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Initially DPP DPP and prolyl tripeptidyl peptidase
2024-01-19
Initially, DPP4, DPP7, and prolyl tripeptidyl peptidase A (PtpA) were the only exopeptidases identified in P. gingivalis. These share substrates according to their altered specificities, as DPP4 is highly specific for Pro at the penultimate position from the N-terminus (P1 position), though it accep
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First investigation of numerous membered ether
2024-01-19
First, investigation of numerous 12-14-membered ether-linked macrocycles revealed that smaller motifs were most lipophilic efficient. Compound (3) (12-membered macrocycle) exhibited good cellular potencies (ALK IC50 = 1.0 nM; ALK-L1196 M IC50 = 20 nM) and the highest LipE (4.4) with picomolar bindin
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A straightforward synthetic pathway was
2024-01-19
A straightforward synthetic pathway was adopted to synthesize the target compounds as outlined in . The starting chloromethylquinazolinones (–) were synthesized from anthranilic SB-505124 hydrochloride in two steps following reported procedures., , , The first step involves chloroacetylation of anth
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Although several studies indicate that
2024-01-19
Although several studies indicate that ALDH2 protects the heart from injury and maladaptive remodeling (reviewed in [11], [12], [13]), accumulating evidence indicates that deficiency of the enzyme could be protective as well. For example, mice expressing the defective Aldh2*2 mutation show lower ald
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br Disclosures br Author contributions
2024-01-19
Disclosures Author contributions Grants This work was supported by National Institutes of Health/National Heart, Lung, and Blood Institute MERIT Award R37 HL040696 to J.A.F. Acknowledgments Introduction The AGC kinases, named after the protein A, G and C kinases, are an evolutionaril
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Growing evidence indicates that GRKs can exert different
2024-01-19
Growing evidence indicates that GRKs can exert different effects within the cell depending on the stimulus, cell type, and localization [97], [121]. In this sense, we were the first to demonstrate a mitochondrial localization for GRK2 [122], later confirmed by other investigators [123], establishing
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br Materials and methods br
2024-01-19
Materials and methods Results Discussions Diabetes is mainly divided into Type 1 diabetes and Type 2 diabetes [16]. Type 2 diabetes, featured by insulin resistance, results from environmental factors and poor eating habits [2]. Type 2 diabetes accounts for more than 95% of the diabetic pati
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Several tertiary prevention studies are currently
2024-01-19
Several tertiary prevention studies are currently underway examining the use of dutasteride for prostate cancer treatment: (1) during expectant management of prostate cancer, (2) after radical prostatectomy in men at high risk for relapse, and (3) in men with metastatic disease. The Reduction by Dut
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DMPO sale The central problem in amnesia developing
2024-01-19
The central problem in amnesia developing following impairment of long-term memory consolidation or reconsolidation is a question of the underlying mechanisms, whether it is caused by impairment of retrieval or memory storage mechanisms [3,8,9,[15], [16], [17], [18]]. To answer this question, severa
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A rational approach for the design of new steroid compounds
2024-01-19
A rational approach for the design of new steroid compounds as possible competitive inhibitors of CYP17 include chemical modification at C17 of the enzyme's natural substrates, pregnenolone (1) and progesterone (2), introducing groups with moderate to strong dipole properties at C20, such as oxime a
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In humans the superior safety profile of lipid associated fo
2024-01-18
In humans, the superior safety profile of lipid-associated formulations is characterized by decreased acute infusion-related reactions and dose-related nephrotoxicity, allowing the administration of larger doses and therefore similar efficacy with fewer administrations. In vitro studies and human cl
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Introduction It has long been
2024-01-18
Introduction It has long been recognized that angiogenesis is critical to the growth, progression, and metastasis of many solid tumor types [1], and thus, drugs targeting the angiogenic pathway have been a topic of clinical investigation in the oncology community for many years. Angiogenesis is reg
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br Androgen interference with the
2024-01-18
Androgen interference with the action of arachidonic BQ-123 metabolites’ actions; the other side of the coin Arachidonic acid, being a polyunsaturated fatty acid present in the phospholipids of the membrane of cells, is highly abundant within the organism. It is mainly involved in cellular signa
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Here we provide evidence that NO contributes
2024-01-18
Here, we provide evidence that NO contributes to changes in synaptic strength, but also offer an explanation as to why previous attempts to link NO to LTP have often failed. Our results describe a model by which cycling AMPARs, held in intracellular pools, are rapidly delivered to the membrane surfa
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Interestingly intermittent high doses of AKT
2024-01-18
Interestingly, intermittent high doses of AKT inhibitors have been shown to be a more effective strategy both clinically and pre-clinically. High doses appear to be required for induction of apoptosis and intermittent schedules overcome the low therapeutic index of these compounds. This is particula
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