Kinasera OÜ

Tel. +372 5331 1111
The research team lead by CSO of Kinasera, Dr. Asko Uri,
has published various articles related to the development of
bisubstrate inhibitors and their bioanalytical applications.
Please read them for more information.

T. Ivan et al. Bifunctional Ligands for Inhibition of Tight-Binding Protein-Protein Interactions. Bioconjug Chem., (2016), 27(8), 1900-10 (PubMed)

K. Ligi et al. Deoxygenation Increases Photoluminescence Lifetime of Protein-Responsive Organic Probes with Triplet-Singlet Resonant Energy Transfer. J Phys Chem B., (2016), 120(22), 4945-54 (PubMed)

D. Lavogina et al. Co-crystal structures of the protein kinase haspin with bisubstrate inhibitors. Acta Crystallogr F Struct Biol Commun., (2016), 72(Pt 5), 339-45 (PubMed)

GB. Manoharan et al. Combining chemical and genetic approaches for development of responsive FRET-based sensor systems for protein kinases. Biophys Chem., (2016), 211, 39-48 (PubMed)

K. Viht et al. Acetoxymethyl Ester of Tetrabromobenzimidazole-Peptoid Conjugate for Inhibition of Protein Kinase CK2 in Living Cells. Bioconjug Chem., (2015), 26(12), 2324-35 (PubMed)

D. Lavogina et al. Fluorescent photoaffinity probes for mitotic protein kinase Aurora A. Bioorg Med Chem Lett., (2015), 25(16), 3290-4 (PubMed)

GB. Manoharan et al. FRET-based screening assay using small-molecule photoluminescent probes in lysate of cells overexpressing RFP-fused protein kinases. Anal Biochem., (2015), 481, 10-7 (PubMed)

K. Kestav et al. Bisubstrate inhibitor approach for targeting mitotic kinase Haspin. Bioconjug Chem., (2015), 26(2), 225-34 (PubMed)

M. Kriisa et al. Inhibition of CREB phosphorylation by conjugates of adenosine analogues and arginine-rich peptides, inhibitors of PKA catalytic subunit. Chembiochem., (2015), 16(2), 312-9 (PubMed)

R. Ekambaram et al. Benzoselenadiazole-based responsive long-lifetime photoluminescent probes for protein kinases. Chem Commun (Camb)., (2014), 50(31), 4096-8 (PubMed)

D. Lavogina et al. Targeting Plasmodium falciparum protein kinases with adenosine analogue-oligoarginine conjugates. Exp Parasitol., (2014), 138, 55-62 (PubMed)

D. Lavogina et al. Long residence times revealed by Aurora A kinase-targeting fluorescent probes derived from inhibitors MLN8237 and VX-689. Chembiochem., (2014), 15(3), 443-50 (PubMed)

R. Ekambaram et al. Selective Bisubstrate Inhibitors with Sub-nanomolar Affinity for Protein Kinase Pim-1. ChemMedChem., (2013), 8(6), 909-13 (PubMed)

M. Kasari et al. Responsive microsecond-lifetime photoluminescent probes for analysis of protein kinases and their inhibitors. Biochim Biophys Acta (BBA) - Proteins & Proteomics, (2013), 1834(7), 1330-5 (PubMed)

A. Vaasa et al. Time-gated luminescence microscopy with responsive nonmetal probes for mapping activity of protein kinases in living cells. Chem. Commun., (2012), (2012), 48(68), 8595-7 (PubMed)

D. Lavogina et al. Conjugates of 5-isoquinolinesulfonylamides and oligo-D-arginine possess high affinity and selectivity towards Rho kinase (ROCK). Bioorg Med Chem Lett, (2012), 22(10), 3425-30 (PubMed)

M. Kasari et al. Time-gated luminescence assay using nonmetal probes for determination of protein kinase activity-based disease markers. Analytical Biochemistry, (2012), 422(2), 79-88. (PubMed)

E. Enkvist et al. Protein-Induced Long Lifetime Luminescence of Nonmetal Probes. ACS Chem Biol., (2011), 6(10), 1052-1062. (PubMed)

A. Pflug et al. Diversity of Bisubstrate Binding Modes of Adenosine Analogue-Oligoarginine Conjugates in Protein Kinase A and Implications for Protein Substrate Interactions. Journal of Molecular Biology, (2010), 403(1), 66-77. (PubMed)

A. Vaasa et al. Small-molecule FRET probes for protein kinase activity monitoring in living cells. Biochemical and Biophysical Research Communications, (2010), 1804(3), 397(4), 750 - 755. (PubMed)

D. Lavogina et al. Adenosine analogue-oligo-arginine conjugates (ARCs) serve as high-affinity inhibitors and fluorescence probes of type I cGMP-dependent protein kinase (PKGIalpha). Biochimica et Biophysica Acta-Proteins and Proteomics, (2010), 1804(9), 1857 - 1868. (PubMed)

A. Uri et al. Bisubstrate fluorescent probes and biosensors in binding assays for HTS of protein kinase inhibitors. Biochimica et Biophysica Acta (BBA) - Proteins & Proteomics, (2010), 1804(3), 541 - 546. (PubMed)

D. Lavogina et al. Bisubstrate inhibitors of protein kinases: from principle to practical applications. ChemMedChem, (2010), 5(1), 23 - 34. (PubMed)

E. Enkvist et al. Effect of the structure of adenosine mimic of bisubstrate-analog inhibitors on their activity towards basophilic protein kinases. Bioorganic & Medicinal Chemistry Letters, (2009), 19(21), 6098 - 6101. (PubMed)

D. Lavogina et al. Structural Analysis of ARC-Type Inhibitor (ARC-1034) Binding to Protein Kinase A Catalytic Subunit and Rational Design of Bisubstrate Analogue Inhibitors of Basophilic Protein Kinases. Journal of Medicinal Chemistry, (2009), 52(2), 308 - 321. (PubMed)

A. Vaasa et al. High-affinity bisubstrate probe for fluorescence anisotropy binding/displacement assays with protein kinases PKA and ROCK. Analytical Biochemistry, (2009), 385(1), 85 - 93. (PubMed)

H. Raagel et al. Adenosine-oligoarginine conjugate, a novel bisubstrate inhibitor, effectively dissociates the actin cytoskeleton. FEBS Journal, (2008), 275(14), 3608 - 3624. (PubMed)

E. Enkvist et al. Carbocyclic 3'-deoxyadenosine-based highly potent bisubstrate-analog inhibitor of basophilic protein kinases. Bioorganic and Medicinal Chemistry Letters, (2007), 17(19), 5336-5339. (PubMed)

E. Enkvist et al. Conjugation of adenosine and hexa-(D-arginine) leads to a nanomolar bisubstrate-analog inhibitor of basophilic protein kinases. Journal of Medicinal Chemistry, (2006), 49(24), 7150-7159. (PubMed)

K. Viht et al. Surface-plasmon-resonance-based biosensor with immobilized bisubstrate analog inhibitor for the determination of affinities of ATP- and protein-competitive ligands of cAMP-dependent protein kinase. Analytical Biochemistry (2007), 362, 268-277. (PubMed)

K. Viht et al. Fluorometric TLC assay for evaluation of protein kinase inhibitors. Analytical Biochemistry. (2005) 340, 165-70. (PubMed)

K. Viht et al. Liquid-phase synthesis of a pegylated adenosine-oligoarginine conjugate, cell-permeable inhibitor of cAMP-dependent protein kinase. Bioorganic and Medicinal Chemistry Letters. (2003) 13(18), 3035-9. (PubMed)

A. Uri et al. Identification of the ability of highly charged nanomolar inhibitors of protein kinases to cross plasma membranes and carry a protein into cells. Bioorganic and Medicinal Chemistry Letters. (2002) 12(16), 2117-20. (PubMed)

M. Loog et al. Bi-substrate analogue ligands for affinity chromatography of protein kinases. FEBS Letters. (2000) 480(2-3), 244-8. (PubMed)

M. Loog et al. Adenosine-5'-carboxylic acid peptidyl derivatives as inhibitors of protein kinases. Bioorganic and Medicinal Chemistry Letters. (1999) 9(10), 1447-52. (PubMed)

A. Uri et al. A new class of compounds, peptide derivatives of adenosine 5'-carboxylic acid, includes inhibitors of ATP receptor-mediated responses. Bioorganic and Medicinal Chemistry Letters. (1994) 2(10), 1099-105. (PubMed)