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Hyperactivity of the hypothalamus pituitary adrenal HPA axis
2024-01-12

Hyperactivity of the hypothalamus-pituitary-adrenal (HPA) axis, which is well described in MDD (Pariante and Lightman, 2008, Marques et al., 2009), is also observed in AD and results in increased glucocorticoid (GC, cortisol in primates) levels in blood and CSF (Davis et al., 1986, Martignoni et al.
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br Methods br Results br Discussion Agitation in dementia
2024-01-12

Methods Results Discussion Agitation in dementia has recently been defined as a syndrome characterized by inferred or observed evidence of emotional distress associated with at least one behavioral component, i.e. excessive motor activity, verbal or physical aggression (Cummings et al., 201
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An important observation is that this patient has been on
2024-01-12

An important observation is that this patient has been on ALK inhibitor for more than 4 years (51 months: 27 months on crizotinib+24 months on alectinib and on-going) and there was no evidence of disease progression in the central nervous system. The other potential driver mutation in this patient’s
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Recently a Phase III study demonstrated that alectinib the s
2024-01-12

Recently, a Phase III study demonstrated that alectinib, the second-generation ALK inhibitor, might have a better response to ALK-rearrangement patients than crizotinib [10]. Should alectinib replace crizotinib as the frontline treatment for ALK-rearranged patients? Or should those patients be treat
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Many metalloenzyme inhibitors consist of two chemical
2024-01-12

Many metalloenzyme inhibitors consist of two chemical components: the MBG, the portion of the inhibitor designed to bind to the metal, and the scaffold, the portion of the inhibitor recognized by the amino Minocycline HCl residues that form the substrate-binding site of the metalloenzyme. The MGB i
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Receptor tyrosine kinase Axl is
2024-01-12

Receptor tyrosine kinase Axl is a member of the TAM (Tyro3/Axl/Mer) family, and has reported been associated with a spectrum of human cancers [8]. Numerous studies have revealed that the oncogenic potential of Axl is attributed to the anti-apoptotic and proliferative signaling pathways triggered by
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Previous studies have demonstrated that the expression of
2024-01-11

Previous studies have demonstrated that the expression of the Aurora B gene is maximally increased at G2/M phage during mitosis (Honda et al., 2003, Fu et al., 2007, Goldenson and Crispino, 2015), and exhibits an extraordinary upregulation in a number of human cancers (Fu et al., 2007, Kollareddy et
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The Type A series contains of the confirmed
2024-01-11

The Type-A series contains 6 of the 11 confirmed hits, making it a highly attractive lead template. Seven (7) out of 8 Type-A series of 3-substituted-2-furoic acids are highly active (84–100% inhibition) at the high concentration of 100μM. We could deduce some interesting, albeit preliminary structu
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Finally intracrine androgen synthesis metabolism can be acti
2024-01-11

Finally, intracrine androgen synthesis/metabolism can be activated thus allowing A 419259 trihydrochloride to bypass the low levels of androgens in the circulation by producing androgens themselves (Cai and Balk, 2011, Rahman et al., 2004). Moreover, changes in AR co-regulators like the overexpress
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At the top of the
2024-01-11

At the top of the S1 subsite cylinder are two “cap” residues: E572 and M1034 [13]. Atomic structures of PfA-M1 have revealed important clues into potential roles for the cap residues in substrate selection. In the PfA-M1:bestatin co-crystal structure ([13]; Fig. 1), the P1 phenyl ring occupies the S
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br Introduction The structural similarities between puromyci
2024-01-11

Introduction The structural similarities between puromycin (1, Fig. 1) and the aminoacyl adenyl terminal of aminoacyl–tRNA allow it to terminate the protein synthesis process by causing premature release of a polypeptide from the ribosome [1], [2]. Tremendous progress in the study of puromycin an
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br Materials and methods br Results br
2024-01-11

Materials and methods Results Discussion Prostate cancer is the most common cancer in men in the United States and the second leading cause of cancer death. Therapeutic interventions include mainly: radical prostatectomy or radiation therapy (RT), with or without androgen deprivation therap
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Imatinib was first approved for
2024-01-11

Imatinib was first approved for the treatment of Philadelphia chromosome positive chronic myelogenous leukemia in 2001 [25]. This first approved small molecule antagonist is quite unusual in that it provides a durable response that lasts for more than a decade in the majority of patients. Imatinib h
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br Material and methods br Results br Discussion
2024-01-11

Material and methods Results Discussion GRK2 activity has increasingly been shown to contribute to the progression of numerous diseases and organ dysfunction [5], [6]. For instance, a large body of work over the last two decades has identified GRK2 as a major regulator of cardiac dysfunctio
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The obtained results indicate that even
2024-01-11

The obtained results indicate that even when the impairment of the same forms of memory are present, amnesia can develop in different ways. Impairment of memory reconsolidation in the conditioned food aversion model through both the serotonin receptor antagonist and the antagonist of NMDA glutamate
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