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br Selective Androgen Receptor Modulators SARMs The AR and i
2024-06-24
Selective Androgen Receptor Modulators (SARMs) The AR and its endogenous ligands, androgens, are important for development and maintenance of muscle and bone, secondary sexual organs, and development of other tissues (Mooradian et al., 1987). Although androgens are important for normal developmen
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The potential use of derivatives belonging to this series
2024-06-24
The potential use of derivatives belonging to this series as therapeutic agents mostly depends on their pharmacokinetics and pharmacodynamics. The pharmacokinetic phase includes absorption, distribution, metabolism and excretion (ADME) of the studied compounds. Therefore, preliminary data for theore
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br Regulation and pharmacology of mPGES mPGES kDa
2024-06-24
Regulation and pharmacology of mPGES-1 mPGES-1 (16 kDa, 152 amino acids) is a trimeric integral membrane protein of the endoplasmic reticulum with each monomer containing four transmembrane domains (Samuelsson et al., 2007; Sjogren et al., 2013). The three active site cavities are located at the
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Taniyama et al reported a female
2024-06-24
Taniyama et al. reported a female with infertility who had a homozygous T-to-A transversion at nucleotide position g.2472 in exon 3 of the CYP17A1 gene (mutation Y201N) and decreased 17-hydroxylase and 17,20-lyase activities of WEHI-539 hydrochloride receptor was initiated using dexamethasone to co
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br The embryological and physiological
2024-06-24
The embryological and physiological roles of ATX ATX is a vital enzyme that is needed for early embryological development. ATX knockout (KO) (ENPP2−/−) embryos die in utero on average at day 9.5 with vascular and neural tube defects [30], [73], [74], [75]. In these mice, malformations in the alla
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The synthesis of compounds in which the ethyl
2024-06-24
The synthesis of compounds in which the ethyl linker has been modified to the carbamate and urea derivatives , and is shown in . Thus the diamine was reacted with glycolic osi sc 175 to give the alcohol followed by Mitsunobu reaction with phthalimide to give . Deprotection with hydrazine gave t
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pdtc br Introduction The vacuolar ATPases V ATPases are ATP
2024-06-22
Introduction The vacuolar ATPases (V-ATPases) are ATP-driven proton pumps that play important roles in both normal and disease processes [1], [2], [3], [4], [5]. V-ATPases within cells function in such processes as intracellular membrane traffic, protein processing and degradation, coupled transp
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The allosteric site of class C receptors
2024-06-22
The allosteric site of class C receptors is generally located on the extracellular side of the TM domain (Brauner-Osborne et al., 2007, Christopher et al., 2015, Dore et al., 2014, Gregory et al., 2011, Harpsoe et al., 2017, Kniazeff et al., 2011, Pin and Prezeau, 2007, Urwyler, 2011, Wu et al., 201
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br Current limitations and future directions There are sever
2024-06-22
Current limitations and future directions There are several limitations associated with PET imaging of aromatase using carbon-11 labeled aromatase inhibitors. Due to the very short half-life of carbon 11 (20min), PET studies with currently available, validated tracers can only be performed in med
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There is limited information regarding hyperargininemia inci
2024-06-22
There is limited information regarding hyperargininemia incidence or prevalence. Reports of incidence vary by an order of magnitude: 0.5 to 5.0 per million [5], [6]. A relatively large U.S. study estimated 1.1 cases per million births [7], but it used an indirect methodology that introduces uncertai
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br Roles of apelin and APJ in cardiovascular diseases br
2024-06-22
Roles of apelin and APJ in cardiovascular diseases Therapeutic potential of apelin/APJ in cardiovascular diseases Since the apelin/APJ system plays a key role in the occurrence and development of cardiovascular diseases, it seems logical to presume that targeting this axis should be feasible a
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Plant defensins are cysteine rich cationic peptides of kDa w
2024-06-22
Plant defensins are cysteine-rich cationic peptides of 5–8 kDa whose mature domain comprises 45 to 54 amino X-NeuNAc residues, with an isoelectric point around 9. The global fold of plant defensins consists of a cysteine-stabilized motif (CSα/β) made up of an α-helix and a triple-stranded β-sheet st
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Earlier studies with SERMs identified that distinct chemical
2024-06-22
Earlier studies with SERMs identified that distinct chemical scaffolds have the ability to induce unique conformational changes in the ER, resulting in interaction with different cofactor subsets. The same has been demonstrated with SARMs, which induce distinct conformational changes compared to tes
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br Obstructing SNARE zippering Sharma et
2024-06-22
Obstructing SNARE “zippering” Sharma et al. demonstrated for the first time that in the postmortem AD brains, the level of SNARE complex formation, which is necessary for driving synaptic vesicle fusion at the presynaptic active zone, is significantly reduced [123]. In the absence of changes in e
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Although it is not known
2024-06-22
Although it is not known if CP-AMPAR regulation is required for LTD, our previous characterization of AKAP150ΔPIX knockin mice that are selectively deficient in CaN anchoring, due to disruption of a PxIxIT-type CaN docking motif, provided important insights. We found that AKAP-CaN signaling dephosph
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