Delving into the Latest Updates on Eurofins Advinus BioPharma Services India Pvt Ltd. with Synapse

概览

疾病领域	数量

内分泌与代谢疾病	1

排名前五的药物类型	数量

小分子化药	1

排名前五的靶点	数量

PPARα x PPARγ	1

关联

1

项与 Eurofins Advinus BioPharma Services India Pvt Ltd. 相关的药物

Ligand 10(University of Bari Aldo Moro)

靶点

PPARα x PPARγ

作用机制

PPARα抑制剂 [+1]

在研机构

Adgyl Lifesciences Pvt Ltd. [+3]

原研机构

Eurofins Advinus Ltd. [+2]

在研适应症

2型糖尿病

非在研适应症-

最高研发阶段临床前

首次获批国家/地区-

首次获批日期-

100 项与 Eurofins Advinus BioPharma Services India Pvt Ltd. 相关的临床结果

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0 项与 Eurofins Advinus BioPharma Services India Pvt Ltd. 相关的专利（医药）

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7

项与 Eurofins Advinus BioPharma Services India Pvt Ltd. 相关的文献（医药）

2025-05-01·European Journal of Medicinal Chemistry

A new potent and selective peroxisome proliferator-activated receptor alpha partial agonist displays anti-steatotic effects In vitro and behaves as a safe hypolipidemic and hypoglycemic agent in a diabetic mouse model

Article

作者: Falbo, Emanuele ; Tortorella, Paolo ; Jayaprakash, Venkatesan ; Wackerlig-Damle, Judith ; Laghezza, Antonio ; Singh, Ravi Pratap ; Lavecchia, Antonio ; Ca, Sudeep ; Thomas, Aurélien ; Pattnaik, Ashok Kumar ; Leuci, Rosalba ; Gilardi, Federica ; Paoli, Paolo ; Piemontese, Luca ; Brunetti, Leonardo ; Tambe, Suhas ; Loiodice, Fulvio ; Biswas, Abanish

A rational drug design approach led to the synthesis of three pairs of enantiomers derived from the peroxisome proliferator-activated receptor (PPAR) pan agonist AL29-26, identifying (S)-2 as a potent and selective PPARα partial agonist. Molecular docking and molecular dynamics simulations elucidated the binding modes of (S)-2 within the ligand-binding domains of PPARα and PPARγ. In vitro, (S)-2 demonstrated significant anti-steatotic effects, upregulating key PPARα target genes involved in lipid metabolism. In vivo, (S)-2 exhibited hypolipidemic and antihyperglycemic activity in a diabetic mouse model, outperforming fenofibrate in lowering blood glucose and lipid levels, while showing no toxicity in major organs (artery, kidney, liver, pancreas). The therapeutic effects of ((S)-2 were attributed to its PPARα selectivity, reduced activation of PPARγ, and mild protein tyrosine phosphatase 1B (PTP1B) inhibition. These findings highlight (S)-2 as a promising lead compound for the development of safer and more effective treatments for dyslipidemic type 2 diabetes.

2025-04-01·European Journal of Medicinal Chemistry

Corrigendum to “A chemical modification of a peroxisome proliferator-activated receptor pan agonist produced a shift to a new dual alpha/gamma partial agonist endowed with mitochondrial pyruvate carrier inhibition and antidiabetic properties” [Eur. J. Med. Chem. 275 (2024) 116567]

作者: Loiodice, Fulvio ; Leuci, Rosalba ; Pattnaik, Ashok Kumar ; Paoli, Paolo ; Pecora, Lucia ; Brunetti, Leonardo ; Capelli, Davide ; Wackerlig, Judith ; Laghezza, Antonio ; Sudeep, C A ; Cerchia, Carmen ; Falbo, Emanuele ; Lavecchia, Antonio ; Simic, Stefan ; Montanari, Roberta ; Tortorella, Paolo ; Piemontese, Luca ; Tambe, Suhas ; Jayaprakash, Venkatesan ; Biswas, Abanish ; Singh, Ravi Pratap ; Genovese, Massimo

2024-09-01·European Journal of Medicinal Chemistry

A chemical modification of a peroxisome proliferator-activated receptor pan agonist produced a shift to a new dual alpha/gamma partial agonist endowed with mitochondrial pyruvate carrier inhibition and antidiabetic properties

Article

作者: Leuci, Rosalba ; Loiodice, Fulvio ; Pattnaik, Ashok Kumar ; Paoli, Paolo ; Lavecchia, Antonio ; Pecora, Lucia ; Capelli, Davide ; Brunetti, Leonardo ; Wackerlig, Judith ; Laghezza, Antonio ; Sudeep, C A ; Cerchia, Carmen ; Falbo, Emanuele ; Simic, Stefan ; Montanari, Roberta ; Tambe, Suhas ; Tortorella, Paolo ; Piemontese, Luca ; Jayaprakash, Venkatesan ; Biswas, Abanish ; Singh, Ravi Pratap ; Genovese, Massimo

New analogs of the PPAR pan agonist AL29-26 encompassed ligand (S)-7 showing potent activation of PPARα and -γ subtypes as a partial agonist. In vitro experiments and docking studies in the presence of PPAR antagonists were performed to help interpretation of biological data and investigate the main interactions at the binding sites. Further in vitro experiments showed that (S)-7 induced anti-steatotic effects and enhancement of the glucose uptake. This latter effect could be partially ascribed to a significant inhibition of the mitochondrial pyruvate carrier demonstrating that (S)-7 also acted through insulin-independent mechanisms. In vivo experiments showed that this compound reduced blood glucose and lipid levels in a diabetic mice model displaying no toxicity on bone, kidney, and liver. To our knowledge, this is the first example of dual PPARα/γ partial agonist showing these combined effects representing, therefore, the potential lead of new drugs for treatment of dyslipidemic type 2 diabetes.

100 项与 Eurofins Advinus BioPharma Services India Pvt Ltd. 相关的药物交易

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100 项与 Eurofins Advinus BioPharma Services India Pvt Ltd. 相关的转化医学

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