Targeting Src N-Terminal regulatory elements in cancer

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Credit: 2023 Mezquita et al.

“(…) Src is a recognized oncotarget.”

BUFFALO, NY- June 9, 2023 – New research perspectives published in Oncotarget Volume 14 on May 19, 2023 entitled, “Targeting N-terminal Src regulatory elements in cancer.”

The signaling pathways displayed by cancer cells often include physiological components, but the overall result is pathological deregulation. In this new paper, researchers Mezquita Bethlem, Marjorie Reyes-Farias And Michael Pons from Barcelona University And International University of Catalonia discuss the non-receptor Src protein tyrosine kinase as a good example.

“Src, the first oncogene to be discovered, is a prominent member of the Src kinase (SFK) family that includes Fyn, Yes, Blk, Yrk, Fgr, Hck, Lck, and Lyn.”

Src is the first described proto-oncogene and demonstrated player in cancer development, as it influences proliferation, invasion, survival, cancer stem and drug resistance. Src activation is associated with poor prognosis in many types of cancer, but mutations in this protein are rarely observed. Moreover, as a demonstrated cancer target, non-specific inhibition of kinase activity has been shown to be inefficient in the clinic because inhibition of Src in non-cancer cells results in unacceptable toxicity.

Thus, a new target area is needed in Src that can inhibit Src activity only in certain cell types, such as cancer cells, while maintaining normal physiological activity in healthy cells. The Src N-terminal regulatory element (SNRE) includes a poorly studied intrinsically disordered region with unique sequences for each member of the Src family. In this perspective, the researchers discuss non-canonical regulatory mechanisms involving SNREs and their potential use as oncotargets.

“Our group has designed a screening system to search a chemical library for the Src SNRE(88) binder and we are currently following up on promising leads.”

Read the full paper: DOI: https://doi.org/10.18632/oncotarget.28434

Correspondence to: Miquel pons – Email: (email protected)

Keywords: Src family kinases, intrinsically disordered proteins, SNREs, cell-type selective drugs, drug resistance

About Oncotarget: Oncotarget (oncology-focused, peer-reviewed, open access journal) aims to maximize research impact through insightful peer-reviews; blurring the boundaries between specialties by linking different fields of oncology, cancer research, and biomedical sciences; and encourage the application of basic and clinical sciences.

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