Dr. Kilian V. M. Huber received his doctorate in Medicinal and Pharmaceutical Chemistry from the Ludwig-Maximilians-Universität (LMU) in Munich working on the design and synthesis of natural product-inspired kinase inhibitors in the group Prof. Franz Bracher. After postdoctoral studies in the laboratory of Prof. Stephen G. Davies at the Department of Chemistry, University of Oxford, and in the laboratory of Prof. Giulio Superti-Furga at the Research Centre for Molecular Medicine (CeMM), Vienna, he joined the SGC in 2015 as Principal Investigator and Chemical Biology Group Leader. In 2014 he was selected as a Winner of the GSK Discovery Fast Track Challenge and in 2015 he received the Young Investigator Award of the German Pharmaceutical Society (DPhG-Stiftung/Horst-Böhme-Stiftung).

Research Areas

Kilian’s main research interests comprise the functional exploration of cellular signaling networks by the development of specific chemical probes and chemical biology approaches apt to identify new therapeutic targets relevant for the treatment of human disease.

Group Members

  • Laura Diaz Saez
  • Andrew Lewis
  • Kathryn Pugh
  • Cynthia Tallant
  • Srikannathasan Velupillai
  • Jenny Ward
  • Sarah Blair-Reid
  • Catherine Rogers
  • Ioanna Panagakou

Publications

Artemisinins Target GABAA Receptor Signaling and Impair α Cell Identity.
Li, J; Casteels, T; Frogne, T; Ingvorsen, C; Honoré, C; Courtney, M; Huber, KV; Schmitner, N; Kimmel, RA; Romanov, RA; Sturtzel, C; Lardeau, CH; Klughammer, J; Farlik, M; Sdelci, S; Vieira, A; Avolio, F; Briand, F; Baburin, I; Májek, P; Pauler, FM; Penz, T; Stukalov, A; Gridling, M; Parapatics, K; Barbieux, C; Berishvili, E; Spittler, A; Colinge, J; Bennett, KL; Hering, S; Sulpice, T; Bock, C; Distel, M; Harkany, T; Meyer, D; Superti-Furga, G; Collombat, P; Hecksher-Sørensen, J; Kubicek, S;
Cell. 2016 :-. doi: 10.1016/j.cell.2016.11.010
PMID: 27916275

Heme drives hemolysis-induced susceptibility to infection via disruption of phagocyte functions.
Martins, R; Maier, J; Gorki, AD; Huber, KV; Sharif, O; Starkl, P; Saluzzo, S; Quattrone, F; Gawish, R; Lakovits, K; Aichinger, MC; Radic-Sarikas, B; Lardeau, CH; Hladik, A; Korosec, A; Brown, M; Vaahtomeri, K; Duggan, M; Kerjaschki, D; Esterbauer, H; Colinge, J; Eisenbarth, SC; Decker, T; Bennett, KL; Kubicek, S; Sixt, M; Superti-Furga, G; Knapp, S;
Nature Immunology. 2016 17:1361-1372. doi: 10.1038/ni.3590
PMID: 27798618

Proteome-wide drug and metabolite interaction mapping by thermal-stability profiling.
Huber, KV; Olek, KM; Müller, AC; Tan, CS; Bennett, KL; Colinge, J; Superti-Furga, G;
Nature Methods. 2015 12:1055-1057. doi:
PMID: 26389571

A cellular screen identifies ponatinib and pazopanib as inhibitors of necroptosis.
Fauster, A; Rebsamen, M; Huber, KV; Bigenzahn, JW; Stukalov, A; Lardeau, CH; Scorzoni, S; Bruckner, M; Gridling, M; Parapatics, K; Colinge, J; Bennett, KL; Kubicek, S; Krautwald, S; Linkermann, A; Superti-Furga, G;
Cell Death and Disease. 2015 6:e1767-. doi:
PMID: 25996294

SLC38A9 is a component of the lysosomal amino acid sensing machinery that controls mTORC1.
Rebsamen, M; Pochini, L; Stasyk, T; de Araújo, ME; Galluccio, M; Kandasamy, RK; Snijder, B; Fauster, A; Rudashevskaya, EL; Bruckner, M; Scorzoni, S; Filipek, PA; Huber, KV; Bigenzahn, JW; Heinz, LX; Kraft, C; Bennett, KL; Indiveri, C; Huber, LA; Superti-Furga, G;
Nature. 2015 519:477-481. doi:
PMID: 25561175

Stereospecific targeting of MTH1 by (S)-crizotinib as an anticancer strategy.
Huber, KV; Salah, E; Radic, B; Gridling, M; Elkins, JM; Stukalov, A; Jemth, AS; Göktürk, C; Sanjiv, K; Strömberg, K; Pham, T; Berglund, UW; Colinge, J; Bennett, KL; Loizou, JI; Helleday, T; Knapp, S; Superti-Furga, G;
Nature. 2014 508:222-227. doi:
PMID: 24695225

Experimental characterization of the human non-sequence-specific nucleic acid interactome.
Dürnberger, G; Bürckstümmer, T; Huber, K; Giambruno, R; Doerks, T; Karayel, E; Burkard, TR; Kaupe, I; Müller, AC; Schönegger, A; Ecker, GF; Lohninger, H; Bork, P; Bennett, KL; Superti-Furga, G; Colinge, J;
Genome Biology: biology for the post-genomic era. 2013 14:R81-. doi:
PMID: 23902751

7,8-dichloro-1-oxo-β-carbolines as a versatile scaffold for the development of potent and selective kinase inhibitors with unusual binding modes.
Huber, K; Brault, L; Fedorov, O; Gasser, C; Filippakopoulos, P; Bullock, AN; Fabbro, D; Trappe, J; Schwaller, J; Knapp, S; Bracher, F;
Journal of Medicinal Chemistry. 2012 55:403-413. doi:
PMID: 22136433

Specific CLK inhibitors from a novel chemotype for regulation of alternative splicing.
Fedorov, O; Huber, K; Eisenreich, A; Filippakopoulos, P; King, O; Bullock, AN; Szklarczyk, D; Jensen, LJ; Fabbro, D; Trappe, J; Rauch, U; Bracher, F; Knapp, S;
Chemistry and Biology. 2011 18:67-76. doi:
PMID: 21276940

Novel 3-arylideneindolin-2-ones as inhibitors of NAD+ -dependent histone deacetylases (sirtuins).
Huber, K; Schemies, J; Uciechowska, U; Wagner, JM; Rumpf, T; Lewrick, F; Süss, R; Sippl, W; Jung, M; Bracher, F;
Journal of Medicinal Chemistry. 2010 53:1383-1386. doi:
PMID: 20030343

2017

Combinatorial Drug Screening Identifies Ewing Sarcoma-specific Sensitivities.
Radic-Sarikas, B; Tsafou, KP; Emdal, KB; Papamarkou, T; Huber, KV; Mutz, C; Toretsky, JA; Bennett, KL; Olsen, JV; Brunak, S; Kovar, H; Superti-Furga, G;
Molecular Cancer Therapeutics. 2017 16:88-101. doi: 10.1158/1535-7163.MCT-16-0235
PMID: 28062706

2016

Discovery of a PCAF Bromodomain Chemical Probe.
Moustakim M, Clark PG, Trulli L, Fuentes de Arriba AL, Ehebauer MT, Chaikuad A, Murphy EJ, Mendez-Johnson J, Daniels D, Hou CD, Lin YH, Walker JR, Hui R, Yang H, Dorrell L, Rogers CM, Monteiro OP, Fedorov O, Huber KV, Knapp S, Heer J, Dixon DJ, Brennan PE
Angew. Chem. Int. Ed. Engl.. 2016 . doi: 10.1002/anie.201610816
PMID: 27966810

Heme drives hemolysis-induced susceptibility to infection via disruption of phagocyte functions.
Martins, R; Maier, J; Gorki, AD; Huber, KV; Sharif, O; Starkl, P; Saluzzo, S; Quattrone, F; Gawish, R; Lakovits, K; Aichinger, MC; Radic-Sarikas, B; Lardeau, CH; Hladik, A; Korosec, A; Brown, M; Vaahtomeri, K; Duggan, M; Kerjaschki, D; Esterbauer, H; Colinge, J; Eisenbarth, SC; Decker, T; Bennett, KL; Kubicek, S; Sixt, M; Superti-Furga, G; Knapp, S;
Nature Immunology. 2016 17:1361-1372. doi: 10.1038/ni.3590
PMID: 27798618

Artemisinins Target GABAA Receptor Signaling and Impair α Cell Identity.
Li, J; Casteels, T; Frogne, T; Ingvorsen, C; Honoré, C; Courtney, M; Huber, KV; Schmitner, N; Kimmel, RA; Romanov, RA; Sturtzel, C; Lardeau, CH; Klughammer, J; Farlik, M; Sdelci, S; Vieira, A; Avolio, F; Briand, F; Baburin, I; Májek, P; Pauler, FM; Penz, T; Stukalov, A; Gridling, M; Parapatics, K; Barbieux, C; Berishvili, E; Spittler, A; Colinge, J; Bennett, KL; Hering, S; Sulpice, T; Bock, C; Distel, M; Harkany, T; Meyer, D; Superti-Furga, G; Collombat, P; Hecksher-Sørensen, J; Kubicek, S;
Cell. 2016 :-. doi: 10.1016/j.cell.2016.11.010
PMID: 27916275

Mapping the chemical chromatin reactivation landscape identifies BRD4-TAF1 cross-talk.
Sdelci, S; Lardeau, CH; Tallant, C; Klepsch, F; Klaiber, B; Bennett, J; Rathert, P; Schuster, M; Penz, T; Fedorov, O; Superti-Furga, G; Bock, C; Zuber, J; Huber, KV; Knapp, S; Müller, S; Kubicek, S;
Nature Chemical Biology. 2016 12:504-510. doi:
PMID: 27159579

Profiling of Small Molecules by Chemical Proteomics.
Huber, KV; Superti-Furga, G;
Methods in Molecular Biology. 2016 1394:211-218. doi:
PMID: 26700051

2015

Proteome-wide drug and metabolite interaction mapping by thermal-stability profiling.
Huber, KV; Olek, KM; Müller, AC; Tan, CS; Bennett, KL; Colinge, J; Superti-Furga, G;
Nature Methods. 2015 12:1055-1057. doi:
PMID: 26389571

Target profiling of an antimetastatic RAPTA agent by chemical proteomics: Relevance to the mode of action
Babak, MV; Meier, SM; Huber, KVM; Reynisson, J; Legin, AA; Jakupec, MA; Roller, A; Stukalov, A; Gridling, M; Bennett, KL; Colinge, J; Berger, W; Dyson, PJ; Superti-Furga, G; Keppler, BK; Hartinger, CG;
Chemical Science. 2015 6:2449-2456. doi: 10.1039/c4sc03905j
PMID:

SLC38A9 is a component of the lysosomal amino acid sensing machinery that controls mTORC1.
Rebsamen, M; Pochini, L; Stasyk, T; de Araújo, ME; Galluccio, M; Kandasamy, RK; Snijder, B; Fauster, A; Rudashevskaya, EL; Bruckner, M; Scorzoni, S; Filipek, PA; Huber, KV; Bigenzahn, JW; Heinz, LX; Kraft, C; Bennett, KL; Indiveri, C; Huber, LA; Superti-Furga, G;
Nature. 2015 519:477-481. doi:
PMID: 25561175

A cellular screen identifies ponatinib and pazopanib as inhibitors of necroptosis.
Fauster, A; Rebsamen, M; Huber, KV; Bigenzahn, JW; Stukalov, A; Lardeau, CH; Scorzoni, S; Bruckner, M; Gridling, M; Parapatics, K; Colinge, J; Bennett, KL; Kubicek, S; Krautwald, S; Linkermann, A; Superti-Furga, G;
Cell Death and Disease. 2015 6:e1767-. doi:
PMID: 25996294

2014

Further Evaluation of Pro-Atherogenic and Anti-Angiogenic Effects of Nilotinib in Mice and in Patients with Ph-Chromosome plus CML
Hadzijusufovic, E; Albrecht-Schgoer, K; Huber, K; Grebien, F; Eisenwort, G; Schgoer, W; Kaun, C; Herndlhofer, S; Theurl, M; Cerny-Reiterer, S; Hoermann, G; Sperr, WR; Rix, U; Sadovnik, I; Jilma, B; Schernthaner, GH; Wojta, J; Wolf, D; Superti-Furga, G; Kirchmair, R; Valent, P;
Blood. 2014 124:-. doi:
PMID:

Nilotinib exerts proatherogenic and growth-inhibitory effects on endothelial cells: a potential mechanism underlying drug-related vasculopathy in Ph plus CML
Hadzijusufovic, E; Albrecht-Schgoer, K; Huber, K; Grebien, F; Eisenwort, G; Schgoer, W; Ghanim, V; Sadovnik, I; Kaun, C; Herndlhofer, S; Theurl, M; Cerny-Reiterer, S; Hoermann, G; Jilma, B; Sperr, WR; Rix, U; Wojta, J; Wolf, D; Superti-Furga, G; Kirchmair, R; Valent, P;
Oncology Research and Treatment. 2014 37:300-300. doi:
PMID:

The solute carrier SLC35F2 enables YM155-mediated DNA damage toxicity.
Winter, GE; Radic, B; Mayor-Ruiz, C; Blomen, VA; Trefzer, C; Kandasamy, RK; Huber, KV; Gridling, M; Chen, D; Klampfl, T; Kralovics, R; Kubicek, S; Fernandez-Capetillo, O; Brummelkamp, TR; Superti-Furga, G;
Nature Chemical Biology. 2014 10:768-773. doi:
PMID: 25064833

Building and exploring an integrated human kinase network: global organization and medical entry points.
Colinge, J; César-Razquin, A; Huber, K; Breitwieser, FP; Májek, P; Superti-Furga, G;
Journal of Proteomics. 2014 107:113-127. doi:
PMID: 24704859

Evaluating the Promiscuous Nature of Tyrosine Kinase Inhibitors Assessed in A431 Epidermoid Carcinoma Cells by Both Chemical- and Phosphoproteomics
Giansanti, P; Preisinger, C; Huber, KVM; Gridling, M; Superti-Furga, G; Bennett, KL; Heck, AJR;
ACS Chemical Biology. 2014 9:1490-1498. doi: 10.1021/cb500116c
PMID:

Inhibition of NAD+-dependent histone deacetylases (sirtuins) causes growth arrest and activates both apoptosis and autophagy in the pathogenic protozoan Trypanosoma cruzi.
Veiga-Santos, P; Reignault, LC; Huber, K; Bracher, F; De Souza, W; De Carvalho, TM;
Parasitology (Cambridge). 2014 141:814-825. doi:
PMID: 24670415

Stereospecific targeting of MTH1 by (S)-crizotinib as an anticancer strategy.
Huber, KV; Salah, E; Radic, B; Gridling, M; Elkins, JM; Stukalov, A; Jemth, AS; Göktürk, C; Sanjiv, K; Strömberg, K; Pham, T; Berglund, UW; Colinge, J; Bennett, KL; Loizou, JI; Helleday, T; Knapp, S; Superti-Furga, G;
Nature. 2014 508:222-227. doi:
PMID: 24695225

Inhibition of the SR protein-phosphorylating CLK kinases of Plasmodium falciparum impairs blood stage replication and malaria transmission.
Kern, S; Agarwal, S; Huber, K; Gehring, AP; Strödke, B; Wirth, CC; Brügl, T; Abodo, LO; Dandekar, T; Doerig, C; Fischer, R; Tobin, AB; Alam, MM; Bracher, F; Pradel, G;
PLoS One. 2014 9:e105732-. doi:
PMID: 25188378

2013

ELUCIDATING THE MOLECULAR MECHANISM OF ACTION OF CANCER DRUGS IN THE SECOND DECADE OF THE NEW MILLENNIUM
Superti-Furga, G; Winter, G; Bigenzahn, J; Radic, B; Colinge, J; Bennett, K; Kubicek, S; Zuber, J; Brummelkamp, T; Huber, K;
Experimental Hematology. 2013 41:S9-S9. doi:
PMID:

Experimental characterization of the human non-sequence-specific nucleic acid interactome.
Dürnberger, G; Bürckstümmer, T; Huber, K; Giambruno, R; Doerks, T; Karayel, E; Burkard, TR; Kaupe, I; Müller, AC; Schönegger, A; Ecker, GF; Lohninger, H; Bork, P; Bennett, KL; Superti-Furga, G; Colinge, J;
Genome Biology: biology for the post-genomic era. 2013 14:R81-. doi:
PMID: 23902751

Regulation of pro-angiogenic tissue factor expression in hypoxia-induced human lung cancer cells.
Eisenreich, A; Zakrzewicz, A; Huber, K; Thierbach, H; Pepke, W; Goldin-Lang, P; Schultheiss, HP; Pries, A; Rauch, U;
Oncology Reports: an international journal devoted to fundamental and applied research in oncology. 2013 30:462-470. doi:
PMID: 23604472

Functional role and therapeutic potential of the pim-1 kinase in colon carcinoma.
Weirauch, U; Beckmann, N; Thomas, M; Grünweller, A; Huber, K; Bracher, F; Hartmann, RK; Aigner, A;
Neoplasia. 2013 15:783-794. doi:
PMID: 23814490

2012

Target/s Identification Approaches – Experimental Biological Approaches
Huber, K; Superti-Furga, G; Winter, GE;
. 2012 :94-110. doi: 10.1039/9781849734912-00094
PMID:

7,8-dichloro-1-oxo-β-carbolines as a versatile scaffold for the development of potent and selective kinase inhibitors with unusual binding modes.
Huber, K; Brault, L; Fedorov, O; Gasser, C; Filippakopoulos, P; Bullock, AN; Fabbro, D; Trappe, J; Schwaller, J; Knapp, S; Bracher, F;
Journal of Medicinal Chemistry. 2012 55:403-413. doi:
PMID: 22136433

2011

After the grape rush: sirtuins as epigenetic drug targets in neurodegenerative disorders.
Huber, K; Superti-Furga, G;
Bioorganic and Medicinal Chemistry. 2011 19:3616-3624. doi:
PMID: 21306906

Specific CLK inhibitors from a novel chemotype for regulation of alternative splicing.
Fedorov, O; Huber, K; Eisenreich, A; Filippakopoulos, P; King, O; Bullock, AN; Szklarczyk, D; Jensen, LJ; Fabbro, D; Trappe, J; Rauch, U; Bracher, F; Knapp, S;
Chemistry and Biology. 2011 18:67-76. doi:
PMID: 21276940

2010

A Versatile Synthesis of 3-Substituted 4-Cyano-1,2,3,4-tetrahydro-1-oxo-beta-carbolines
Huber, K; Kast, O; Bracher, F;
Synthesis: journal of synthetic organic chemistry. 2010 :3849-3854. doi: 10.1055/s-0030-1258282
PMID:

PIM serine/threonine kinases in the pathogenesis and therapy of hematologic malignancies and solid cancers.
Brault, L; Gasser, C; Bracher, F; Huber, K; Knapp, S; Schwaller, J;
Haematologica: the hematology journal. 2010 95:1004-1015. doi:
PMID: 20145274

Novel 3-arylideneindolin-2-ones as inhibitors of NAD+ -dependent histone deacetylases (sirtuins).
Huber, K; Schemies, J; Uciechowska, U; Wagner, JM; Rumpf, T; Lewrick, F; Süss, R; Sippl, W; Jung, M; Bracher, F;
Journal of Medicinal Chemistry. 2010 53:1383-1386. doi:
PMID: 20030343

2007

Cytotoxic hybrids between the aromatic alkaloids bauerine C and rutaecarpine
Huber, K; Bracher, F;
Zeitschrift fuer Naturforschung, Section B: A Journal of Chemical Sciences. 2007 62:1313-1316. doi:
PMID:

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