Protein & Peptide Letters

Prof. Ben M. Dunn  
Department of Biochemistry and Molecular Biology
University of Florida
College of Medicine
P.O. Box 100245
Gainesville, FL


Design of a Peptide Inhibitor of Tyrosine Kinase 2

Author(s): Melissa G. Works, Benben Song, Patrick Kibler, Mary J. Tanga, Amit K. Galande and Annalisa D’Andrea

Affiliation: Center for Immunology and Infectious Diseases, Biosciences Division, SRI International, 333 Ravenswood Avenue, Menlo Park CA 94025, USA.


Tyrosine kinase inhibitors show great promise as clinical therapies, but small molecule inhibitors that are available in the clinic and under development bind to the adenosine triphosphate binding domain of the kinase, potentially limiting efficacy and selectivity. The development of antisense peptide inhibitors is a relatively unexplored area of research, and here we investigate inhibitory peptides specific for the Janus-associated kinase (JAK) family member, tyrosine kinase 2 (TYK2). We have developed peptides that are 2–3 times more selective for TYK2 than other JAK family members, with a TYK2 IC50 of 1.2 μM. In addition, TYK2 inhibitory peptides show specificity for TYK2-mediated functions over JAK1 functions in cell-based assays. These peptides provide a new tool for the development of specific peptide inhibitors for closely related tyrosine kinases.

Keywords: Antisense peptide, JAK, TYK2, tyrosine kinase.

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Article Details

Page: [419 - 425]
Pages: 7
DOI: 10.2174/0929866520666131203101841