Last update 01 Nov 2024

hERG x CD29

Last update 01 Nov 2024

Basic Info

Related Targets

hERGCD29

Drugs associated with hERG x CD29

scDb-hERG1-β1

Target

CD29 x hERG

Mechanism

CD29 modulators [+1]

Active Org.

University of Florence

Originator Org.

University of Florence

Active Indication

Pancreatic Ductal Adenocarcinoma

Inactive Indication-

Drug Highest PhasePreclinical

First Approval Ctry. / Loc.-

First Approval Date20 Jan 1800

100 Clinical Results associated with hERG x CD29

100 Translational Medicine associated with hERG x CD29

0 Patents (Medical) associated with hERG x CD29

Literatures (Medical) associated with hERG x CD29

09 Aug 2019·Current Pharmaceutical Design

Effects of As2O3 and Resveratrol on the Proliferation and Apoptosis of Colon Cancer Cells and the hERG-mediated Potential Mechanisms

Article

Author: Zhang, Guocui ; Li, Baoxin ; Yan, Caichuan ; Zhang, Yuhao ; Zhao, Xin ; Li, Fengmei ; Li, Yuexin ; Wang, Fang ; Li, Yang ; Li, Mingzhu

Background:As2O3 and resveratrol have been widely considered to be effective in anti-cancer therapies and the underlying mechanisms have been reported extensively. However, the combined treatment effect and potential target of As2O3 and resveratrol in the treatment of tumors remains elusive. The purpose of this study was to investigate the benefits and efficacy of As2O3 in combination with resveratrol in the treatment of colon cancer, as well as looking for new targets that could provide alternative explanation of the efficacy of drugs.Methods:The proliferation of cancer cells was measured by the MTT and EdU staining assay, while the apoptosis of cancer cells was determined by the flow cytometry. Western blot and immunoprecipitation were performed to measure the expression levels of proteins and the interaction between hERG and integrin β1, respectively.Results:In this study, we found that both As2O3 and resveratrol can effectively inhibit cell proliferation and promote cell apoptosis in colon cancer, and the combined effect of the two drugs on colon cancer cells is more preeminent. The combination of As2O3 with resveratrol, on the one hand reduced the expression of hERG channels on the membrane, and on the other hand weaken the binding between hERG and integrin β 1, which may be the main cause of downstream signaling pathways alterations, including the activation of the apoptotic pathway.Conclusion: Taken together, hERG, as a subunit of potassium ion channel on the cell membrane, is highly likely to be involved in the As2O3 and resveratrol induced intracellular signaling cascade disorder, and this novel signaling pathway that sustains the progression of colon cancer may be a promising therapeutic target for human colon cancer treatment in the future.

01 Feb 2016·Cancer ResearchQ1 · MEDICINE

SIGMAR1 Regulates Membrane Electrical Activity in Response to Extracellular Matrix Stimulation to Drive Cancer Cell Invasiveness

Q1 · MEDICINE

Article

Author: Popa, Alexandra ; Alcaraz-Perez, Francisca ; Paquet, Agnès ; Soriani, Olivier ; Martial, Sonia ; Presta, Marco ; Tichet, Mélanie ; Pellissier, Bernard ; Crottès, David ; Cayuela, Maria Luisa ; Rapetti-Mauss, Raphael ; Tartare-Deckert, Sophie ; Martin, Patrick ; Borgese, Franck ; Guizouarn, Hélène ; Loubat, Agnès ; Gariano, Giuseppina

AbstractThe sigma 1 receptor (Sig1R) is a stress-activated chaperone that regulates ion channels and is associated with pathologic conditions, such as stroke, neurodegenerative diseases, and addiction. Aberrant expression levels of ion channels and Sig1R have been detected in tumors and cancer cells, such as myeloid leukemia and colorectal cancer, but the link between ion channel regulation and Sig1R overexpression during malignancy has not been established. In this study, we found that Sig1R dynamically controls the membrane expression of the human voltage-dependent K+ channel human ether-à-go-go-related gene (hERG) in myeloid leukemia and colorectal cancer cell lines. Sig1R promoted the formation of hERG/β1-integrin signaling complexes upon extracellular matrix stimulation, triggering the activation of the PI3K/AKT pathway. Consequently, the presence of Sig1R in cancer cells increased motility and VEGF secretion. In vivo, Sig1R expression enhanced the aggressiveness of tumor cells by potentiating invasion and angiogenesis, leading to poor survival. Collectively, our findings highlight a novel function for Sig1R in mediating cross-talk between cancer cells and their microenvironment, thus driving oncogenesis by shaping cellular electrical activity in response to extracellular signals. Given the involvement of ion channels in promoting several hallmarks of cancer, our study also offers a potential strategy to therapeutically target ion channel function through Sig1R inhibition. Cancer Res; 76(3); 607–18. ©2015 AACR.

01 Feb 2001·Journal of Biological Chemistry

HERG K+ Channels Activation during β1Integrin-mediated Adhesion to Fibronectin Induces an Up-regulation of αvβ3 Integrin in the Preosteoclastic Leukemia Cell Line FLG 29.1

Article

Author: Giovanna Hofmann ; Simone Polvani ; Paola Defilippi ; Alessia Cherubini ; Serena Pillozzi ; Vera Solazzo ; Olivia Crociani ; Annarosa Arcangeli ; Elena Lastraioli ; Laura Gragnani ; Benedetta Bartolozzi ; Leonardo Guasti ; Massimo Olivotto ; Pietro Antonio Bernabei ; Enzo Wanke ; Barbara Rosati

Integrin receptors have been demonstrated to mediate either "inside-to-out" and "outside-to-in" signals, and by this way are capable of regulating many cellular functions, such as cell growth and differentiation, cell migration, and activation. Among the various integrin-centered signaling pathways discovered so far, we demonstrated that the modulation of the electrical potential of the plasma membrane (V(REST)) is an early integrin-mediated signal, which is related to neurite emission in neuroblastoma cells. This modulation is sustained by the activation of HERG K(+) channels, encoded by the ether-à-go-go-related gene (herg). The involvement of integrin-mediated signaling is being discovered in the hemopoietic system: in particular, osteoclasts are generated as well as induced to differentiate by interaction of osteoclast progenitors with the stromal cells, through the involvement of integrin receptors. We studied the effects of cell interaction with the extracellular matrix protein fibronectin (FN) in a human leukemic preosteoclastic cell line (FLG 29.1 cells), which has been demonstrated to express HERG currents. We report here that FLG 29.1 cells indeed adhere to purified FN through integrin receptors, and that this adhesion induces an osteoclast phenotype in these cells, as evidenced by the appearance of tartrate-resistant acid phosphatase, as well as by the increased expression of CD51/alpha(v)beta(3) integrin and calcitonin receptor. An early activation of HERG current (I(HERG)), without any increase in herg RNA or modifications of HERG protein was also observed in FN-adhering cells. This activation is apparently sustained by the beta(1) integrin subunit activation, through the involvement of a pertussis-toxin sensitive G(i) protein, and appears to be a determinant signal for the up-regulation of alpha(v)beta(3) integrin, as well as for the increased expression of calcitonin receptor.

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