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In type diabetic subjects with mean
2021-10-28

In type-2 diabetic subjects with mean baseline glycated hemoglobin A (HbA) of 8.4%, q.d. administration of MK-0893 for 12weeks as a monotherapy resulted in dose-dependent decreases in HbA and FPG. Administration of MK-0893 q.d. at doses of 20, 40, 60, and 80mg led to observed reductions in HbA of 0.
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Recent research has focused on identifying key agonists
2021-10-28

Recent research has focused on identifying key agonists and receptors mediating nutrient-induced GLP-1 and insulin secretion. The long-chain fatty SMIP004 receptor GPR40 is the most abundant GPCR expressed in islet β cells and is also expressed on intestinal L-cells, where it contributes to GLP-1 re
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br Promotion of GLS expression Glutamine metabolism is anoth
2021-10-28

Promotion of GLS2 expression Glutamine metabolism is another target for alteration in ferroptosis. Glutamine is required for the induction of ferroptosis during serum-induced injury after amino acetylcholine receptors starvation [72]. The first step of glutamine catabolism is its conversion to g
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Enasidenib br Experimental br Results and discussion One
2021-10-28

Experimental Results and discussion One of the major challenges of oral drug delivery via nanocarriers is the fairly low efficiency of crossing the intestinal barrier. While there is the possibility of a paracellular transport for polar substances below 1000 Dalton [26], the key mechanism of o
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Structurally HMTs can be broadly categorized
2021-10-28

Structurally, HMTs can be broadly categorized into three functional enzymatic families, the SET (Suppressor of variegation, Enhancer of zeste, Trithorax)-domain- containing methyltransferases, the non-SET DOT1-like (DOT1L) lysine methyltransferases, the PRDM family, containing a PR (PRDI-BF1-RIZ1 ho
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gsk525762 The dramatically reduced expression of CFTR in hum
2021-10-27

The dramatically reduced expression of CFTR in human colorectal cancer tissues identified herein is consistent with our previous findings using human breast cancer tissues, prostate cancer tissues, and colon cancer tissues, and suggests that the loss of CFTR is likely a general phenomenon in epithel
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Several studies have proposed that high levels of
2021-10-27

Several studies have proposed that high levels of KYNA in the TC-I 2000 contribute to cognitive dysfunctions presented by patients who suffer from schizophrenia [30], [31], [32], [33]. Considering that: (i) KYNA is a known GPR35 agonist [2], (ii) cognitive impairments in patients with schizophrenia
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br Experimental br Acknowledgments The authors are grateful
2021-10-27

Experimental Acknowledgments The authors are grateful to Fundamental Scientific Research Fund of Chinese Academy of Medical Sciences (No. 2016ZX350030) for financial support. Introduction 2-Lysophosphatidylcholines (1-acyl-glycero-3-phosphocholines, 2-LPC) are blood derived factors involve
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To effectively evaluate prospective mechanisms by
2021-10-27

To effectively evaluate prospective mechanisms by which chronic HIV infection induces pulmonary fibrotic changes in humans, we confirmed that predisposition to fibrotic change in older individuals could be mimicked in a mouse model. Hydroxyproline is a nonessential amino Cdk1/2 Inhibitor III require
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br Introduction Depression is a prevalent and
2021-10-27

Introduction Depression is a prevalent and disabling psychiatric illness that affects millions of individuals worldwide, resulting in enormous personal suffering and public health costs [1]. Traditional antidepressants such as monoamine oxidase inhibitors (MAOIs) and selective serotonin reuptake
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Work in the Ruiz i Altaba
2021-10-27

Work in the Ruiz i Altaba lab was funded by grants from the Swiss National Science Foundation, the Ligue Suisse Contre le Cancer, the European FP7 Marie-Curie Initial Training Network HEALING, a James McDonnell Foundation 21st Century Science Initiative in Brain Cancer-Research Award and funds from
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Our own search towards aryl imidazole derived GSMs
2021-10-27

Our own search towards aryl-imidazole derived GSMs led to the discovery of the benzimidazole derivative (). It is one of the most potent GSMs to date, suffering however from sub-optimal drug-like properties. More recently, we have described the design and synthesis of bicyclic triazolo-derivatives,
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The extensive worldwide research efforts
2021-10-27

The extensive worldwide research efforts in the decade following FFA1 de-orphaning aimed at developing clinically useful FFA1 agonists were nearly halted after Takeda’s first-in-class agent fasiglifam (TAK-875) was discontinued in phase III of human trials. On the date of submission of this manuscri
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br FAAH mediation of fear and
2021-10-27

FAAH mediation of fear and extinction In addition to being a major target and modulator of stress, the BLA is a critical node within the neural circuitry subserving learned fear behaviors. The BLA is activated during the formation, expression, and extinction of conditioned fear memories, and dama
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Occupying at least of brain volume astroglial cells not
2021-10-27

Occupying at least 50% of PFI 3 volume, astroglial cells not only possess a high level of association in network through gap junctions and direct intercellular communications [28], but also are extensively exposed to extracellular fluid and contribute in shaping different types of synapses [29]. Our
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