activity was of much interest, and it necessitated closer examination of its
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The biological characteristics of cancer invasion and metast
2023-10-07
The biological characteristics of cancer invasion and metastasis are mainly attributed to the poor prognosis in cancer. It has been reported that overexpression of Ack1 promoted the migratory and invasive properties of breast cancer Matrine mg by sustaining expression of epidermal growth factor. In
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The role of DHT in
2023-10-07
The role of DHT in early teleost embryogenesis is not entirely clear or established, however additional studies that treat fish embryos to DHT or to specific srd5a inhibitors at critical stages of development (i.e. prior to sex differentiation) will shed light on the early functions of this androgen
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Because of its role in tumor growth proliferation and metast
2023-10-07
Because of its role in tumor growth, proliferation and metastasis, Axl is considered a therapeutic target. Several Axl inhibitors, including low-molecular-weight agents and antibodies, have been reported. Axl inhibition, using low-molecular-weight inhibitors or shRNA knockdown, resulted in reduced t
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Aurora kinases are a conserved family
2023-10-07
Aurora kinases are a conserved family of serine/threonine kinases that are important for the transition through mitosis and amplification and overexpression of Aurora kinases have been implicated in parp apoptosis pathway and transformation. Aurora B is located at the centromere and controls aspect
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Human leukemic blasts from both
2023-10-07
Human leukemic blasts from both AML and ALL patients demonstrated 5-, 12-, and 15-LOX expression [54]; however, using quantitative PCR, 5-LOX was much more prevalent than 15-LOX. When 15-HETE, 12-HETE, and LTB4 were tested for a direct effect on leukemic blasts, none induced apoptosis [54]. In contr
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Oocytes from the African clawed frog
2023-10-07
Oocytes from the African clawed frog Xenopus laevis have been widely used as an expression system to study the modulation of NMDA receptors by metabotropic receptors, such as metabotropic glutamate receptors [12], μ opioid receptors [13], insulin receptors [14] and serotonin receptors [15]. No data
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There is little question that as we become more proficient
2023-10-07
There is little question that as we become more proficient in the diagnosis of arginase 1 deficiency individuals with intermediary elevations in arginine on newborn screening and partial defects in enzymatic activity will be found. There are no reliable data to determine a safe level of arginine and
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br Acknowledgements This work is
2023-10-07
Acknowledgements This work is sponsored by the National Natural Science Foundation of China (grant no. 31201963) and Youth Backbone Teachers Project in Henan Province Department of Education, China (grant no. 2016GGJS-061). Introduction Acute lymphoblastic leukemia (ALL) is a malignant disord
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