Top 3 Biorxiv Papers Today in Pharmacology And Toxicology


2.006 Mikeys
#1. In silico screening of GMQ-like compounds reveals guanabenz and sephin1 as new allosteric modulators of acid-sensing ion channel 3
Gerard Callejo, Luke A Pattison, Jack C Greenhalgh, Sampurna Chakrabarti, Evangelia Andreopoulou, James RF Hockley, Ewan Smith, Taufiq Rahman
Acid-sensing ion channels (ASICs) are voltage-independent cation channels that detect decreases in extracellular pH. ASICs are involved in pain, fear, learning, neurodegeneration after ischemic stroke, and mechanosensation. Of all the ASIC subunits, ASIC3 has been suggested as the key sensor of acid-induced pain and has also been shown to have a crucial role in different models of inflammatory pain including models of rheumatoid arthritis. Interestingly, ASIC3 has been proposed to play a dual role in arthritis: lack of ASIC3 ameliorates pain, but increases inflammatory processes in the arthritic joint. Therefore, the identification of new ASIC3 modulators and the mechanistic understanding of how these compounds modulate ASIC3 could be important for the development of new strategies to counteract the detrimental effects of dysregulated ASIC3 activity in inflammation. Here, we report the identification of novel ASIC3 modulators based on the ASIC3 specific agonist, 2-guanidine-4-methylquinazoline (GMQ). Through a GMQ-guided in silico...
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biorxivpreprint: In silico screening of GMQ-like compounds reveals guanabenz and sephin1 as new allosteric modulators of acid-sensing ion channel 3 https://t.co/1E26wvJhKI #bioRxiv
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Authors: 8
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1.955 Mikeys
#2. Nutritive diet becomes unhealthy if taken in a wrong ratio: Scientific validation of Ayurvedic concept of "incompatible diet" (Virrudh Aahar)
Prerana Aditi, Shivani Srivastava, Harsh Pandey, Yamini Bhusan Tripathi
Honey and ghee is an important constituent of our diet. Honey contain about 200 components in its which play an important role as antioxidative, anti-inflammatory, antimicrobial, wound healing and sunburn, etc. Ghee has also many essential constituents such as phospholipids, PUFA, fat-soluble vitamins, etc. It is mention in Charak Samhita that equal ratio of honey and ghee when taken in food become toxic to health. This study was designed to explore the mechanism of toxicity through the biochemical and histological parameter. For this study, 24 Charles foster rats were taken and divided into four groups (n=6) normal, honey, ghee, and honey+ghee (1:1). After 60 days rats were sacrificed. Weight loss, Hair loss and red patches on ear were found on honey+ghee fed rats. LFT, amadori test, AGE, UV, glucose, DPP-4 and LPO were found significantly increased in honey+ghee group. SOD, Catalase, GSH, ABTS+, GLP-1, GIP-1, ACB and HB were found significantly decreased in honey+ghee group. No changes were found in RFT. H&E show normal...
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1.946 Mikeys
#3. A NanoBRET-based binding assay for Smoothened allows real time analysis of small-molecule ligand binding and distinction of two separate ligand binding sites for BODIPY-cyclopamine
Pawel Kozielewicz, Carl-Fredrik Bowin, Gunnar Schulte
Background and Purpose: Smoothened (SMO) is a GPCR that mediates hedgehog signaling. Hedgehog binds the Patched, which in turn regulates SMO activation. Overactive SMO signaling is oncogenic and is therefore a clinically established drug target. Here, we establish a nanoluciferase bioluminescence resonance energy transfer (NanoBRET)-based ligand binding assay for SMO providing a sensitive and high throughput-compatible addition to the toolbox of GPCR pharmacologists. Experimental Approach: In the NanoBRET-based binding assay, SMO is N terminally tagged with nanoluciferase (Nluc) and binding of BODIPY-cyclopamine is assessed by quantifying resonance energy transfer between receptor and ligand. The assay allows kinetic analysis of ligand-receptor binding in living HEK293 cells and competition binding experiments using commercially available SMO ligands (SANT-1, cyclopamine-KAAD, SAG1.3 and purmorphamine). Key Results: The NanoBRET binding assay for SMO is sensitive and superior to purely fluorescence-based binding assays....
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