Establishing selectivity of FAK-paxillin PPI inhibitor using pulldown proteomics and a focal adhesion protein selectivity panel.

Hunter O'Brien, Brock Hay, Huzaifah Sheikh, Liam McCreary, Krishna Parsawar, Timothy Marlowe

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Article in Biochemistry and biophysics reports, 2026. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.

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6 authors.

Hunter O'BrienDepartment of Internal Medicine, University of Arizona College of Medicine - Phoenix, 475 N. 5th Street, Phoenix, AZ, 85004, USA.

Brock HayDepartment of Internal Medicine, University of Arizona College of Medicine - Phoenix, 475 N. 5th Street, Phoenix, AZ, 85004, USA.

Huzaifah SheikhDepartment of Internal Medicine, University of Arizona College of Medicine - Phoenix, 475 N. 5th Street, Phoenix, AZ, 85004, USA.

Liam McCrearyDepartment of Internal Medicine, University of Arizona College of Medicine - Phoenix, 475 N. 5th Street, Phoenix, AZ, 85004, USA.

Krishna ParsawarUniversity of Arizona Analytical & Biological Mass Spectrometry Facility, 1657 E. Helen Street, Tucson, AZ, 85721, USA.

Timothy MarloweDepartment of Internal Medicine, University of Arizona College of Medicine - Phoenix, 475 N. 5th Street, Phoenix, AZ, 85004, USA.

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

UA-2012 (and related non-myristoylated analog UA-1907) is a lead alpha-helical cyclic peptide which inhibits the focal adhesion kinase (FAK)-paxillin protein-protein interaction (PPI) and is being evaluated for the treatment of cutaneous melanoma. However, the development of an empirical approach to measure PPI inhibitor selectivity remains an important need. We report the development of a pulldown-MS proteomic approach, including a custom synthesized non-myristoylated UA-1907-agarose probe, to evaluate the binding selectivity of candidate FAK PPI inhibitors. Melanoma lysates were probed with UA-1907-conjugated agarose beads and eluted associated proteins were analyzed through untagged mass-spectroscopy proteomics. The identified proteins led to the development of a custom focal adhesion (FA) selectivity panel comprised of recombinant VinT, VinH, PARVA, PARVB, Talin-1 Rod 8, and the FAK FAT domain. Surface plasmon resonance (SPR) screening of these FA proteins against UA-1907 determined that only the FAK-FAT domain has a nanomolar binding affinity (K

Indexed as

Drug selectivityInteractomeMass spectrometryPeptide therapeuticProteomicsSurface plasmon resonance

Identifiers

PMID41492449

DOI10.1016/j.bbrep.2025.102410

PMCPMC12765108

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