TY - JOUR
T1 - Limited inhibition of multiple nodes in a driver network blocks metastasis
AU - Yesilkanal, Ali Ekrem
AU - Yang, Dongbo
AU - Valdespino, Andrea
AU - Tiwari, Payal
AU - Sabino, Alan U.
AU - Nguyen, Long Chi
AU - Lee, Jiyoung
AU - Xie, Xiao He
AU - Sun, Siqi
AU - Dann, Christopher
AU - Robinson-Mailman, Lydia
AU - Steinberg, Ethan
AU - Stuhlmiller, Timothy
AU - Frankenberger, Casey
AU - Goldsmith, Elizabeth
AU - Johnson, Gary L.
AU - Ramos, Alexandre F.
AU - Rosner, Marsha R.
N1 - Funding Information:
National Institutes of Health R01 GM121735-01 Marsha R Rosner National Institutes of Health CA058223 Gary L Johnson University of Chicago Rustandy Fund Marsha R RosnerUniversity of Chicago Women’s Board Grants Fund Ali Ekrem YesilkanalUniversity of Sao Paulo Use of Intelligent Systems Alexandre F Ramos University of São Paulo 18.5.245.86.7 Alexandre F Ramos Coordenação de Aperfeiçoamento de Pessoal de Nível Superior 88881.062174/2014-01 Alexandre F RamosCoordenação de Aperfeiçoa-mento de Pessoal de Nível Superior Alan U Sabino.
Publisher Copyright:
© Yesilkanal et al.
PY - 2021/5
Y1 - 2021/5
N2 - Metastasis suppression by high-dose, multi-drug targeting is unsuccessful due to network heterogeneity and compensatory network activation. Here, we show that targeting driver network signaling capacity by limited inhibition of core pathways is a more effective anti-metastatic strategy. This principle underlies the action of a physiological metastasis suppressor, Raf Kinase Inhibitory Protein (RKIP), that moderately decreases stress-regulated MAP kinase network activity, reducing output to transcription factors such as pro-metastastic BACH1 and motility-related target genes. We developed a low-dose four-drug mimic that blocks metastatic colonization in mouse breast cancer models and increases survival. Experiments and network flow modeling show limited inhibition of multiple pathways is required to overcome variation in MAPK network topology and suppress signaling output across heterogeneous tumor cells. Restricting inhibition of individual kinases dissipates surplus signal, preventing threshold activation of compensatory kinase networks. This low-dose multi-drug approach to decrease signaling capacity of driver networks represents a transformative, clinically relevant strategy for anti-metastatic treatment.
AB - Metastasis suppression by high-dose, multi-drug targeting is unsuccessful due to network heterogeneity and compensatory network activation. Here, we show that targeting driver network signaling capacity by limited inhibition of core pathways is a more effective anti-metastatic strategy. This principle underlies the action of a physiological metastasis suppressor, Raf Kinase Inhibitory Protein (RKIP), that moderately decreases stress-regulated MAP kinase network activity, reducing output to transcription factors such as pro-metastastic BACH1 and motility-related target genes. We developed a low-dose four-drug mimic that blocks metastatic colonization in mouse breast cancer models and increases survival. Experiments and network flow modeling show limited inhibition of multiple pathways is required to overcome variation in MAPK network topology and suppress signaling output across heterogeneous tumor cells. Restricting inhibition of individual kinases dissipates surplus signal, preventing threshold activation of compensatory kinase networks. This low-dose multi-drug approach to decrease signaling capacity of driver networks represents a transformative, clinically relevant strategy for anti-metastatic treatment.
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U2 - 10.7554/eLife.59696
DO - 10.7554/eLife.59696
M3 - Article
C2 - 33973518
AN - SCOPUS:85106552662
SN - 2050-084X
VL - 10
JO - eLife
JF - eLife
M1 - e59696
ER -