PI3Kα x HSP90

Last update 23 Jan 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 Feb 2025·Journal of Ethnopharmacology

Chrysotoxine regulates ferroptosis and the PI3K/AKT/mTOR pathway to prevent cervical cancer

Article

Author: Guo, Tianyao ; Lu, Xingjun ; Feng, Liyuan ; Meng, Qingxin ; Wu, Ben ; Guo, Zhenyu ; Peng, Xiaozhen ; Zhou, Ji

ETHNOPHARMACOLOGICAL RELEVANCEDendrobium (commonly known as Shihu in China), a traditional Chinese medicinal herb recognized in the Pharmacopoeia of China (2020 edition), boasts a rich history of medicinal application. Extensive research has been conducted on its Chinese medicinal prescription due to its demonstrated anti-tumour effects in clinical settings. Dendrobium is comprised of a diverse range of chemical compounds, notably the Bibenzyls, Erianin, and Gigantol, which have exhibited significant inhibitory and therapeutic effects on cervical cancer, thereby suggesting potential therapeutic value. However, the comprehensive investigation of Chrysotoxine, a naturally occurring active ingredient of Bibenzyls in Dendrobium, remains incomplete in treatment of cervical cancer.AIMS OF THE STUDYThis study aimed to conduct a comprehensive investigation of Chrysotoxine and its regulatory impact on ferroptosis in cervical cancer.MATERIALS AND METHODSInitially, the effects of chrysotoxine on the cervical cancer cell line HeLa were assessed using CCK-8, transwell, colony formation, and flow cytometry to evaluate cell proliferation, invasion, migration, and apoptosis. Subsequently, network pharmacology and molecular docking techniques were employed to identify the molecular targets of chrysotoxine in cervical cancer. Finally, confocal microscopy assessed the expression levels of ROS and lipid compounds in response to chrysotoxine treatment, and the influence of chrysotoxine on signaling pathways was investigated using Western blot analysis, guided by KEGG pathway analysis.RESULTSOur cell-based experiments revealed that CTX effectively suppresses the cell proliferation, migration, invasion, and apoptosis in CC. Subsequently, we comprehensively analyzed that HSP90AA1, ESR1, PIK3CA, mTOR and MAPK1 may be the possible targets of CTX in CC by combining network pharmacology with molecular docking techniques. Finally, we observed that CTX enhances the production of intracellular ROS and excessive lipid peroxides. Simultaneously, we detected that CTX promotes ferroptosis-based p53/GPX4/SLC7A11 pathway and inhibits PI3K/AKT/mTOR pathway-induced cell death of CC by Western blot.CONCLUSIONOur study indicates that chrysotoxine shows promise as a novel medication for treating CC. The findings provide a scientific foundation for the regulation of cervical cancer by chrysotoxine, presenting new insights into the application of traditional Chinese medicine for fighting CC.

02 Jan 2025·Combinatorial Chemistry & High Throughput Screening

Verification of Qianlong Shutong Formula in the Treatment of Benign Prostatic Hyperplasia

Article

Author: Zhu, Min ; Huang, Shu-ping ; Chen, Yu ; Zhang, Ze-chao ; Shang, Chang-jie ; Wei, Zhi-feng

Aims:To investigate the mechanisms through which Qianlong Shutong Formula (QLSTF) exerts its effects on the management of benign prostatic hyperplasia (BPH).Background:BPH is a prevalent condition among older men and poses significant management challenges due to the limited effectiveness and potential side effects associated with current treatment options. QLSTF, a traditional Chinese medicine, has been utilized in the treatment of BPH; however, its mechanism of action remains inadequately understood.Objective:This study aimed to identify potential therapeutic targets of QLSTF for the management of BPH through the application of network pharmacology and subsequent experimental validation.Methods:QLSTF compounds were identified utilizing liquid chromatography-mass spectrometry (LC-MS). Potential targets of QLSTF, as well as BPH-related targets, were retrieved from public databases. Crucial bioactive ingredients, potential targets, and signaling pathways were acquired through bioinformatics analysis, including protein-protein interaction (PPI), as well as the Gene Ontology (GO) and the Kyoto Encyclopedia of Genes and Genomes (KEGG) analysis. Subsequently, molecular docking was carried out to predict the combination of active compounds with core targets. Lastly, in vitro and in vivo experiments were conducted to further verify the findings.Results:A total of 52 bioactive ingredients of QLSTF and 760 QLSTF-BPH-related targets were screened. Bioinformatics analysis revealed that Afzelin, Ononin, Glycitin, Emodin and Erythritol may be potential candidate agents. AKT1, SRC, STAT3, GRB2, HRAS, MAPK3, PIK3CA, PIK3R1, HSP90AA1, and EP300 could become potential therapeutic targets. PI3KAKT signaling pathway might play an important role in QLSTF against BPH. Moreover, molecular docking suggested that Afzelin, Ononin, Glycitin, Emodin, and Erythritol combined well with AKT1, SRC, STAT3, HRAS, MAPK3, PIK3CA, and PIK3R1, respectively. In vitro and in vivo experiments showed that QLSTF could inhibit the proliferation of cells, as well as the PI3K-Akt signaling pathway, which further confirmed the prediction by network pharmacology strategy and molecular docking.Conclusions:QLSTF may exert its therapeutic effects on BPH by modulating the PI3K/AKT signaling pathway and inhibiting glandular hyperplasia. This study offers valuable insights into the therapeutic targets of QLSTF in the management of BPH.

01 Jan 2025·Advanced Biology

Mechanism of Action of Tongjiang Mixture for Treating Reflux Esophagitis: A Study Using Serum Pharmacochemistry and Network Pharmacology

Article

Author: Weiwei, Tao ; Wanli, Liu ; Yi, Gu ; Yuzhen, Huang ; Yan, Wang ; Lu, Yang ; Lili, Wu

AbstractTongjiang Mixture (TJM) is a traditional Chinese formula for treating reflux esophagitis (RE). Nevertheless, its active ingredients and potential pharmacological mechanisms are not yet clearly elucidated. This study will identify the active ingredients of TJM using serum pharmacochemistry and to elucidate the mechanism on RE through network pharmacology. The blood‐borne ingredients of TJM are identified by the Ultra‐performance liquid chromatography‐quadrupole‐time of flight‐mass spectrometer. Subsequently, a “compound‐target‐disease” network is established and obtained core targets associated with TJM and RE. Then, the potential signaling pathways are forecasted through the Kyoto Encyclopedia of Genes and Genomes pathway enrichment analysis. Finally, the rat model of RE is established to verify the results predicted by network pharmacology through animal experiments. Fifteen blood‐borne ingredients of TJM are identified, with eight active ingredients‐namely Tangeretin, Tricin, Palmati, Berberine, Limonin, Evodiamine, Tetrahydropalmatine and Rutecarpine – making significant contributions to its efficacy. Moreover, TJM is predicted to act on 193 targets related to RE, involving AKT1, HSP90AA1, PIK3CA, and other targets, which enriches mainly in PI3K/AKT /NF‐κB signaling. Additionally, TJM can alleviate inflammation of the esophageal mucosa, reduce pathological damage, and increase gastric pH. It can downregulate PI3K, AKT, and NF‐κB mRNA transcription levels and reduce the protein expression of PI3K, AKT, and NF‐κB. Furthermore, it can inhibit the overproduction of IL‐6, TNF‐α and IL‐17. TJM can alleviate immune‐inflammatory responses and ameliorate RE by restraining the PI3K/AKT pathway and its downstream NF‐κB.

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