PI3Kα x HSP90

Last update 08 May 2025

Basic Info

Related Targets

PI3KαHSP90

Drugs associated with PI3Kα x HSP90

HSP90-PI3K SMDC(SciClone Pharmaceuticals LLC)

Target

HSP90 x PI3Kα

Mechanism

HSP90 inhibitors [+1]

Active Org.

SciClone Pharmaceuticals LLC

Originator Org.

SciClone Pharmaceuticals LLC

Active Indication

Neoplasms

Inactive Indication-

Drug Highest PhasePreclinical

First Approval Ctry. / Loc.-

First Approval Date20 Jan 1800

100 Clinical Results associated with PI3Kα x HSP90

100 Translational Medicine associated with PI3Kα x HSP90

0 Patents (Medical) associated with PI3Kα x HSP90

Literatures (Medical) associated with PI3Kα x HSP90

01 Jun 2025·Current Computer-Aided Drug Design

Exploration of Pharmacological Mechanisms of Dapagliflozin against Type 2 Diabetes Mellitus through PI3K-Akt Signaling Pathway based on Network Pharmacology Analysis and Deep Learning Technology

Article

Author: Chen, Yufan ; Liu, Junru ; Li, Xingxing ; Zhang, Fen ; Liu, Xizhi ; Dong, Yang ; Wu, Jie ; Hu, Guoliang ; Shi, Shuai

Background:Dapagliflozin is commonly used to treat type 2 diabetes mellitus (T2DM). However, research into the specific anti-T2DM mechanisms of dapagliflozin remains scarce.Objective:This study aimed to explore the underlying mechanisms of dapagliflozin against T2DM.Methods:Dapagliflozin-associated targets were acquired from CTD, SwissTargetPrediction, and SuperPred. T2DM-associated targets were obtained from GeneCards and DigSee. VennDiagram was used to obtain the overlapping targets of dapagliflozin and T2DM. GO and KEGG analyses were performed using clusterProfiler. A PPI network was built by STRING database and Cytoscape, and the top 30 targets were screened using the degree, maximal clique centrality (MCC), and edge percolated component (EPC) algorithms of CytoHubba. The top 30 targets screened by the three algorithms were intersected with the core pathway-related targets to obtain the key targets. DeepPurpose was used to evaluate the binding affinity of dapagliflozin with the key targets.Results:In total, 155 overlapping targets of dapagliflozin and T2DM were obtained. GO and KEGG analyses revealed that the targets were primarily enriched in response to peptide, membrane microdomain, protein serine/threonine/tyrosine kinase activity, PI3K-Akt signaling pathway, MAPK signaling pathway, and AGE-RAGE signaling pathway in diabetic complications. AKT1, PIK3CA, NOS3, EGFR, MAPK1, MAPK3, HSP90AA1, MTOR, RELA, NFKB1, IKBKB, ITGB1, and TP53 were the key targets, mainly related to oxidative stress, endothelial function, and autophagy. Through the DeepPurpose algorithm, AKT1, HSP90AA1, RELA, ITGB1, and TP53 were identified as the top 5 anti-targets of dapagliflozin.Conclusion:Dapagliflozin might treat T2DM mainly by targeting AKT1, HSP90AA1, RELA, ITGB1, and TP53 through PI3K-Akt signaling.

13 Feb 2025·Current Pharmaceutical Design

Systems Pharmacology-based Drug Discovery and Active Mechanism of Ganoderma lucidum Triterpenoids for Type 2 Diabetes Mellitus by Integrating Network Pharmacology and Molecular Docking

Article

Author: Li, Wei ; Li, Ming ; Shi, Junkai ; Chen, Jialiang ; Ding, Yan ; Cheng, Chitong ; Ye, Shuhong ; Liu, Zhaofang

Background:Type 2 Diabetes Mellitus (T2DM) is a chronic metabolic disease primarily characterized by insufficient insulin secretion or reduced insulin sensitivity in the body's cells, leading to persistently high blood glucose levels. Ganoderma lucidum triterpenoids, as important secondary metabolites of Ganoderma lucidum, have shown preliminary potential efficacy in the treatment of T2DM according to existing research. However, due to the structural complexity and diversity of these triterpenoid compounds, as well as the intricate interactions between their therapeutic targets and active ingredients, the precise molecular and pharmacological mechanisms remain to be further explored.Objective:In the present research, we aim to fully employ the integrated approach of network pharmacology and molecular docking methodologies, delving deeply into the potential therapeutic targets and their underlying pharmacological mechanisms in the management of T2DM via Ganoderma lucidum triterpenoids.Methods:The active compounds were sourced from prior research and the Traditional Chinese Medicine Systems Pharmacology (TCMSP) database. Their potential targets were predicted with the aid of Swiss Target Prediction. Genes linked to T2DM were gathered from DisGeNET and GeneCards. Using Cytoscape, we established the network connecting active ingredients, targets, and pathways, and the target protein-protein interaction (PPI) network was created using data from the STRING database. The core targets of Ganoderma lucidum triterpenoids underwent gene enrichment analysis via DAVID. Lastly, to validate our chosen Ganoderma lucidum triterpenoids, we conducted molecular docking experiments between the compounds and their targets.Results:A total of 53 Ganoderma lucidum triterpenoids and 116 associated targets were identified. Among these, SRC, MAPK1, MAPK3, HSP90AA1, TP53, PIK3CA, and AKT1 emerged as pivotal targets. We retrieved 447 Gene Ontology (GO) functional annotations and 153 Kyoto Encyclopedia of Genes and Genomes (KEGG) pathways, notably including the PI3K-Akt signaling pathway, Endocrine resistance, Rap1 signaling pathway, and Lipid and Atherosclerosis, which are known to be associated with T2DM. Our findings suggest that Ganoderma lucidum triterpenoids may confer resistance to T2DM through mechanisms related to hyperexcitability, cell death, cell survival, proliferation, differentiation, and inflammation.result:In total, 53 Ganoderma lucidum triterpenoids and 116 associated targets were yielded. SRC, MAPK1, MAPK3, HSP90AA1, TP53, PIK3CA, and AKT1 were defined as core targets. 447 GO function items and 153 KEGG pathways were obtained, including PI3K-Akt signaling pathway, Endocrine resistance, Rap1 signaling pathway, and Lipid and Atherosclerosis that were related to T2DM. Ganoderma lucidum triterpenoids could enable resistance against T2DM by hyperexcitability, cell death, cell survival, proliferation, differentiation, and inflammation.Conclusion:A comprehensive, interdisciplinary, and multi-technology approach has been established, which uncovers the collaborative effects and underlying principles of Ganoderma lucidum triterpenoids in the management and therapy of T2DM from a holistic perspective. This approach provides new insights into the development of novel biological control products for Type 2 Diabetes Mellitus (T2DM) and lays the foundation for future systematic studies on the interactions between Ganoderma triterpenes and different targets, elucidating their primary and secondary pathways for lowering blood glucose.

03 Feb 2025·Journal of Pharmacy and Pharmacology

Mechanism of traditional drug treatment of cancer-related ascites: through the regulation of IL-6/JAK-STAT3 pathway

Article

Author: Zhu, Yongfu ; Ma, Jia ; Huo, Xingxing ; Song, Hang ; Chen, Youmou ; Zhang, Pengcheng ; Sun, Yehan

AbstractContextOur clinical observation found that JiJiaoLiHuang Pill (JJLH), a classic traditional Chinese medicine (TCM) formulation, can significantly reduce the abdominal circumference of patients with malignant ascites, increase urine output, and improve the quality of life of patients, with preliminary efficacy. But, the exact mechanism is not yet clear.ObjectiveBased on the above observations, the potential mechanism of action of the treatment was preliminarily explored.MethodsWe identified active ingredients by constructing a “Chinese medicine ingredient-key target-target” network, and verified them by molecular docking using AutoDock tools and PyMOL. Finally, we conducted preliminary verification of the validated pathways and targets using a mouse model of liver cancer ascites.ResultsNetwork pharmacology analysis obtained the top five active ingredients were quercetin, EUPATIN, kaempferol, Obtucarbamate B, and isorhamnetin and the top five key genes were SRC, HSP90AA1, MAPK1, STAT3, and PIK3CA. Molecular docking showed that all 5 active compounds were closely bound to key target genes (binding energy <−6). The animal experiment results showed that JJLH can significantly reduce abdominal circumference, increase urine output, and exhibit dose-dependent inhibition of the AQP-3/JAK-STAT-3 signaling pathway and the expression of related inflammatory factors.ConclusionsThe JJLH potentially inhibits the recurrence of liver cancer malignant ascites through the AQP-3/JAK-STAT-3 pathway and affects the prognosis of MA patients.

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