#DrugDiscovery #Peptides #Inflammatory #IBD #Candidates #SmallMolecule #BuildingBlocks #Proteins #FXR #CRO #FFS #FTE #CMO Based on the results of RNA-seq analysis, we further investigated the therapeutic potential of the combination of compound 33 with 5-ASA. Overall, the results indicated that compound 33 is a promising drug candidate for IBD treatment.
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Daprodustat (JESDUVROQ): The First HIF-PHD Inhibitor Approved for Anemia in the US | https://lnkd.in/gwhaXM7M GSK's daprodustat is the first HIF-prolyl hydroxylase domain (PHD) inhibitor approved for the treatment of anemia in chronic kidney disease (CKD) on dialysis in the US. PHDs have been attractive targets for treating anemia, especially in CKD patients, because the enzymes regulate levels of hypoxia-inducible factors (HIFs) including HIF-2, which induces the production of erythropoietin that in turn stimulates red blood cell production. This article highlights why HIF-PHDs are anemia targets, how daprodustat mimics the natural co-factor 2-oxoglutarate, and how the small molecule drug has similar safety and activity as epoetin alfa, an injected biologic. Article | https://lnkd.in/gwhaXM7M
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Already into the first week of the new year and 2024 is shaping up be a big one for the Peptide Therapeutic Market! This month we'll be walking through some of the biggest predictions and examining how they will impact a variety of patients and diseases. The first one we are excited about is the prediction of more accessible peptide medications through oral administration. Leading the forefront of this prediction are the new family of GLP-1 Receptor Agonist drugs like #Ozempic and #Mounjaro to treat diabetes. We expect we're right around the corner of seeing a grand uptick in new formulas made for oral use rather than simply just injectibles! What new peptide innovations do you think will come to market this year? #peptidetherapeutics #glp1 #trending #peptides #2024
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Celecoxib, a nonsterioidal anti-inflammatory drug works by selectively inhibiting the cyclooxygenase-2 (COX-2) enzyme, which is responsible for prostaglandin synthesis, an integral part of the pain and inflammation pathway. This pharmacologic activity gives celecoxib its analgesic, anti-inflammatory, and antipyretic effects. Warnings: * Nonsteroidal anti-inflammatory drugs (NSAIDs) may increase risk of serious cardiovascular thrombotic events, myocardial infarction (MI), and stroke, which can be fatal. * NSAIDs increase risk of serious gastrointestinal (GI) adverse events, including bleeding, ulceration, and gastric or intestinal perforation, which can be fatal. Sources: https://lnkd.in/dR7KjQrS https://lnkd.in/dSufE4vx
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We stand on the shoulders of those who came before us ... Do we know that in joint inflammation (rheumatoid arthritis or RA), a mediator (IL-6) is increased and may reduce activity of drug metabolizing enzyme (CYP450)? 🤔 What is most intriguing is that tocilizumab, an anti-RA drug, reduces IL-6, reduces IL-6-induced suppression of CYP450 activity and reduces the exposure of a co-administered drug substrate (e.g. statin) (Schmitt et al https://lnkd.in/gFT2Ehuh) This symbolises a unique case of disease-protein drug-small molecular weight drug interaction! Clinical implication: RA patients who are already stabilized on statin need extra care when initiating tocilizumab! 😎 Dr. Edward Morgan received the prestigious Bernard B. Brodie Award in DMD at #ASPET2024, in recognition of his long and impactful career studying the regulation of P450 enzymes by inflammatory stimuli, and the underlying mechanisms. The translational outcome of tocilizumab research is impossible without the pioneering work of Eddie! We all stand on the shoulders of these pioneering giants, don't we agree? 💯 I hope you like what I share in this basic #pharmacokinetics #concepts #Season2 #Post33. Do look out for my next posts on PK concepts. #Pharmacokinetics #Concepts #LearningWithoutBarriers #WeeklyDoseOfPK
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Biotechnologist | Microbiologist | R&D | Research Assistant | Laboratory Technician | GLP | SOP | GMP
"Molecular docking of the bioactive compound Calotropagenin, derived from the plant Calotropis gigantea, targeting the NLRP3 receptor implicated in triggering Rheumatoid Arthritis." (A promising Drug) Binding Score: -7.7 #moleculardocking #drugdesigning #molecularmodelling #bioinformatics #CADD #Arthitis
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Let's talk about proton pump inhibitors (PPI's) and CYP2C19! I apologize for not getting this out yesterday. I was feeling a little draggy after working 3 days in a row, and then I went down the rabbit hole on this subject earlier today. Here are the finer points: To start, there are 6 PPI's available in the U.S. Four of them are primarily metabolized through CYP2C19: lansoprazole (1a), omeprazole (1a), pantoprazole (1a), and dexlansoprazole (1a). For the remaining two, esomeprazole (3) and rabeprazole (2a), this pathway is less important. All are metabolized to some degree through CYP3A4. As we learn from PGx, everyone's liver functions differently for genetic reasons, which leads to many drugs varying in efficacy. In the case of PPI's, a fast metabolizer clears the drug quickly, leading to less effect. For a slow metabolizer, the drug remains in the body longer, leading to better therapeutic effect, but also the potential for increased adverse events with prolonged use (hypomagnesemia, infections, kidney disease, and bone fractures). Here's the estimated breakdown of patient genotypes: UM: 2-5%: consider a 50-100% dosage increase. RM: 2-30%: consider a 50-100% dosage increase. NM: 35-50%: normal dosing. IM: 18-45%: Consider reducing dose by 50% after clinical resolution (~12 weeks). PM: 2-15%: Consider reducing dose by 50% after clinical resolution (~12 weeks). **Notably, 57% of Pacific Islanders and other Oceanic peoples are Poor Metabolizers and another 37% are Intermediate Metabolizers.** For more in-depth information, please check out the CPIC and PharmGKB websites. As always, there's a quiz: 1. Did you find this information helpful? 2. What would you like to hear about next? #pharmacogenomics #MTM #precisionmedicine
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We're excited to introduce our latest service, the Cardiomyocyte Contraction Assay. Here's what our service offers: ✅ Drug Screening: Evaluate pharmacological compounds' effects on cardiomyocyte function, facilitating rapid screening of potential therapeutics for cardiovascular diseases. ✅ Mechanistic Insights: Uncover the underlying molecular mechanisms of drug candidates by studying their impact on cardiomyocyte contractility, providing critical insights into their mode of action. ✅ Safety Assessment: Assess the cardiotoxic effects of drugs and environmental toxins early in the drug development process, ensuring the safety and efficacy of your compounds. ✅ Flexibility: Our Cardiomyocyte Contraction Assay is available for both Rat Primary Cardiomyocytes and hiPSC-CMs, providing flexibility and adaptability to suit your research needs. #cardiomyocytes #safetypharmacology #drugdiscovery #contraction
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Revolutionize Your Rheumatoid Arthritis Research! Discover how Central BioHub’s high-quality biospecimen can enhance your autoimmune and rheumatoid arthritis (RA) studies! We provide serum, plasma and urine samples that are tested for common RA specific lab parameters like anti-CCP, RF, CRP, ESR and others, ensuring they meet the rigorous demands of your research. Sample Specifications 🧪 – · Matrix: Serum, Plasma, Urine · Lab Parameter: anti-Cyclic citrullinated peptide (CCP) / anti-Citrullinated protein antibodies (ACPA) | Rheumatoid factor (RF) | C-reactive protein (CRP) | Erythrocyte sedimentation rate (ESR) | · ICD-10: M05. + | M06. + Explore our online marketplace and discover how Central BioHub's Rheumatoid Arthritis samples can make a difference. · https://lnkd.in/eGwyE-PX #ResearchAndDevelopment #Biobanking #Diagnostics #Onlinemarketplace #DrugDiscovery #BiomedicalResearch #ClinicalResearch #IVD #Biotechnology #Healthcare #Pharma #Biomedicine
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Benzene is classified as a human carcinogen. It works by causing cells not to work correctly. Exposure to benzene can occur by inhalation, orally, and through the skin and it potentially can result in cancers including leukemia and blood cancer of the bone marrow and blood disorders which can be life threatening. It can damage the immune system by changing blood levels of antibodies and causing the loss of white blood cells which is the body’s defense against infections. There was a recall of TING 1% (tolnaftate) Athlete’s Foot Spray by Insight Pharmaceuticals because a recent review by their manufacturer and their third-party lab found that samples from two lots of the product contained elevated levels of benzene. While benzene is not an ingredient in any Ting Antifungal Spray products, the review showed that unexpected levels of benzene came from the propellant that sprays the product out of the can. At SBL, we develop and carry out methods for detecting, controlling and quantifying irregularities in pharmaceutical products. Contact us today for a consultation! Your safety is our priority and with this information we hope you can make informed decisions on what you consume. #STAYSAFE #STAYHEALTHY #STAYINFORMED
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#HighlyCitedPapers 📝 Non-Insulin Novel Antidiabetic Drugs Mechanisms in the Pathogenesis of COVID-19 — Salmen, et al. In this paper, the authors aimed to analyze the published data and to realize an update about the use and pathogenesis of the novel antidiabetic drugs, respectively, dipeptidyl peptidase-4 inhibitors (DPP-4i), glucagon-like peptide-1 receptor agonists (GLP-1 Ra), and sodium-glucose co-transporter-2 inhibitors (SGLT-2i), in patients with type 2 diabetes mellitus (T2DM) and coronavirus disease (COVID-19). Full text is available 👇 https://lnkd.in/d4HkYhWn #medicine #health #research #science
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