Compositions and methods for inhibiting kinase activity

Kern, Douglas; Zorba, Adelajda

Compositions and methods for inhibiting kinase activity

Patent · 07 March 2022

OSTI ID:1892675

Kern, Douglas; Zorba, Adelajda

The present invention features therapeutic compositions comprising an agent that specifically binds to a PIF pocket of Aurora A kinase and an agent that specifically binds to an ATP-binding site of Aurora A kinase, and the use of the therapeutic compositions to modulate Aurora A kinase for the treatment of cancer.

Research Organization:: Brandeis Univ., Waltham, MA (United States)

Sponsoring Organization:: USDOE

DOE Contract Number:: FG02-05ER15699

Assignee:: Brandeis University (Waltham, MA)

Patent Number(s):: 11,266,616

Application Number:: 16/075,550

OSTI ID:: 1892675

Country of Publication:: United States

Language:: English

References (11)

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A potent and highly specific FN3 monobody inhibitor of the Abl SH2 domain Wojcik, John; Hantschel, Oliver; Grebien, Florian Nature Structural & Molecular Biology, Vol. 17, Issue 4 https://doi.org/10.1038/nsmb.1793	journal	March 2010
Phospho-regulation of human protein kinase Aurora-A: analysis using anti-phospho-Thr288 monoclonal antibodies Ohashi, S.; Sakashita, G.; Ban, R. Oncogene, Vol. 25, Issue 59 https://doi.org/10.1038/sj.onc.1209754	journal	June 2006
Allosteric modulation of AURKA kinase activity by a small-molecule inhibitor of its protein-protein interaction with TPX2 Janeček, Matej; Rossmann, Maxim; Sharma, Pooja Scientific Reports, Vol. 6, Issue 1 https://doi.org/10.1038/srep28528	journal	June 2016
CEP: a conformational epitope prediction server Kulkarni-Kale, U.; Bhosle, S.; Kolaskar, A. S. Nucleic Acids Research, Vol. 33, Issue Web Server https://doi.org/10.1093/nar/gki460	journal	July 2005
Allosteric inhibition of Aurora-A kinase by a synthetic vNAR domain Burgess, Selena G.; Oleksy, Arkadiusz; Cavazza, Tommaso Open Biology, Vol. 6, Issue 7 https://doi.org/10.1098/rsob.160089	journal	July 2016
The epitope space of the human proteome Berglund, Lisa; Andrade, Jorge; Odeberg, Jacob Protein Science, Vol. 17, Issue 4 https://doi.org/10.1110/ps.073347208	journal	April 2008
Monoclonal antibodies directed to different regions of vascular endothelial cadherin extracellular domain affect adhesion and clustering of the protein and modulate endothelial permeability Corada, M. Blood, Vol. 97, Issue 6 https://doi.org/10.1182/blood.V97.6.1679	journal	March 2001
High-Throughput Ligand Discovery Reveals a Sitewise Gradient of Diversity in Broadly Evolved Hydrophilic Fibronectin Domains Woldring, Daniel R.; Holec, Patrick V.; Zhou, Hong PLOS ONE, Vol. 10, Issue 9 https://doi.org/10.1371/journal.pone.0138956	journal	September 2015
Danusertib, an aurora kinase inhibitor Meulenbeld, Hielke J.; Mathijssen, Ron HJ; Verweij, Jaap Expert Opinion on Investigational Drugs, Vol. 21, Issue 3 https://doi.org/10.1517/13543784.2012.652303	journal	January 2012

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