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br Concluding Remarks The effects
2024-08-08
Concluding Remarks The effects of point mutations of the four ARs on ligand binding affinities, functional potencies, and efficacies constitute a valuable source of pharmacological information. We analyzed the existing data and mapped it on the collection of available AR crystal structures, allow
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Compounds were profiled for their inhibitory activity agains
2024-08-08
Compounds – were profiled for their inhibitory activity against dipeptidyl peptidase-IV Activity and/or Structure Homologues (DASH) [e.g. DPP2, DPP8 and DPP9] and non-DASH [eg. post-proline cleaving enzyme (PPCE), neutral endopeptidase (NEP), aminopeptidase P (APP), aminopeptidase N (APN)] enzymes.
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ACE inhibition is often thought
2024-08-08
ACE inhibition is often thought to play a central role in the mechanisms of blood pressure reduction in vivo, and most ACE inhibitory (ACEi) peptides were characterized based on in vitro ACE inhibition. A relationship between in vitro ACE inhibition and antihypertensive activity, however, is not app
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br Dihydrotestosterone in adult fish and frogs
2024-08-08
Dihydrotestosterone in adult fish and frogs New perspectives and next directions Similar to other androgens, DHT can modulate reproductive endpoints in both fish and amphibians. However, predicting the effects of DHT can be challenging, as reproductive homeostasis is dependent upon the balance
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The srd a isoforms showed unique expression profiles in earl
2024-08-08
The srd5a isoforms showed unique expression profiles in early FHM development (Fig. 2). Similar to amphibian embryos, there was a high abundance of both srd5a1 and srd5a3 at 1dpf in FHMs, suggesting that mRNA for these enzymes may be maternally deposited and that these enzymes may play a key role in
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Acknowledgements The work was supported by grants from Swedi
2024-08-08
Acknowledgements The work was supported by grants from Swedish Research Council (J.Z.H.) (A.R.M.). We thank Protein Science Facility (PSF), Department of Medical Biochemistry and Biophysics, Karolinska Institute, Stockholm, Sweden. We thank Prof. Ralf Morgenstern (Department for Environmental Medi
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HT modulates cortical and hippocampal
2024-08-08
5-HT modulates cortical and hippocampal pyramidal cell function in a very complex manner, since most 5-HT receptor subtypes (excitatory as well as inhibitory) are expressed on pyramidal b catenin inhibitor as well as GABAergic interneurons that exert inhibitory control over pyramidal cells (Leiser
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The synthesis of compounds in which the
2024-08-08
The synthesis of compounds in which the ethyl linker has been modified to the carbamate and urea derivatives , and is shown in . Thus the diamine was reacted with glycolic Lurasidone HCl to give the alcohol followed by Mitsunobu reaction with phthalimide to give . Deprotection with hydrazine ga
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br Methods br Results br
2024-08-08
Methods Results Discussion Autotaxin has been shown to have effects on major cell types implicated in OA, notably chondrocytes, osteoblasts, osteoclasts, and synoviocytes, through its enzymatic product LPA [20]. However, a paucity of research exists on the involvement of autotaxin in OA. Fi
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br Conflicts of interest br Introduction Phosphatidic acid p
2024-08-08
Conflicts of interest Introduction Phosphatidic e3 ligases phosphatase (PAP) enzymes are responsible for catalyzing the reaction that dephosphorylates phosphatidic acid (PA), which in turn produces diacylglycerol (DAG) and a phosphate group during phospholipid regulation (Fig. 1A) [1]. Subseq
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Co is an essential element
2024-08-08
Co is an essential element for life in minute amounts [5]. The human adult contains about 1.1mg Co with the daily requirement of 0.1μg/day. Co is a component of vitamin B12. Co induces erythropoietin and blocks iodine uptake by the thyroid, controls the transfer of enzymes like homocysteine methyltr
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Two major categories of arginase inhibitors have
2024-08-08
Two major categories of arginase inhibitors have been distinguished (Fig. 3): the first category comprises synthetic arginase inhibitors, which have been developed from the substrate l-arginine [35]; and the second category includes inhibitors derived from natural products [36]. The category of synt
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br Technical Note Fungal spoilage of dairy products remains
2024-08-08
Technical Note Fungal spoilage of dairy products remains a major concern for dairy manufacturers despite the use of preventive and control approaches, including the use of chemical preservatives. Among methods that are increasingly used by industries for microbial contaminant control, biopreserva
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The current antifungal pipeline contains several categories
2024-08-08
The current antifungal pipeline contains several categories of compounds at different stages of development [1], [9], [10], [96]. In Table 1 we summarize the most promising antifungal molecules that are in preclinical and in clinical development. Several compounds in the pipeline are derivatives of
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The habit of prescribing antibiotics just in case
2024-08-08
The habit of prescribing AI-10-49 mg “just-in-case” there is an infection is based on the misguided perception that antibiotics are “safe” drugs and therefore pose little risk to patients. Surgeons need to dispel this myth. In the outpatient setting, antibiotic-associated ADEs account for 19% of all
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