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Salinas Parra, N.

Publications and source records attributed to Salinas Parra, N..

2 recordsLinked to original sources

Dissection of Gαs and Hedgehog signaling crosstalk reveals therapeutic opportunities to target adenosine receptor 2b in Hedgehog-dependent tumors

Basal cell carcinoma (BCC), the most common human cancer, is driven by hyperactivation of Hedgehog Smoothened (SMO) and GLI transcription. Gs and protein kinase A (PKA) negatively regulate Hedgehog signaling, offering an alternative BCC development and treatment pathway. Here, using histology alongside bulk and single-cell RNA sequencing, we find that mouse BCC-like tumors that originate from Gs pathway inactivation are strikingly similar to those driven by canonical Hedgehog SMO. Interestingly, mutations that reduce Gs and PKA activity are present in human BCC. Tumors from Gs pathway inactivation are independent of the canonical Hedgehog regulators SMO and GPR161, establishing them as an SMO-independent oncogenic Hedgehog signaling model. Finally, we demonstrate that activation of the Gs-coupled adenosine 2B receptor counteracts oncogenic SMO, reducing Hedgehog signaling and tumor formation and offering a potential therapeutic strategy for BCC.

cancer biology↗

YAP1-TAZ/TEAD transcriptional networks restrain differentiation downstream of oncogenic Hedgehog-SMO activity

Disruption of the transcriptional activity of the Hippo pathway members YAP1 and TAZ has become a major target for cancer treatment. However, detailed analysis of the effectivity and networks affected by YAP1/TAZ transcriptional targeting are limited. Here, by comparing the effects of YAP1/TAZ knockdown with those resulting from TEAD blockage, we unveil the consequences of YAP1/TAZ transcriptional inhibition in cancer cells. We utilize TEADi, an inhibitor of the binding of YAP1 and TAZ with their main transcriptional target TEAD. In a mouse model of basal cell carcinoma (BCC) driven by the smoothened oncogene (SmoM2), TEADi and YAP1/TAZ knockdown lead to reduced proliferation and increased differentiation of tumor cells both in vitro and in vivo. We find that TEAD transcriptional networks inactivate differentiation in BCC by regulating KLF4. Furthermore, we determine YAP1/TAZ TEAD-independent effects in cancer cells that impact Stat3 and NF-{kappa}B gene networks. Our results reveal the TEAD dependent and independent roles of YAP1/TAZ in cancer and expose potential pitfalls for targeting TEAD transcription in tumors.

cancer biology↗