Current Drug Targets - Volume 24, Issue 8, 2023
Volume 24, Issue 8, 2023
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The Potential of Mur Enzymes as Targets for Antimicrobial Drug Discovery
The extensive development in the strains of resistant bacteria is a potential hazard to public health worldwide. This necessitates the development of newer agents with the antibacterial property having new mechanisms of action. Mur enzymes catalyze the steps related to the biosynthesis of peptidoglycan, which constitutes a major part of the cell wall in bacteria. Peptidoglycan increases the stiffness of the cell wall, helping it to survive in unfavorable conditions. Therefore, the inhibition of Mur enzymes may lead to novel antibacterial agents that may help in controlling or overcoming bacterial resistance. Mur enzymes are classified into MurA, MurB, MurC, MurD, MurE, and MurF. Until-date, multiple inhibitors are reported for each class of the Mur enzymes. In this review, we have summarized the development of Mur enzyme inhibitors as antibacterial agents in the last few decades.
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Investigational Agents Targeting SGLT1 and SGLT2 in the Treatment of Type 2 Diabetes Mellitus
Authors: Haigang Cui, Xin Luo, Mingwei Chen, Jun Lu and Johnson J. LiuTargeting sodium-dependent glucose transporters (SGLT1 and SGLT2) represents a new class of pharmacotherapy for type 2 diabetes mellitus, a major global health issue with an increasing social and economic burden. Following recent successes in market approvals of SGLT2 inhibitors, the ongoing effort has paved the way for the discovery of novel agents via structure-activity relationship studies, preclinical and clinical testing, including SGLT2 inhibitors, SGLT1/2 dual inhibitors, and selective SGLT1 inhibitors. A growing understanding of the physiology of SGLTs allows drug developers to explore additional cardiovascular and renal protective benefits of these agents in T2DM patients at risk. This review provides an overview of the recent investigational compounds and discusses future perspectives of drug discovery in this area.
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Nano Architect-Based Targeted Delivery Systems for Diabetic Nephropathy: A Review
Authors: Aruna Rawat, Vikas Jhawat and Rohit DuttDiabetes mellitus is a long-lasting disease that is very common in the age group above 20 years and is characterized by hyperglycemia with other complications like Diabetic Nephropathy (DN). The management of DN focuses on mainly four regions: reduction of cardiovascular risks, control of blood glycemic levels, control of the blood pressure (BP) profile, and the use of therenin-angiotensin system (RAS). Although BP management and RAS-acting agents can postpone the onset of DN, they cannot prevent it. In the modern era, nanotechnological interventions have spread rapidly in the field of medicine. Patient defiance is considered important in diabetes management when long-term or continuous management is required. Nano pharmaceuticals have been shown to increase compliance of diabetic patients by providing multiple ways of drug delivery, controlling release profile, increasing biological steadiness, targeting efficacy, and decreasing toxic profile. Nanoscale formulations of botanical antidiabetic molecules improve clinical efficacy and treatment compliance by overcoming associated biopharmaceutical and pharmacokinetic barriers. Therefore, the development of nanopharmaceuticals can be considered to be a possible answer to attain the finest scientific effect of the plant-based anti-diabetic molecule. Nevertheless, further studies are needed to create clinical research-based and therapeutically effective nanoforms of antidiabetic plant-based molecules to combat the most dreaded disease of diabetes and its known present complications.
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Gelatin-based Targeted Delivery Systems for Tissue Engineering
Authors: Xinyue Zhai, Yuqian Wu and Huaping TanGelatin is an attractive material for drug delivery and tissue engineering applications due to its excellent biocompatibility and biodegradability, which has been utilized as cell, drug, and gene carriers. Gelatin is less immunogenic compared to collagen and its precursor and retains informational signals, such as RGD (Arg-Gly-Asp) sequence, thus promoting cell adhesion and proliferation. To tune the mechanical strength and bioactivity, gelatin can be easily modified via chemical reactions and physical methods to obtain various derivatives. Furthermore, gelatin-based biomaterials can be achieved through chemical immobilization of specific molecules and physical combination with other biopolymers. This review focuses on the recent advances of gelatin and its derivatives as biomaterials in the field of drug delivery, including cell scaffolds for tissue engineering applications.
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Deferoxamine Interference in Fibro-inflammation: Additional Action in Control of Obese Adipose Tissue Dysfunction
Introduction: Several studies demonstrated that deferoxamine, an iron chelator, can improve inflammatory alterations in adipose tissue induced by obesity. Obesity alterations in adipose tissue are also associated with tissue remodeling, and deferoxamine has anti-fibrosis action previously described in sites like the skin and liver. Methods: In this work, we analyzed deferoxamine effects on adipose tissue fibro-inflammation during obesity induced by diet in mice. in vitro approaches with fibroblasts and macrophages were also carried out to elucidate deferoxamine activity. Results: Our results demonstrated that in addition to exerting anti-inflammatory effects, reducing the cytokine production in adipose tissue of obese mice and by human monocyte differentiated in macrophage in vitro, deferoxamine can alter metalloproteinases expression and extracellular matrix production in vivo and in vitro. Conclusion: Deferoxamine could be an alternative to control fibro-inflammation in obese adipose tissue, contributing to the metabolic improvements previously described.
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Volumes & issues
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Volume 26 (2025)
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Volume 25 (2024)
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Volume 24 (2023)
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Volume 23 (2022)
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Volume 22 (2021)
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Volume 21 (2020)
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Volume 20 (2019)
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Volume 19 (2018)
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Volume 18 (2017)
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Volume 17 (2016)
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Volume 16 (2015)
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Volume 15 (2014)
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Volume 14 (2013)
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Volume 13 (2012)
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Volume 12 (2011)
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Volume 11 (2010)
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Volume 10 (2009)
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Volume 9 (2008)
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Volume 8 (2007)
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Volume 7 (2006)
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Volume 6 (2005)
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Volume 5 (2004)
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Volume 4 (2003)
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Volume 3 (2002)
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Volume 2 (2001)
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Volume 1 (2000)
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