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Identification of Selective PPAR-γ Modulators by Combining Pharmacophore Modeling, Molecular Docking, and Adipogenesis Assay.
Author: ByranGowramma, KrishnamurthyPraveen Thaggikuppe, KsNagashree, LiYunwei
Original Abstract of the Article :
The clinically used glitazones (rosiglitazone and pioglitazone) for type 2 diabetes mellitus therapy have been linked to serious side effects such as fluid retention, congestive heart failure, weight gain, bone loss, and an increased risk of bladder cancer. The complete activation of PPAR-γ receptor...See full text at original site
Dr.Camel's Paper Summary Blogラクダ博士について
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* 解説の内容は Health Journal が独自に解釈・作成したものであり、原論文の著者または出版社の見解を反映するものではありません。
引用元:
https://doi.org/10.1007/s12010-022-04190-2
データ提供:米国国立医学図書館(NLM)
PPAR-γ Modulators: Navigating the Desert of Diabetes Treatment
Type 2 diabetes mellitus (T2DM) is a global health crisis, with millions of individuals seeking effective and safe treatments. This research delves into the complex world of peroxisome proliferator-activated receptor gamma (PPAR-γ) modulators, exploring their potential in managing T2DM. The study meticulously combines pharmacophore modeling, molecular docking, and adipogenesis assays to identify novel thiazolidine analogs as selective PPAR-γ modulators (SPPARγMs). The researchers meticulously analyze the structure-activity relationships of these compounds, uncovering promising candidates for the development of safer and more effective T2DM therapies. This research is like a seasoned desert explorer meticulously mapping out the path for a safe and effective journey through the complexities of diabetes treatment.
SPPARγMs: A New Route for Diabetes Management?
The research offers promising findings, identifying several thiazolidine analogs that exhibit partial agonistic activity towards PPAR-γ. These SPPARγMs demonstrate the potential to offer therapeutic benefits similar to full agonists, but with potentially reduced side effects. This research is like discovering a hidden oasis in the vast and unforgiving desert of diabetes research, offering a glimmer of hope for a brighter future.
A Balancing Act: The Importance of Precision
This research underscores the crucial need for precision in drug development, particularly in the context of T2DM. The study emphasizes the potential risks associated with complete PPAR-γ activation and highlights the importance of targeting specific pathways to achieve therapeutic benefits while minimizing side effects. It is like navigating a delicate balance in the desert; a skilled traveler must carefully consider each step to avoid the pitfalls of over-activation or under-activation.
Dr.Camel's Conclusion
This research provides valuable insights into the potential of SPPARγMs for the treatment of T2DM. The findings suggest that these partial agonists may offer an effective and safer alternative to traditional PPAR-γ agonists, paving the way for a more targeted and personalized approach to managing this chronic condition.
Date :
- Date Completed 2023-01-23
- Date Revised 2023-01-23
Further Info :
Related Literature
English
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