Publications

At PamGene we have developed a robust and unique microarray technology for multiplex kinase activity profiling. Our technology reveals the bigger picture of cellular signaling and provides mechanistic insights needed to fully understand diseases and cell alterations. On this page you will find a selection of scientific publications where PamGene’s technology has been applied.

Publications

At PamGene we have developed a robust and unique microarray technology for multiplex kinase activity profiling. On this page you will find a selection of scientific publications where PamGene’s technology has been applied.

Target interaction
Biochemical characterization
Compound-based patient stratification
Diseases model characterization
Pathway elucidation
Retance mechanism

Download our flyer with select recent publications highlighting PamGene’s kinome profiling Applications

Blood-based kinase activity profiling: a potential predictor of response to immune checkpoint inhibition in metastatic cancer

Hurkmans DP, Verdegaal EME, Hogan SA et al.

Journal for ImmunoTherapy of Cancer, (2020)

Blood-Based Multiplex Kinase Activity Profiling as a Predictive Marker for Clinical Response to Checkpoint Blockade in Advanced NSCLC.

Hurkmans, D. et al. P2.04-06

J. Thorac. Oncol. 14, S709 (2019).

Blood-based multiplex kinase activity profiling as a predictive marker for clinical response to checkpoint blockade in advanced melanoma.

Hurkmans, D. et al.

J. Clin. Oncol. 36, 9579 (2018).

Phosphoproteomic and Kinomic Signature of Clinically Aggressive Grade I (1.5) Meningiomas Reveals Rb1 signaling as a Novel Mediator and Biomarker.

Parada, C. A. et al.

Clin. Cancer Res. clincanres (2020)

Systemic analysis of tyrosine kinase signaling reveals a common adaptive response program in a HER2-positive breast cancer.

Schwill, M. et al.

Sci. Signal. 12, (2019).

Identification of new possible targets for leukemia treatment by kinase activity profiling.

Ter Elst, A. et al.

Leuk. Lymphoma 52, 122–130 (2011).

Inactive immune pathways in triple negative breast cancers that showed resistance to neoadjuvant chemotherapy as inferred from kinase activity profiles.

Sawada, T. et al.

Oncotarget 9, 34229–34239 (2018).

Profiling activity of cellular kinases in migrating T-cells.

Chirumamilla, C. S. et al.

Methods Mol. Biol. 1930, 99–113 (2019).

Differential Kinase Activation in Peripheral Blood Mononuclear Cells from Non-Small-Cell Lung Cancer Patients Treated with Nivolumab.

Noé, G. et al.

Cancers (Basel). 11, 762 (2019).

Lithium effects on serine-threonine kinases activity: high throughput Kinomic Profiling of lymphoblastoid cell lines from excellent-responders and non-responders bipolar patients.

Moreira J, Noe G, Rangarajan S, Courtin C, Etain B, Geoffroy PA, Laplanche JL, Vidal M, Bellivier F and Marie-Claire C

The World Journal of Biological Psychiatry (2018)

Blood-based kinase activity profiling: a potential predictor of response to immune checkpoint inhibition in metastatic cancer

Daan P Hurkmans, Els M E Verdegaal, Sabrina A Hogan R et. al.

Immunother Cancer 2020

Analyzing tyrosine kinase activity in head and neck cancer by functional kinomics: Identification of hyperactivated Src family kinases as prognostic markers and potential targets.

Bussmann L, Hoffer K, von Bargen CM, Droste C, Lange T, Kemmling J, Nollau P, Rangarajan S, de Wijn R et. al.

Int J Cancer. 2021 Apr 22.

Clinical and kinomic analysis identifies peripheral blood mononuclear cells as a potential pharmacodynamic biomarker in metastatic renal cell carcinoma patients treated with sunitinib.

Noé G, Bellesoeur A, Thomas-Schoemann A, Rangarajan S, Naji F, Alexandre J, Blanchet B, Vidal M.

Oncotarget. Aug 29. (2016)

The evolving landscape of biomarkers for checkpoint inhibitor immunotherapy.

Havel JJ et al.

Nat. Rev. Cancer 19, 133–150 (2019).

Profiling of human lymphocytes reveals a specific network of protein kinases modulated by endurance training status.

Alack, K. et al.

Sci Rep. Jan 21;10(1):888 (2020).

Kinase activity profiling in renal cell carcinoma, benign renal tissue and in response to four different tyrosine kinase inhibitors

Andliena Tahiri, Katarina Puco, Faris Naji, Vessela N. Kristensen, Jan Oldenburg and Jürgen Geisleret al,

Oncotarget, 2022

Cancer-Associated Fibroblasts Regulate Kinase Activity in Mesothelioma Cell Lines via Paracrine Signaling and Thereby Dictate Cell Faith and Behaviorr

Alexander Mathilakathu, MichaelWessolly, Elena Mairinger, and Sabrina Borchert et al,

Mol. Sci. 2022, 23, 3278

Inhibition of Cyclin-Dependent Kinase 8/Cyclin-Dependent Kinase 19 Suppresses Its Pro-Oncogenic Effects in Prostate Cancer

Anne Offermann, Vincent Joerg, Finn Becker, Marie C. Roesch,y Duan Kang, Sven Perner et al,

The American Journal of Pathology, Vol. 192, No. 5, May 2022

Kinomics platform using GBM tissue identifies BTK as being associated with higher patient survival

Sofian Al Shboul, Olimpia E Curran, Javier A Alfaro, Fiona Lickiss, Ted R Hupp, Paul M Brennan et al,

Life Science Alliance 2021

Tyrosine Kinase Inhibitor Sunitinib Delays Platelet- Induced Coagulation: Additive Effects of Aspirin

Bibian M. E. Tullemans, Delia I. Fernández, Alicia Veninga, Constance C. F. M. J. Baaten, JohanW. M. Heemskerk, Marijke J. E. Kuijpers

Thrombosis and Haemostasis 2021

Kinase activity profiling in renal cell carcinoma, benign renal tissue and in response to four different tyrosine kinase inhibitors

Andliena Tahiri, Katarina Puco, Faris Naji, Vessela N. Kristensen, Jan Oldenburg and Jürgen Geisleret al,

Oncotarget, 2022

Flavopiridol (Alvocidib), a Cyclin-dependent Kinases (CDKs) Inhibitor, Found Synergy Effects with Niclosamide in Cutaneous T-cell Lymphoma

Xu Hannah Zhang*, Jack Hsiang, Steven T. Rosen et al,

J Clin Haematol. 2021

Intratumoral spatial heterogeneity of BTK kinomic activity dictates distinct therapeutic response within a single glioblastoma tumor.

Ibrahim AN, Yamashita D, Anderson JC, Abdelrashid M, Alwakeal A, Estevez-Ordonez D, Komarova S, Markert JM, Goidts V, Willey CD, Nakano I.

J Neurosurg. Oct 18:1-12.(2019)

Macrophage-Mediated Antibody Dependent Effector Function in Aggressive B-Cell Lymphoma Treatment is Enhanced by Ibrutinib via Inhibition of JAK2

Verena Barbarino, Sinika Henschke, Stuart James Blakemore. et al

Cancers 2020,

Differential Inhibition of Ex-Vivo Tumor Kinase Activity by Vemurafenib in BRAF(V600E) and BRAF Wild-Type Metastatic Malignant Melanoma.

Tahiri, A. et al.

PLoS One 8, (2013).

Molecular mechanism underlying the pharmacological interactions of the protein kinase C-β inhibitor enzastaurin and erlotinib in non-small cell lung cancer cells.

Steen NV, Potze L, Giovannetti E, Cavazzoni A, Ruijtenbeek R, Rolfo C, Pauwels P, Peters GJ.

Am J Cancer Res. Apr 1;7(4):816-830. eCollection 2017.

Multiparametric Assessment of the Effects of Tyrosine Kinase Inhibitors (TKIs) on the (Electro)physiology of Human Induced Pluripotent Stem Cell (hiPSC)-Derived Cardiomyocytes.

de Korte T, Nacken P, Pijnenburg D, Ruijtenbeek R, Stevenhagen F, Wilbers R, den Hartogh S, Groten J, Braam S and Vlaming M

Journal of Pharmacological and Toxicological Methods. 88. 236-237. 10.1016. (2017)

Kinome profiling of cholangiocarcinoma organoids reveals potential druggable targets that hold promise for treatment stratification

Ruby Lieshout, Alessandra V. S. Faria, M. A. Verstegen1 and Gwenny M. Fuhler

Molecular Medicine (2022)

Suppression of tumor-associated neutrophils by lorlatinib attenuates pancreatic cancer growth and improves treatment with immune checkpoint blockade

Sebastian R. Nielsen, Jan E. Strøbech, Edward R. Horton, et al.

NATURE COMMUNICATIONS | (2021)

Constitutive activation of Lyn kinase enhances BCR responsiveness, but not the development of CLL in Em-TCL1 mice

Viktoria Kohlhas, Michael Hallek,* and Phuong-Hien Nguyen*, et al.

Blood adavances | (2021)

EGFRvIII upregulates DNA mismatch repair resulting in increased temozolomide sensitivity of MGMT promoter methylated glioblastoma

Nina Struve, Zev A. Binder, Lucy F. Stead, Tim Brend

SPRINGER NATURE 2020 Oncogene

Combined Inhibition of SHP2 and MEK Is Effective in Models of NF1-Deficient Malignant Peripheral Nerve Sheath Tumors

Jiawan Wang, Kai Pollard, Amy N. Allen1, Tushar Tomar, Dirk Pijnenburg, Zhan Yao,
Fausto J. Rodriguez, and Christine A. Pratilas

Cancer Res; 2020

Emerging Kinase Therapeutic Targets in Pancreatic Ductal Adenocarcinoma and Pancreatic Cancer Desmoplasia.

Creeden JF, Alganem K, Imami AS, Henkel ND, Brunicardi FC, Liu SH, Shukla R, Tomar T, Naji F, McCullumsmith RE.

Int J Mol Sci. Nov 21;21(22):8823 (2020)

Targeting cyclin-dependent kinases for the treatment of pulmonary arterial hypertension.

Weiss A, Neubauer MC, Yerabolu D, Kojonazarov B, Schlueter BC, Neubert L, Jonigk D, Baal N, Ruppert C, Dorfmuller P, Pullamsetti SS, Weissmann N, Ghofrani HA, Grimminger F, Seeger W, Schermuly RT.

Nat Commun. May 17;10(1):2204.(2019)

ARv7 Represses Tumor-Suppressor Genes in Castration-Resistant Prostate Cancer.

Cato L, de Tribolet-Hardy J, Lee I, Rottenberg JT, Coleman I, Liu XS, Cato ACB, Lack NA, Nelson PS, Plymate SR, Groner AC, Brown M.

Cancer Cell. (2019)

Rational development of synergistic combinations of chemotherapy and molecular targeted agents for colorectal cancer treatment.

Tosi D, Pérez-Gracia E, Atis S, Vié N, Combès E, Gabanou M, Larbouret C, Jarlier M, Mollevi C, Torro A, Del Rio M, Martineau P, Gongora C.

BMC Cancer. Aug 13;18(1):812. (2018)

Pharmacological inhibition of protein tyrosine kinases axl and fyn reduces TNF-α-induced endothelial inflammatory activation in vitro

Sophie F. Ellermann, Rianne M. Jongman, Matthijs Luxen, Timara Kuiper, Josee Plantinga, Jill Moser, Thomas W. L. Scheeren, Gregor Theilmeier, Grietje Molema and Matijs Van Meurs et al.

Frontiers in Pharmacology | (2022)

Chemical genetics strategy to profile kinase target engagement reveals role of FES in neutrophil
phagocytosis

Tom van der Wel , Riet Hilhorst, Hans den Dulk et al.

NATURE COMMUNICATIONS | (2020) 11:3216

Metformin induces lipogenic differentiation in myofibroblasts to reverse lung fibrosis.

Kheirollahi V, Wasnick RM, Biasin V, Vazquez-Armendariz AI, Chu X, Moiseenko A, Weiss A, Wilhelm J, Zhang JS, Kwapiszewska G, Herold S, Schermuly RT, Mari B, Li X, Seeger W, Günther A, Bellusci S, El Agha E.

Nat Commun. Jul 5;10(1):2987. (2019)

Mechanically activated Piezo1 channels of cardiac fibroblasts stimulate p38 mitogen-activated protein kinase activity and interleukin-6 secretion.

Blythe NM, Muraki K, Ludlow MJ, Stylianidis V, Gilbert HTJ, Evans EL, Cuthbertson K, Porter KE, Beech DJ, Turner NA.

J Biol Chem. (2019)

Decrease in phospho-PRAS40 plays a role in the synergy between erlotinib and crizotinib in an EGFR and cMET wild-type squamous non-small cell lung cancer cell line.

Van Der Steen N, Leonetti A, Keller K, Dekker H, Funel N, Lardon F, Ruijtenbeek R, Tiseo M, Rolfo C, Pauwels P, Peters GJ, Giovannetti E.

Biochem Pharmacol. 2019 Aug;166:128-138. (2019)

Gemcitabine: An Alternative Treatment for Oxaliplatin-Resistant Colorectal Cancer

Mathieu Chocry , Ludovic Leloup, Fabrice Parat, Mélissa Messé, Alessandra Pagano and Hervé Kovacic

Cancers 2022

An in vivo model of glioblastoma radiation resistance identifies long noncoding RNAs and targetable kinases

Christian T. Stackhouse, G. Yancey Gillespie, Christopher D. Willey

JCI Insight. 2022

Combined Inhibition of SHP2 and MEK Is Effective in Models of NF1-Deficient Malignant Peripheral Nerve Sheath Tumors

Jiawan Wang, Kai Pollard, Amy N. Allen1, Tushar Tomar, Dirk Pijnenburg, Zhan Yao, Fausto J. Rodriguez, and Christine A. Pratilas

Cancer Res; 2020

The Aurora kinase/β-catenin axis contributes to dexamethasone resistance in leukemia

Kinjal Shah, Mehreen Ahmed and Julhash U. Kazi et. al.

Precision Oncology (2021)

Kinome profiling of cholangiocarcinoma organoids reveals potential druggable targets
that hold promise for treatment stratification

Ruby Lieshout, Alessandra V. S. Faria, M. A. Verstegen1 and Gwenny M. Fuhler

Molecular Medicine (2022)

Kinase activity profiling identifies putative downstream targets of cGMP/PKG signaling in inherited retinal neurodegeneration

Akanksha Roy Arianna Tolone, Riet Hilhorst, John Groten, Tushar Tomar and François Paquet-Durand

Cell Death Discovery ( 2022)

Cardiomyocyte stromal interaction molecule 1 is a key regulator of Ca2+-dependent
kinase and phosphatase activity in the mouse heart

Helen E. Collins1 | Joshua C. Anderson2 | Adam R. Wende3 | John C. Chatham

Physiological Reports. 2022

Hepatic kinome atlas: An in-depth identification of kinase pathways in liver fibrosis of humans and rodents

Justin F. Creeden | Zachary A. Kipp | Mei Xu | Robert M. Flight | Terry D. Hinds Jr

Hepatology. 2022

Identification of Novel Substrates for cGMP Dependent Protein Kinase (PKG) through Kinase Activity Profiling to Understand Its Putative Role in Inherited Retinal Degeneration.

Roy A, Groten J, Marigo V, Tomar T, Hilhorst R.

Int J Mol Sci. Jan 25;22(3):1180 (2021)

Combined Inhibition of SHP2 and MEK Is Effective in Models of NF1-Deficient Malignant Peripheral Nerve Sheath Tumors.

Wang J, Pollard K, Allen AN, Tomar T, Pijnenburg D, Yao Z, Rodriguez FJ, Pratilas CA

Cancer Res. Dec 1;80(23):5367-5379 (2020)

Large-scale reduction of tyrosine kinase activities in human monocytes stimulated in vitro with N. meningitidis.

Gopinathan, U. et al.

PLoS One 13, 1–23 (2018).

Neuronal impact of patient-specific aberrant NRXN1α splicing.

Flaherty E, Zhu S, Barretto N, Cheng E, Deans PJM, Fernando MB, Schrode N, Francoeur N, Antoine A, Alganem K, Halpern M, Deikus G, Shah H, Fitzgerald M, Ladran I, Gochman P, Rapoport J, Tsankova NM, McCullumsmith R, Hoffman GE, Sebra R, Fang G, Brennand KJ.

Nat Genet. Dec;51(12):1679-1690. (2019).

Intratumoral spatial heterogeneity of BTK kinomic activity dictates distinct therapeutic response within a single glioblastoma tumor.

Ibrahim AN, Yamashita D, Anderson JC, Abdelrashid M, Alwakeal A, Estevez-Ordonez D, Komarova S, Markert JM, Goidts V, Willey CD, Nakano I.

J Neurosurg. Oct 18:1-12. (2019)

Systemic analysis of tyrosine kinase signaling reveals a common adaptive response program in a HER2-positive breast cancer.

Schwill M, Tamaskovic R, Gajadhar AS, Kast F, White FM, Plückthun A.

Sci Signal. Jan 22;12(565) (2019)

Analysis of Jak2 catalytic function by peptide microarrays: the role of the JH2 domain and V617F mutation.

Sanz A, Ungureanu D, Pekkala T, Ruijtenbeek R, Touw IP, Hilhorst R, Silvennoinen O.

PLoS One. (2011) Apr 18;6(4):e18522.

Human β-defensin 2 ameliorates acute GVHD by limiting ileal neutrophil infiltration and restraining T cell receptor signaling

Tamina Rückert, Geoffroy Andrieux, Melanie Boerries, Robert Zeiser, Natalie Köhler et. al.

Sci. Transl. Med. 14, eabp9675 (2022)

Echinacea purpurea (L.) Moench treatment of monocytes promotes tonic interferon signaling, increased innate immunity gene expression and DNA repeat hypermethylated silencing of endogenous retroviral sequences

Ken Declerck, Claudina Perez Novo, Lisa Grielens, Guy Van Camp, Andreas Suter and Wim Vanden Berghe et. al.

BMC Complementary Medicine and Therapies /2021

The Aurora kinase/β-catenin axis contributes to dexamethasone resistance in leukemia

Kinjal Shah, Mehreen Ahmed and Julhash U. Kazi et. al.
Precision Oncology

Blood-based kinase activity profiling: a potential predictor of response to immune checkpoint inhibition in metastatic cancer

Daan P Hurkmans ,1,2 Els M E Verdegaal ,3 Sabrina A Hogan R et. al.
Immunother Cancer 2020

Macrophage-Mediated Antibody Dependent Effector
Function in Aggressive B-Cell Lymphoma Treatment
is Enhanced by Ibrutinib via Inhibition of JAK2

Verena Barbarino, Sinika Henschke, Stuart James Blakemore. et al

Cancers 2020, 12, 2303; doi:10.3390/cancers12082303

Suppression of tumor-associated neutrophils by lorlatinib attenuates pancreatic cancer growth and improves treatment with immune checkpoint blockade

Sebastian R. Nielsen, Jan E. Strøbech, Edward R. Horton, et al.

NATURE COMMUNICATIONS | (2021) 12:3414

Kinase activity profiling reveals contribution of G-protein signaling
modulator 2 deficiency to impaired regulatory T cell migration in
rheumatoid arthritis

Anja Meyer a, Shuaifeng Yan, Christian P. Pallasch b,c,e,f, David M. Kofler et al.

Journal of Autoimmunity | (2021)

Finnish-specific AKT2 gene variant leads to impaired insulin signalling in myotubes

Selina Mäkinen, Neeta Datta, Savithri Rangarajan, Yen H Nguyen, Vesa M Olkkonen, Aino Latva-Rasku, Pirjo Nuutila, Markku Laakso and Heikki A Koistinene et al,

Journal of Molecular Endocrinology 2022

Targeting of CXCR4 by the Naturally Occurring CXCR4 Antagonist EPI-X4 in Waldenström’s Macroglobulinemia

Lisa Marie Kaiser , Mirja Harms, Daniel Sauter , Vijay P. S. Rawat, Mirco Glitscher ,
Eberhard Hildt, Daniel Tews, Zachary Hunter, Jan Münch 2 and Christian Buske et al,

Cancers 2021

Kinomics platform using GBM tissue identifies BTK as being associated with higher patient survival

Sofian Al Shboul, Olimpia E Curran, Javier A Alfaro, Fiona Lickiss, Ted R Hupp, Paul M Brennan et al,

Life Science Alliance 2021

Knockdown of AKT3 Activates HER2 and DDR Kinases in Bone-Seeking Breast Cancer Cells, Promotes Metastasis In Vivo and Attenuates the TGF/CTGF Axis

Nico Hinz, Anke Baranowsky, Michael Horn, Malte Kriegs, Freya Sibbertsen, Daniel J. Smit,
Philippe Clezardin, Tobias Lange, Thorsten Schinke and Manfred Jücker

Cells 2021

TNFa-Signaling Modulates the Kinase Activity of Human Effector Treg and Regulates IL-17A Expression

Paulo C. M. Urbano, Xuehui He, Bennie van Heeswijk, Omar P. S. Filho, Henk Tijssen,
Ruben L. Smeets , Irma Joosten and Hans J. P. M. Koenen

Frontiers in Immunology | www.frontiersin.org January 2020

STAT5-regulated microRNA-193b controls haematopoietic stem and progenitor cell expansion by modulating cytokine receptor signalling.

Haetscher N, Feuermann Y, Wingert S, Rehage M, Thalheimer FB, Weiser C, Bohnenberger H, Jung K, Schroeder T, Serve H, Oellerich T, Hennighausen L, Rieger MA.

Nat Commun. Nov 25;6:8928. (2015)

Profiling of human lymphocytes reveals a specific network of protein kinases modulated by endurance training status

Katharina Alack, Astrid Weiss, Karsten Krüger, Mona Höret, Ralph Schermuly,
Torsten Frech, Martin Eggert & Frank-Christoph Mooren

Scientific Reports | (2020) 10:888

Kinomic profiling of tumour xenografts derived from patients with non-small cell lung cancer confirms their fidelity and reveals potentially actionable pathways.

Tabbò F, Guerrera F, van den Berg A, Gaudiano M, Maletta F, Bessone L, Nottegar A, Costardi L, de Wijn R, Ruijtenbeek R et. al.

Eur J Cancer. Feb;144:17-30 (2021)

Novel EPHB4 Receptor Tyrosine Kinase Mutations and Kinomic Pathway Analysis in Lung Cancer.

Ferguson BD, Tan YH, Kanteti RS, Liu R, Gayed MJ, Vokes EE, Ferguson MK, Iafrate AJ, Gill PS, Salgia R.

Sci Rep. 5:10641. doi: 10.1038/srep10641. (2015)

Inactive immune pathways in triple negative breast cancers that showed resistance to neoadjuvant chemotherapy as inferred from kinase activity profiles.

Sawada T, Hilhorst R, Rangarajan S, Yoshida M, Tanabe Y, Tamura K, Kinoshita T, Shimoyama T, van Beuningen R, Ruijtenbeek R, Tsuda H, Koizumi F.

Oncotarget. Sep 28;9(76):34229-34239. (2018)

Reversion of resistance to oxaliplatin by inhibition of p38 MAPK in colorectal cancer cell lines: involvement of the calpain / Nox1 pathway.

Chocry M, Leloup L, Kovacic H.

Oncotarget. 2017 Oct 10;8(61):103710-103730.

MicroRNA-26b Attenuates Platelet Adhesion and Aggregation in Mice

Linsey J. F. Peters, Constance C. F. M. J. Baaten, Sanne L. Maas, Marijke J. E. Kuijpers and Emiel P. C. van der Vorst

Biomedicines 2022, 10, 983

Publications

Publications

At PamGene we have developed a robust and unique microarray technology for multiplex kinase activity profiling. On this page you will find a selection of scientific publications where PamGene’s technology has been applied.

Overview

Diagnostics

Blood-based kinase activity profiling: a potential predictor of response to immune checkpoint inhibition in metastatic cancer

Blood-Based Multiplex Kinase Activity Profiling as a Predictive Marker for Clinical Response to Checkpoint Blockade in Advanced NSCLC.

Blood-based multiplex kinase activity profiling as a predictive marker for clinical response to checkpoint blockade in advanced melanoma.

Phosphoproteomic and Kinomic Signature of Clinically Aggressive Grade I (1.5) Meningiomas Reveals Rb1 signaling as a Novel Mediator and Biomarker.

Systemic analysis of tyrosine kinase signaling reveals a common adaptive response program in a HER2-positive breast cancer.

Identification of new possible targets for leukemia treatment by kinase activity profiling.

Inactive immune pathways in triple negative breast cancers that showed resistance to neoadjuvant chemotherapy as inferred from kinase activity profiles.

Profiling activity of cellular kinases in migrating T-cells.

Differential Kinase Activation in Peripheral Blood Mononuclear Cells from Non-Small-Cell Lung Cancer Patients Treated with Nivolumab.

Lithium effects on serine-threonine kinases activity: high throughput Kinomic Profiling of lymphoblastoid cell lines from excellent-responders and non-responders bipolar patients.

Biomarker discovery

Blood-based kinase activity profiling: a potential predictor of response to immune checkpoint inhibition in metastatic cancer

Analyzing tyrosine kinase activity in head and neck cancer by functional kinomics: Identification of hyperactivated Src family kinases as prognostic markers and potential targets.

Clinical and kinomic analysis identifies peripheral blood mononuclear cells as a potential pharmacodynamic biomarker in metastatic renal cell carcinoma patients treated with sunitinib.

The evolving landscape of biomarkers for checkpoint inhibitor immunotherapy.

Profiling of human lymphocytes reveals a specific network of protein kinases modulated by endurance training status.

Cancer Profiling

Kinase activity profiling in renal cell carcinoma, benign renal tissue and in response to four different tyrosine kinase inhibitors

Cancer-Associated Fibroblasts Regulate Kinase Activity in Mesothelioma Cell Lines via Paracrine Signaling and Thereby Dictate Cell Faith and Behaviorr

Inhibition of Cyclin-Dependent Kinase 8/Cyclin-Dependent Kinase 19 Suppresses Its Pro-Oncogenic Effects in Prostate Cancer

Kinomics platform using GBM tissue identifies BTK as being associated with higher patient survival

Kinase Inhibitor Discovery / Optimization

Tyrosine Kinase Inhibitor Sunitinib Delays Platelet- Induced Coagulation: Additive Effects of Aspirin

Kinase activity profiling in renal cell carcinoma, benign renal tissue and in response to four different tyrosine kinase inhibitors

Flavopiridol (Alvocidib), a Cyclin-dependent Kinases (CDKs) Inhibitor, Found Synergy Effects with Niclosamide in Cutaneous T-cell Lymphoma

Intratumoral spatial heterogeneity of BTK kinomic activity dictates distinct therapeutic response within a single glioblastoma tumor.

Macrophage-Mediated Antibody Dependent Effector Function in Aggressive B-Cell Lymphoma Treatment is Enhanced by Ibrutinib via Inhibition of JAK2

Differential Inhibition of Ex-Vivo Tumor Kinase Activity by Vemurafenib in BRAF(V600E) and BRAF Wild-Type Metastatic Malignant Melanoma.

Molecular mechanism underlying the pharmacological interactions of the protein kinase C-β inhibitor enzastaurin and erlotinib in non-small cell lung cancer cells.

Multiparametric Assessment of the Effects of Tyrosine Kinase Inhibitors (TKIs) on the (Electro)physiology of Human Induced Pluripotent Stem Cell (hiPSC)-Derived Cardiomyocytes.

Target discovery

Kinome profiling of cholangiocarcinoma organoids reveals potential druggable targets that hold promise for treatment stratification

Suppression of tumor-associated neutrophils by lorlatinib attenuates pancreatic cancer growth and improves treatment with immune checkpoint blockade

Constitutive activation of Lyn kinase enhances BCR responsiveness, but not the development of CLL in Em-TCL1 mice

EGFRvIII upregulates DNA mismatch repair resulting in increased temozolomide sensitivity of MGMT promoter methylated glioblastoma

Combined Inhibition of SHP2 and MEK Is Effective in Models of NF1-Deficient Malignant Peripheral Nerve Sheath Tumors

Emerging Kinase Therapeutic Targets in Pancreatic Ductal Adenocarcinoma and Pancreatic Cancer Desmoplasia.

Targeting cyclin-dependent kinases for the treatment of pulmonary arterial hypertension.

ARv7 Represses Tumor-Suppressor Genes in Castration-Resistant Prostate Cancer.

Rational development of synergistic combinations of chemotherapy and molecular targeted agents for colorectal cancer treatment.

Target interaction

Pharmacological inhibition of protein tyrosine kinases axl and fyn reduces TNF-α-induced endothelial inflammatory activation in vitro

Chemical genetics strategy to profile kinase target engagement reveals role of FES in neutrophilphagocytosis

Metformin induces lipogenic differentiation in myofibroblasts to reverse lung fibrosis.

Mechanically activated Piezo1 channels of cardiac fibroblasts stimulate p38 mitogen-activated protein kinase activity and interleukin-6 secretion.

Decrease in phospho-PRAS40 plays a role in the synergy between erlotinib and crizotinib in an EGFR and cMET wild-type squamous non-small cell lung cancer cell line.

Resistance mechanism

Gemcitabine: An Alternative Treatment for Oxaliplatin-Resistant Colorectal Cancer

An in vivo model of glioblastoma radiation resistance identifies long noncoding RNAs and targetable kinases

Combined Inhibition of SHP2 and MEK Is Effective in Models of NF1-Deficient Malignant Peripheral Nerve Sheath Tumors

The Aurora kinase/β-catenin axis contributes to dexamethasone resistance in leukemia

Diseases Model / Biochemical – characterization

Kinome profiling of cholangiocarcinoma organoids reveals potential druggable targetsthat hold promise for treatment stratification

Kinase activity profiling identifies putative downstream targets of cGMP/PKG signaling in inherited retinal neurodegeneration

Cardiomyocyte stromal interaction molecule 1 is a key regulator of Ca2+-dependentkinase and phosphatase activity in the mouse heart

Hepatic kinome atlas: An in-depth identification of kinase pathways in liver fibrosis of humans and rodents

Identification of Novel Substrates for cGMP Dependent Protein Kinase (PKG) through Kinase Activity Profiling to Understand Its Putative Role in Inherited Retinal Degeneration.

Combined Inhibition of SHP2 and MEK Is Effective in Models of NF1-Deficient Malignant Peripheral Nerve Sheath Tumors.

Large-scale reduction of tyrosine kinase activities in human monocytes stimulated in vitro with N. meningitidis.

Neuronal impact of patient-specific aberrant NRXN1α splicing.

Intratumoral spatial heterogeneity of BTK kinomic activity dictates distinct therapeutic response within a single glioblastoma tumor.

Systemic analysis of tyrosine kinase signaling reveals a common adaptive response program in a HER2-positive breast cancer.

Analysis of Jak2 catalytic function by peptide microarrays: the role of the JH2 domain and V617F mutation.

Immune Cell

Human β-defensin 2 ameliorates acute GVHD by limiting ileal neutrophil infiltration and restraining T cell receptor signaling

Echinacea purpurea (L.) Moench treatment of monocytes promotes tonic interferon signaling, increased innate immunity gene expression and DNA repeat hypermethylated silencing of endogenous retroviral sequences

The Aurora kinase/β-catenin axis contributes to dexamethasone resistance in leukemia

Blood-based kinase activity profiling: a potential predictor of response to immune checkpoint inhibition in metastatic cancer

Macrophage-Mediated Antibody Dependent EffectorFunction in Aggressive B-Cell Lymphoma Treatmentis Enhanced by Ibrutinib via Inhibition of JAK2

Suppression of tumor-associated neutrophils by lorlatinib attenuates pancreatic cancer growth and improves treatment with immune checkpoint blockade

Kinase activity profiling reveals contribution of G-protein signalingmodulator 2 deficiency to impaired regulatory T cell migration inrheumatoid arthritis

Pathway elucidation

Finnish-specific AKT2 gene variant leads to impaired insulin signalling in myotubes

Targeting of CXCR4 by the Naturally Occurring CXCR4 Antagonist EPI-X4 in Waldenström’s Macroglobulinemia

Kinomics platform using GBM tissue identifies BTK as being associated with higher patient survival

Chemical genetics strategy to profile kinase target engagement reveals role of FES in neutrophil
phagocytosis

Kinome profiling of cholangiocarcinoma organoids reveals potential druggable targets
that hold promise for treatment stratification

Cardiomyocyte stromal interaction molecule 1 is a key regulator of Ca2+-dependent
kinase and phosphatase activity in the mouse heart

Macrophage-Mediated Antibody Dependent Effector
Function in Aggressive B-Cell Lymphoma Treatment
is Enhanced by Ibrutinib via Inhibition of JAK2

Kinase activity profiling reveals contribution of G-protein signaling
modulator 2 deficiency to impaired regulatory T cell migration in
rheumatoid arthritis

Knockdown of AKT3 Activates HER2 and DDR Kinases in Bone-Seeking Breast Cancer Cells, Promotes Metastasis In Vivo and Attenuates the TGF/CTGF Axis