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Adenosine receptors activate a number of signalling pathways
2024-03-06

Adenosine receptors activate a number of signalling pathways involved in tissue survival including several mitogen-activated protein kinases (Fredholm et al., 2001). The common feature of all adenosine receptors is the positive coupling to ERK1/2, whilst A2B and A3 receptors can also activate the st
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Oxidative stress has recently been reported as
2024-03-06

Oxidative stress has recently been reported as one of the important mechanisms of toxic effect of Cd2+[43]. The mechanism of Cd2+-induced oxidative stress involves an imbalance between generation and removal of ROS in tissues and cellular components, causing damage to membranes, DNA, and proteins [4
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The role of DHT in early teleost
2024-03-05

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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Protein phosphorylation is an important posttranslational me
2024-02-29

Protein phosphorylation is an important posttranslational mechanism for the regulation of distribution, trafficking, and function of modified proteins (Wang et al., 2014). GluA1 phosphorylation at S845 also has functional consequences (Lu and Roche, 2012). For instance, S845 phosphorylation drove tr
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br Angiogenesis as a critical event in diabetic retinopathy
2024-02-23

Angiogenesis as a critical event in diabetic retinopathy Angiogenesis refers to the abnormal proliferation of blood vessels during various pathological conditions. It acquires the stature of being one of the most detrimental events responsible for the progression of diabetic retinopathy. Angiogen
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The renin angiotensin system RAS
2024-02-23

The renin-angiotensin system (RAS) is a hormonal system which plays a role in the regulation of blood pressure and body fluid 92 8 [14]. The main bioactive peptide of RAS is angiotensin II (Ang II) whose biological functions are interposed through angiotensin type 1 receptor (AT1R) and angiotensin
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Luo Dehm Raj Luo Attard Balk Bevan
2024-02-23

Luo, Dehm, Raj. Luo, Attard, Balk, Bevan, Burnstein, Cato, Cherkasov, De Bono, Dong, Gao, Gleave, Heemers, Kanayama, Kittler, Lang, Lee, Logothetis, Matusik, Plymate, Sawyers, Selth, Soule, Tilley, Weigel, Zoubeidi, Dehm, Raj. Luo, Attard, Balk, Bevan, Burnstein, Cato, Cherkasov, De Bono, Dong,
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br Conflict of interest statement br Introduction Currently
2024-02-23

Conflict of interest statement Introduction Currently, adenocarcinoma is the most common histological subtype of lung cancer. Activating mutations and translocations with a potential for targeted therapy are reported predominantly in non-smokers. ALK rearrangement is found in less than 5% of u
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The lactam emerged as lead candidate due to
2024-02-23

The lactam (6) emerged as lead candidate due to its high selectivity, outstanding potency (against ALK or in clinically known ALK mutants), low in vitro clearance, and low efflux potential. The lactam (6) was selected for further profiling against the resistant ALK mutants. Preclinical rat pharmacok
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br Study approval br Author
2024-02-23

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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Analyses of brain CSCs isolated from
2024-02-23

Analyses of GSK343 CSCs isolated from 24 pediatric and six adult brain tumors detected ALDH levels proportional to tumor type and aggressiveness. ALDH-expressing cells (ALDH+) formed spheroids while ALDH1 pharmacological inhibition by a combination of DEAB and RA decreased significantly sphere numb
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ret proto oncogene Previously we described that cadmium
2024-02-23

Previously, we described that cadmium induces a more pronounced, but not selective, cell death on primary cholinergic neurons from basal forebrain (Del Pino et al., 2014). Degeneration of septal cholinergic neurons from basal forebrain, as happens in AD, results in memory deficits (Scheiderer et al.
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br Methods and results ACE is a Canadian satellite
2024-02-23

Methods and results ACE is a Canadian satellite mission [7] that measures atmospheric SBE 13 HCl spectra in the limb geometry using the Sun as a light source (solar occultation). The ACE orbit (74° inclination to the equator, 650 km altitude) concentrates measurements at high latitudes but also
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Prostate cancer is the second leading cause of cancer relate
2024-02-23

Prostate cancer is the second leading cause of cancer-related death in men in the United States [25]. Similar to pancreatic cancer, prostate cancer has few diagnostic options available, particularly to differentiate indolent from aggressive disease. Axl is also overexpressed in ∼50% of prostate canc
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Having taken a step back from affinity to gain better
2024-02-23

Having taken a step back from affinity to gain better exposure and solubility, we started work to replace the unstable oxazolinone, and address the selectivity over the hERG channel. Keeping in mind the binding mode of the series from crystal structures, triazole was identified as another mildly aci
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