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The idea of boron based pro estrogens has been
2019-08-27
The idea of boron-based pro-estrogens has been utilized before; in previous studies, the selective estrogen receptor modulators (SERMs) tamoxifen and endoxifen have been masked as boronate esters.13, 14, 15 Tamoxifen and endoxifen both target ERα as therapies for breast cancer. The previous work foc
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Both progesterone and the calcium ionophore A rely on the
2019-08-27
Both progesterone and the calcium ionophore A23187 rely on the synthesis of cAMP by sAC to elicit exocytosis in human sperm (Fig. 2E-H and [8], [60]). We had reported earlier that digestion of endogenous cAMP with recombinant cAMP-specific phosphodiesterase 4D [9] or inhibition of its synthesis with
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The Wnt catenin signaling pathway is a
2019-08-27
The Wnt/β-catenin signaling pathway is a downstream target of SOX9 and is involved in a variety of cellular responses, including cell migration, proliferation, and differentiation [14]. Several studies have identified the Wnt/β-catenin signaling pathway as essential for cartilage function, and it is
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Despite a high affinity for progesterone
2019-08-27
Despite a high affinity for progesterone and a relatively high affinity for testosterone [7], the binding of progesterone and testosterone to CBG is often disregarded [1], [2], [3]. However, the concentrations of these two hormones varies considerably under both normal physiological and pathophysiol
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Using the juxtarenal PPE the induction of juxta and
2019-08-27
Using the juxtarenal PPE, the induction of juxta- and suprarenal aneurysms is described herein (Fig. 3A). The infra-/suprarenal part of the LY2090314 kinase can now be investigated separately, taking into account different embryological backgrounds and varying reactivity to differing stimuli (revie
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Nilotinib monohydrochloride monohydrate There is evidence th
2019-08-27
There is evidence that the response of CYP450 activity to DEX is species-specific. CYP1A and CYP3A expressions were strongly induced by DEX in porcine hepatocytes (Rasmussen et al., 2014) and in rat and human, but not minipig or beagle dog hepatocytes (Lu and Li, 2001). Within fish, there are also s
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dihydroxycholesterol OHC was recently identified by
2019-08-27
7α,25-dihydroxycholesterol (7α,25-OHC) was recently identified by classic analytical methods as a high-affinity ligand for EBI2 (Hannedouche et al., 2011; Liu et al., 2011). 7α,25-OHC was previously identified as an intermediate in the alternate pathway of hepatic bile ARQ 621 synthesis (Russell, 2
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HOIP s ability to build linear Ub
2019-08-27
HOIP\'s ability to build linear Ub chains arises from a unique domain that follows directly after the RING2 domain, the linear ubiquitin chain-determining domain (LDD) (Fig. 1). Structures have revealed that the LDD is structurally integrated into RING2, creating a single RING2–LDD unit (Fig. 2D) [4
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Identification of the drug to be used as
2019-08-26
Identification of the drug to be used as first-step antihypertensive treatment has always been, and remains, a matter of debate. The decision wihich drug (or drug combination) to choose as first-line therapy depend on many variables such as coexisting metabolic disorders, obesity, presence of subcli
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br In order to determine the physiological
2019-08-26
In order to determine the physiological roles of WT (wild type) EWSR1, Dr. Lee\'s group established a conventional Ewsr1 KO mouse [38]. Since then, the Ewsr1 KO (−/−) mouse model has successfully been utilized to decipher many important in vivo roles of EWSR1 (Fig. 1). EWSR1 deficiency alters m
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A recent analysis of urine samples collected
2019-08-26
A recent analysis of 2721 urine samples collected from 245 men and 408 women across the US general population between 2005 and 2010 showed that MP, PP and BuP were measurable in 99.9%, 98.3% and 73.6% of samples from women and 99.3%, 90.2% and 35.9% of samples from men, respectively (Smith et al., 2
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br Materials and methods br Results br Discussion
2019-08-26
Materials and methods Results Discussion In particular, we showed that pancreatic neuroendocrine tumor signal transducer and activator of transcription 6 fragment recognize cAMP as a stimulatory signal for cell proliferation. Conversely, cAMP was found to have an inhibitory effect on cell p
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The host virus coexistence is completely dependent on the ba
2019-08-26
The host-virus coexistence is completely dependent on the balance between a strong immune response inhibiting virus replication and immune evasion and survival of the virus with periodic shedding to enable transmission to new hosts. In the process of ensuring this balance, the virus manipulates 7TM
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Muscle Ring Fingers MuRFs comprising TRIM
2019-08-26
Muscle Ring Fingers (MuRFs) comprising TRIM63 (MuRF1), TRIM55 (MuRF2) and TRIM54 (MuRF3) are the most studied TRIMs in the heart. However, with increasing knowledge of E3 ligases and recent advancements in the field, many other TRIMs such as TRIM8, TRIM21, TRIM24, TRIM32, TRIM45, TRIM69 and TRIM72 w
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In contrast crystal structures of
2019-08-26
In contrast, crystal structures of the oxyester-linked Ubc13 and UbcH5b conjugates (Eddins et al., 2006, Sakata et al., 2010), and the NMR structure of the disulfide-linked UbcH8 conjugate (Serniwka & Shaw, 2009), revealed distinct open conformations (Fig. 10.3). In part, differences in the position
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