Susanne Müller-Knapp studied Human Biology in Marburg Germany followed by a PhD in molecular biology at the Karolinska Institute in Stockholm, Sweden (1997). She then had more than 6 years of postdoctoral training in the area of inflammation and gene regulation at the Karolinska Institute and at the DIBIT San Raffaele Scientific Institute in Milan, Italy.

In 2004 Susanne joined the Structural Genomics Consortium, SGC, in Oxford. The SGC is an international public private partnership that currently comprises 8 international pharmaceutical companies and a large network of academic and industrial collaborators. Susanne worked at the SGC first as External Research Manager and then Scientific Coordinator. She has been the Project Manager of the Epigenetic Probe Project, which generates tool compounds with defined specificity and selectivity for epigenetic targets and the cell based assay group at the SGC in Oxford testing the cellular activity of the in vitro characterised tool compounds. In her role as Chief Operating Officer at the SGC Frankfurt Susanne is now coordinating several probe programs including the global SGC kinase chemical probe program and the donated probe program, which makes probes available from the pharmaceutical partners of the SGC. She is also Director of Operations of the Chemical Probes Portal, an online platform, providing e recommendations for the right choice and use of chemical probes https://www.chemicalprobes.org/.

Research Areas

The Cellular assay group establishes cellular model systems to establish the efficacy of the developed inhibitors and then further uses them to increase the knowledge of the biological function of the targeted proteins as well as validate their role in disease as a target for pharmacological intervention.

Identification of molecular targets for the targeted treatment of gastric cancer using dasatinib.
Montenegro RC, Howarth A, Ceroni A, Fedele V, Farran B, Mesquita FP, Frejno M, Berger BT, Heinzlmeir S, Sailem HZ, Tesch R, Ebner D, Knapp S, Burbano R, Kuster B, Müller S
Oncotarget. 2020 11(5):535-549. doi: 10.18632/oncotarget.27462
PMID: 32082487

A chemical toolbox for the study of bromodomains and epigenetic signaling.
Wu Q, Heidenreich D, Zhou S, Ackloo S, Krämer A, Nakka K, Lima-Fernandes E, Deblois G, Duan S, Vellanki RN, Li F, Vedadi M, Dilworth J, Lupien M, Brennan PE, Arrowsmith CH, Müller S, Fedorov O, Filippakopoulos P, Knapp S
Nat Commun. 2019 10(1):1915. doi: 10.1038/s41467-019-09672-2
PMID: 31015424

Donated chemical probes for open science.
Müller S, Ackloo S, Arrowsmith CH, Bauser M, Baryza JL, Blagg J, Böttcher J, Bountra C, Brown PJ, Bunnage ME, Carter AJ, Damerell D, Dötsch V, Drewry DH, Edwards AM, Edwards J, Elkins JM, Fischer C, Frye SV, Gollner A, Grimshaw CE, IJzerman A, Hanke T, Hartung IV, Hitchcock S, Howe T, Hughes TV, Laufer S, Li VM, Liras S, Marsden BD, Matsui H, Mathias J, O'Hagan RC, Owen DR, Pande V, Rauh D, Rosenberg SH, Roth BL, Schneider NS, Scholten C, Singh Saikatendu K, Simeonov A, Takizawa M, Tse C, Thompson PR, Treiber DK, Viana AY, Wells CI, Willson TM, Zuercher WJ, Knapp S, Mueller-Fahrnow A
Elife. 2018 7:. doi: 10.7554/eLife.34311
PMID: 29676732

Highly selective inhibition of histone demethylases by de novo macrocyclic peptides.
Kawamura A, Münzel M, Kojima T, Yapp C, Bhushan B, Goto Y, Tumber A, Katoh T, King ON, Passioura T, Walport LJ, Hatch SB, Madden S, Müller S, Brennan PE, Chowdhury R, Hopkinson RJ, Suga H, Schofield CJ
Nat Commun. 2017 8:14773. doi: 10.1038/ncomms14773
PMID: 28382930

Assessing histone demethylase inhibitors in cells: lessons learned.
Hatch SB, Yapp C, Montenegro RC, Savitsky P, Gamble V, Tumber A, Ruda GF, Bavetsias V, Fedorov O, Atrash B, Raynaud F, Lanigan R, Carmichael L, Tomlin K, Burke R, Westaway SM, Brown JA, Prinjha RK, Martinez ED, Oppermann U, Schofield CJ, Bountra C, Kawamura A, Blagg J, Brennan PE, Rossanese O, Müller S
Epigenetics Chromatin. 2017 10:9. doi: 10.1186/s13072-017-0116-6
PMID: 28265301

Epigenomic regulation of oncogenesis by chromatin remodeling.
Kumar, R; Li, D-Q; Müller, S; Knapp, S;
Oncogene. 2016 35:4423-4436. doi: 10.1038/onc.2015.513
PMID: 26804164

Selective targeting of the BRG/PB1 bromodomains impairs embryonic and trophoblast stem cell maintenance.
Fedorov O, Castex J, Tallant C, Owen DR, Martin S, Aldeghi M, Monteiro O, Filippakopoulos P, Picaud S, Trzupek JD, Gerstenberger BS, Bountra C, Willmann D, Wells C, Philpott M, Rogers C, Biggin PC, Brennan PE, Bunnage ME, Schüle R, Günther T, Knapp S, Müller S
Sci Adv. 2015 1(10):e1500723. doi: 10.1126/sciadv.1500723
PMID: 26702435

Assessing cellular efficacy of bromodomain inhibitors using fluorescence recovery after photobleaching.
Philpott M, Rogers CM, Yapp C, Wells C, Lambert JP, Strain-Damerell C, Burgess-Brown NA, Gingras AC, Knapp S, Müller S
Epigenetics Chromatin. 2014 7:14. doi: 10.1186/1756-8935-7-14
PMID: 25097667

Dual kinase-bromodomain inhibitors for rationally designed polypharmacology.
Ciceri P, Müller S, O'Mahony A, Fedorov O, Filippakopoulos P, Hunt JP, Lasater EA, Pallares G, Picaud S, Wells C, Martin S, Wodicka LM, Shah NP, Treiber DK, Knapp S
Nat. Chem. Biol.. 2014 10(4):305-12. doi: 10.1038/nchembio.1471
PMID: 24584101

Structure of cyclin G-associated kinase (GAK) trapped in different conformations using nanobodies.
Chaikuad, A; Keates, T; Vincke, C; Kaufholz, M; Zenn, M; Zimmermann, B; Gutiérrez, C; Zhang, R-G; Hatzos-Skintges, C; Joachimiak, A; Muyldermans, S; Herberg, FW; Knapp, S; Müller, S;
Biochemical Journal. 2014 459:59-69. doi: 10.1042/BJ20131399
PMID: 24438162

2021

Conformational plasticity of the ULK3 kinase domain.
Mathea S, Salah E, Tallant C, Chatterjee D, Berger BT, Konietzny R, Müller-Knapp S, Kessler BM, Knapp S
Biochem J. 30.6.2021 . doi: 10.1042/BCJ20210257
PMID: 34190988

C81-evoked inhibition of the TNFR1-NFκB pathway during inflammatory processes for stabilization of the impaired vascular endothelial barrier for leukocytes.
Krishnathas GM, Strödke B, Mittmann L, Zech T, Berger LM, Reichel CA, Rösser S, Schmid T, Knapp S, Müller S, Bracher F, Fürst R, Bischoff-Kont I
FASEB J. 28.5.2021 35(6):e21656. doi: 10.1096/fj.202100037R
PMID: 34042211

Structure-kinetic relationship reveals the mechanism of selectivity of FAK inhibitors over PYK2.
Berger BT, Amaral M, Kokh DB, Nunes-Alves A, Musil D, Heinrich T, Schröder M, Neil R, Wang J, Navratilova I, Bomke J, Elkins JM, Müller S, Frech M, Wade RC, Knapp S
Cell Chem Biol. 21.1.2021 . doi: 10.1016/j.chembiol.2021.01.003
PMID: 33497606

Development of a potent and selective chemical probe for the pleiotropic kinase CK2.
Wells CI, Drewry DH, Pickett JE, Tjaden A, Krämer A, Müller S, Gyenis L, Menyhart D, Litchfield DW, Knapp S, Axtman AD
Cell Chem Biol. 11.1.2021 . doi: 10.1016/j.chembiol.2020.12.013
PMID: 33484635

The Kinase Chemogenomic Set (KCGS): An Open Science Resource for Kinase Vulnerability Identification.
Wells CI, Al-Ali H, Andrews DM, Asquith CRM, Axtman AD, Dikic I, Ebner D, Ettmayer P, Fischer C, Frederiksen M, Futrell RE, Gray NS, Hatch SB, Knapp S, Lücking U, Michaelides M, Mills CE, Müller S, Owen D, Picado A, Saikatendu KS, Schröder M, Stolz A, Tellechea M, Turunen BJ, Vilar S, Wang J, Zuercher WJ, Willson TM, Drewry DH
Int J Mol Sci. 8.1.2021 22(2):. doi: 10.3390/ijms22020566
PMID: 33429995

2020

Epigenetic Mechanisms in Canine Cancer.
Xavier PLP, Müller S, Fukumasu H
Front Oncol. 17.11.2020 10:591843. doi: 10.3389/fonc.2020.591843
PMID: 33194754

HighVia-A Flexible Live-Cell High-Content Screening Pipeline to Assess Cellular Toxicity.
Howarth A, Schröder M, Montenegro RC, Drewry DH, Heba S, Millar V, Müller S, Ebner DV
SLAS Discov. 27.5.2020 2472555220923979. doi: 10.1177/2472555220923979
PMID: 32458721

Therapeutic targeting of p300/CBP HAT domain for the treatment of NUT midline carcinoma.
Zhang X, Zegar T, Lucas A, Morrison-Smith C, Knox T, French CA, Knapp S, Müller S, Siveke JT
Oncogene. 4.5.2020 . doi: 10.1038/s41388-020-1301-9
PMID: 32366905

Quantifying Target Occupancy of Small Molecules within Living Cells
Robers MB, Friedman-Ohana R, Huber KVM, Huber KVM, Kilpatrick L, Kilpatrick L, Vasta JD, Berger BT, Chaudhry C, Hill S, Hill S, Müller S, Müller S, Knapp S, Knapp S, Knapp S, Knapp S, Wood KV, Wood KV
Annual Review of Biochemistry. 24.03.2020 89:557-581. doi: 10.1146/annurev-biochem-011420-092302
PMID: 32208767

A Highly Selective Chemical Probe for Activin Receptor-like Kinases ALK4 and ALK5.
Hanke T, Wong JF, Berger BT, Abdi I, Berger LM, Tesch R, Tredup C, Bullock AN, Müller-Knapp S, Knapp S
ACS Chem. Biol.. 16.3.2020 . doi: 10.1021/acschembio.0c00076
PMID: 32176847

Identification of molecular targets for the targeted treatment of gastric cancer using dasatinib.
Montenegro RC, Howarth A, Ceroni A, Fedele V, Farran B, Mesquita FP, Frejno M, Berger BT, Heinzlmeir S, Sailem HZ, Tesch R, Ebner D, Knapp S, Burbano R, Kuster B, Müller S
Oncotarget. 4.2.2020 11(5):535-549. doi: 10.18632/oncotarget.27462
PMID: 32082487

Hepatitis Delta Virus histone mimicry drives the recruitment of chromatin remodelers for viral RNA replication.
Abeywickrama-Samarakoon N, Cortay JC, Sureau C, Müller S, Alfaiate D, Guerrieri F, Chaikuad A, Schröder M, Merle P, Levrero M, Dény P
Nat Commun. 21.1.2020 11(1):419. doi: 10.1038/s41467-020-14299-9
PMID: 31964889

Effects of epigenetic pathway inhibitors on corticotroph tumour AtT20 cells.
Lines KE, Filippakopoulos P, Stevenson M, Muller S, Lockstone HE, Wright B, Knapp S, Buck D, Bountra C, Thakker RV
Endocr. Relat. Cancer. 1.1.2020 . doi: 10.1530/ERC-19-0448
PMID: 31935194

2019

An epigenetic screening determines BET proteins as targets to suppress self-renewal and tumorigenicity in canine mammary cancer cells.
Xavier PLP, Cordeiro YG, Alexandre PA, Pires PRL, Saranholi BH, Silva ER, Müller S, Fukumasu H
Sci Rep. 22.11.2019 9(1):17363. doi: 10.1038/s41598-019-53915-7
PMID: 31758045

A chemical toolbox for the study of bromodomains and epigenetic signaling.
Wu Q, Heidenreich D, Zhou S, Ackloo S, Krämer A, Nakka K, Lima-Fernandes E, Deblois G, Duan S, Vellanki RN, Li F, Vedadi M, Dilworth J, Lupien M, Brennan PE, Arrowsmith CH, Müller S, Fedorov O, Filippakopoulos P, Knapp S
Nat Commun. 23.4.2019 10(1):1915. doi: 10.1038/s41467-019-09672-2
PMID: 31015424

SGC-GAK-1: a chemical probe for cyclin G associated kinase (GAK).
Asquith CRM, Berger BT, Wan J, Bennett JM, Capuzzi SJ, Crona DJ, Drewry D, East MP, Elkins JM, Fedorov O, Godoi PH, Hunter DM, Knapp S, Müller S, Torrice CD, Wells CI, Earp HS, Willson T, Zuercher W
J. Med. Chem.. 15.2.2019 . doi: 10.1021/acs.jmedchem.8b01213
PMID: 30768268

WNT Activates the AAK1 Kinase to Promote Clathrin-Mediated Endocytosis of LRP6 and Establish a Negative Feedback Loop.
Agajanian MJ, Walker MP, Axtman AD, Ruela-de-Sousa RR, Serafin DS, Rabinowitz AD, Graham DM, Ryan MB, Tamir T, Nakamichi Y, Gammons MV, Bennett JM, Couñago RM, Drewry DH, Elkins JM, Gileadi C, Gileadi O, Godoi PH, Kapadia N, Müller S, Santiago AS, Sorrell FJ, Wells CI, Fedorov O, Willson TM, Zuercher WJ, Major MB
Cell Rep. 2.1.2019 26(1):79-93.e8. doi: 10.1016/j.celrep.2018.12.023
PMID: 30605688

2018

NVP-BHG712: Effects of Regioisomers on the Affinity and Selectivity toward the EPHrin Family.
Tröster A, Heinzlmeir S, Berger BT, Gande SL, Saxena K, Sreeramulu S, Linhard V, Nasiri AH, Bolte M, Müller S, Kuster B, Médard G, Kudlinzki D, Schwalbe H
ChemMedChem. 20.8.2018 13(16):1629-1633. doi: 10.1002/cmdc.201800398
PMID: 29928781

Development, Optimization and Structure-Activity Relationships of Covalent-Reversible JAK3 Inhibitors Based on a Tricyclic Imidazo[5,4-d]pyrrolo[2,3-b]pyridine Scaffold.
Forster M, Chaikuad A, Dimitrov T, Döring E, Holstein J, Berger BT, Gehringer M, Ghoreschi K, Müller S, Knapp S, Laufer SA
J. Med. Chem.. 31.5.2018 . doi: 10.1021/acs.jmedchem.8b00571
PMID: 29852068

Donated chemical probes for open science.
Müller S, Ackloo S, Arrowsmith CH, Bauser M, Baryza JL, Blagg J, Böttcher J, Bountra C, Brown PJ, Bunnage ME, Carter AJ, Damerell D, Dötsch V, Drewry DH, Edwards AM, Edwards J, Elkins JM, Fischer C, Frye SV, Gollner A, Grimshaw CE, IJzerman A, Hanke T, Hartung IV, Hitchcock S, Howe T, Hughes TV, Laufer S, Li VM, Liras S, Marsden BD, Matsui H, Mathias J, O'Hagan RC, Owen DR, Pande V, Rauh D, Rosenberg SH, Roth BL, Schneider NS, Scholten C, Singh Saikatendu K, Simeonov A, Takizawa M, Tse C, Thompson PR, Treiber DK, Viana AY, Wells CI, Willson TM, Zuercher WJ, Knapp S, Mueller-Fahrnow A
Elife. 20.4.2018 7:. doi: 10.7554/eLife.34311
PMID: 29676732

2017

Quantitative, Wide-Spectrum Kinase Profiling in Live Cells for Assessing the Effect of Cellular ATP on Target Engagement.
Vasta JD, Corona CR, Wilkinson J, Zimprich CA, Hartnett JR, Ingold MR, Zimmerman K, Machleidt T, Kirkland TA, Huwiler KG, Ohana RF, Slater M, Otto P, Cong M, Wells CI, Berger BT, Hanke T, Glas C, Ding K, Drewry DH, Huber KVM, Willson TM, Knapp S, Müller S, Meisenheimer PL, Fan F, Wood KV, Robers MB
Cell Chem Biol. 13.11.2017 . doi: 10.1016/j.chembiol.2017.10.010
PMID: 29174542

Discovery of a highly selective cell-active inhibitor of KDM2/7.
Gerken P, Wolstenhulme J, Tumber A, Hatch S, Zhang Y, Müller S, Chandler S, Mair B, Li F, Nijman S, Konietzny R, Szommer T, Yapp C, Fedorov O, Benesch J, Vedadi M, Kessler B, Kawamura A, Brennan P, Smith MD
Angew. Chem. Int. Ed. Engl.. 4.10.2017 . doi: 10.1002/anie.201706788
PMID: 28976073

Selective targeting of Bromodomains of the Bromodomain-PHD Fingers family impairs osteoclast differentiation.
Meier JC, Tallant C, Fedorov O, Witwicka H, Hwang SY, van Stiphout RG, Lambert JP, Rogers C, Yapp C, Gerstenberger BS, Fedele V, Savitsky P, Heidenreich D, Daniels DL, Owen DR, Fish PV, Igoe NM, Bayle ED, Haendler B, Oppermann UCT, Buffa F, Brennan PE, Müller S, Gingras AC, Odgren PR, Birnbaum MJ, Knapp S
ACS Chem. Biol.. 29.8.2017 . doi: 10.1021/acschembio.7b00481
PMID: 28849908

Progress towards a public chemogenomic set for protein kinases and a call for contributions.
Drewry DH, Wells CI, Andrews DM, Angell R, Al-Ali H, Axtman AD, Capuzzi SJ, Elkins JM, Ettmayer P, Frederiksen M, Gileadi O, Gray N, Hooper A, Knapp S, Laufer S, Luecking U, Michaelides M, Müller S, Muratov E, Denny RA, Saikatendu KS, Treiber DK, Zuercher WJ, Willson TM
PLoS ONE. 3.8.2017 12(8):e0181585. doi: 10.1371/journal.pone.0181585
PMID: 28767711

Design of a chemical probe for the Bromodomain and Plant Homeodomain Finger-containing (BRPF) family of proteins.
Igoe N, Bayle ED, Tallant C, Fedorov O, Meier JC, Savitsky P, Rogers C, Morias Y, Scholze S, Boyd H, Cunoosamy D, Andrews DM, Cheasty A, Brennan PE, Müller S, Knapp S, Fish PV
J. Med. Chem.. 17.7.2017 . doi: 10.1021/acs.jmedchem.7b00611
PMID: 28714688

In Vivo Biotinylation of Antigens in E. coli.
Gräslund S, Savitsky P, Müller-Knapp S
Methods Mol. Biol.. 5.5.2017 1586:337-344. doi: 10.1007/978-1-4939-6887-9_22
PMID: 28470616

Benzo-isoquinoline-diones As Potent and Selective Inhibitors of BRPF2 and TAF1/TAF1L Bromodomains.
Bouché L, Christ CD, Siegel S, Fernández-Montalván AE, Holton SJ, Fedorov O, Ter Laak A, Sugawara T, Stöckigt D, Tallant C, Bennett JM, Monteiro OP, Díaz-Sáez L, Siejka P, Meier J, Puetter V, Weiske J, Müller S, Huber KV, Hartung IV, Haendler B
J. Med. Chem.. 12.4.2017 . doi: 10.1021/acs.jmedchem.7b00306
PMID: 28402630

Highly selective inhibition of histone demethylases by de novo macrocyclic peptides.
Kawamura A, Münzel M, Kojima T, Yapp C, Bhushan B, Goto Y, Tumber A, Katoh T, King ON, Passioura T, Walport LJ, Hatch SB, Madden S, Müller S, Brennan PE, Chowdhury R, Hopkinson RJ, Suga H, Schofield CJ
Nat Commun. 6.4.2017 8:14773. doi: 10.1038/ncomms14773
PMID: 28382930

Assessing histone demethylase inhibitors in cells: lessons learned.
Hatch SB, Yapp C, Montenegro RC, Savitsky P, Gamble V, Tumber A, Ruda GF, Bavetsias V, Fedorov O, Atrash B, Raynaud F, Lanigan R, Carmichael L, Tomlin K, Burke R, Westaway SM, Brown JA, Prinjha RK, Martinez ED, Oppermann U, Schofield CJ, Bountra C, Kawamura A, Blagg J, Brennan PE, Rossanese O, Müller S
Epigenetics Chromatin. 8.3.2017 10:9. doi: 10.1186/s13072-017-0116-6
PMID: 28265301

Potent and Selective KDM5 Inhibitor Stops Cellular Demethylation of H3K4me3 at Transcription Start Sites and Proliferation of MM1S Myeloma Cells.
Tumber A, Nuzzi A, Hookway ES, Hatch SB, Velupillai S, Johansson C, Kawamura A, Savitsky P, Yapp C, Szykowska A, Wu N, Bountra C, Strain-Damerell C, Burgess-Brown NA, Ruda GF, Fedorov O, Munro S, England KS, Nowak RP, Schofield CJ, La Thangue NB, Pawlyn C, Davies F, Morgan G, Athanasou N, Müller S, Oppermann U, Brennan PE
Cell Chem Biol. 27.2.2017 . doi: 10.1016/j.chembiol.2017.02.006
PMID: 28262558

Design of a Biased Potent Small Molecule Inhibitor of the Bromodomain and PHD Finger-Containing (BRPF) Proteins Suitable for Cellular and in Vivo Studies.
Igoe N, Bayle ED, Fedorov O, Tallant C, Savitsky P, Rogers C, Owen DR, Deb G, Somervaille TC, Andrews DM, Jones N, Cheasty A, Ryder H, Brennan PE, Müller S, Knapp S, Fish PV
J. Med. Chem.. 9.1.2017 . doi: 10.1021/acs.jmedchem.6b01583
PMID: 28068087

2016

Promiscuous targeting of bromodomains by bromosporine identifies BET proteins as master regulators of primary transcription response in leukemia.
Picaud S, Leonards K, Lambert JP, Dovey O, Wells C, Fedorov O, Monteiro O, Fujisawa T, Wang CY, Lingard H, Tallant C, Nikbin N, Guetzoyan L, Ingham R, Ley SV, Brennan P, Muller S, Samsonova A, Gingras AC, Schwaller J, Vassiliou G, Knapp S, Filippakopoulos P
Sci Adv. 21.10.2016 2(10):e1600760. doi: 10.1126/sciadv.1600760
PMID: 27757418

Development of Selective CBP/P300 Benzoxazepine Bromodomain Inhibitors.
Popp TA, Tallant C, Rogers C, Fedorov O, Brennan PE, Müller S, Knapp S, Bracher F
J. Med. Chem.. 27.9.2016 . doi: 10.1021/acs.jmedchem.6b00774
PMID: 27673482

Discovery and optimization of a selective ligand for the Switch/Sucrose Non-Fermenting-related bromodomains of Polybromo protein-1 by the use of virtual screening and hydration analysis.
Myrianthopoulos V, Gaboriaud-Kolar N, Tallant C, Hall ML, Grigoriou S, Brownlee PM, Fedorov O, Rogers C, Heidenreich D, Wanior M, Drosos N, Mexia N, Savitsky P, Bagratuni T, Kastritis E, Terpos E, Filippakopoulos P, Müller S, Skaltsounis AL, Downs JA, Knapp S, Mikros E
J. Med. Chem.. 12.9.2016 . doi: 10.1021/acs.jmedchem.6b00355
PMID: 27617704

Generation and analyses of human synthetic antibody libraries and their application for protein microarrays.
Säll A, Walle M, Wingren C, Müller S, Nyman T, Vala A, Ohlin M, Borrebaeck CA, Persson H
Protein Eng. Des. Sel.. 1.9.2016 . doi: 10.1093/protein/gzw042
PMID: 27590051

Targeting the Bromome: are we there yet?
Müller S
Future Med Chem. 31.8.2016 . doi: 10.4155/fmc-2016-0136
PMID: 27578167

BET inhibition as a new strategy for the treatment of gastric cancer.
Montenegro RC, Clark PG, Howarth A, Wan X, Ceroni A, Siejka P, Nunez-Alonso GA, Monteiro O, Rogers C, Gamble V, Burbano R, Brennan PE, Tallant C, Ebner D, Fedorov O, O'Neill E, Knapp S, Dixon D, Müller S
Oncotarget. 1.6.2016 . doi: 10.18632/oncotarget.9766
PMID: 27259267

Protein-protein interaction inhibition (2P2I)-oriented chemical library accelerates hit discovery.
Milhas S, Raux B, Betzi S, Derviaux C, Roche P, Restouin A, Basse MJ, Rebuffet E, Lugari A, Badol M, Kashyap R, Lissitzky JC, Eydoux C, Hamon V, Gourdel ME, Combes S, Zimmermann P, Aurrand-Lions M, Roux T, Rogers C, Müller S, Knapp S, Trinquet E, Collette Y, Guillemot JC, Morelli X
ACS Chem. Biol.. 24.5.2016 . doi: 10.1021/acschembio.6b00286
PMID: 27219844

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
Nat. Chem. Biol.. 9.5.2016 . doi: 10.1038/nchembio.2080
PMID: 27159579

Identification and development of 2,3-dihydropyrrolo[1,2-a]quinazolin-5(1H)-one inhibitors targeting bromodomains within the Switch/Sucrose Non-Fermenting complex.
Sutherell CL, Tallant C, Monteiro OP, Yapp C, Fuchs JE, Fedorov O, Siejka P, Müller S, Knapp S, Brenton JD, Brennan PE, Ley SV
J. Med. Chem.. 27.4.2016 . doi: 10.1021/acs.jmedchem.5b01997
PMID: 27119626

Identification of a chemical probe for family VIII bromodomains through optimization of a fragment hit.
Gerstenberger BS, Trzupek JD, Tallant C, Fedorov O, Filippakopoulos P, Brennan PE, Fedele V, Martin S, Picaud S, Rogers CM, Parikh MD, Taylor A, Samas BM, O'Mahony A, Berg EL, Pallares G, Torrey AV, Treiber DK, Samardjiev IJ, Nasipak BT, Padilla-Benavides T, Wu Q, Imbalzano AN, Nickerson JA, Bunnage ME, Müller S, Knapp S, Owen DR
J. Med. Chem.. 26.4.2016 . doi: 10.1021/acs.jmedchem.6b00012
PMID: 27115555

Structure-based design of an in vivo active selective BRD9 inhibitor.
Martin LJ, Koegl M, Bader G, Cockcroft XL, Fedorov O, Fiegen D, Gerstberger T, Hofmann MH, Hohmann AF, Kessler D, Knapp S, Knesl P, Kornigg S, Müller S, Nar H, Rogers C, Rumpel K, Schaaf O, Steurer S, Tallant C, Vakoc CR, Zeeb M, Zoephel A, Pearson M, Boehmelt G, McConnell D
J. Med. Chem.. 25.2.2016 . doi: 10.1021/acs.jmedchem.5b01865
PMID: 26914985

Frapid: achieving full automation of FRAP for chemical probe validation.
Yapp C, Rogers C, Savitsky P, Philpott M, Müller S
Biomed Opt Express. 1.2.2016 7(2):422-41. doi: 10.1364/BOE.7.000422
PMID: 26977352

8-Substituted Pyrido[3,4-d]pyrimidin-4(3H)-one Derivatives As Potent, Cell Permeable, KDM4 (JMJD2) and KDM5 (JARID1) Histone Lysine Demethylase Inhibitors.
Bavetsias V, Lanigan RM, Ruda GF, Atrash B, McLaughlin MG, Tumber A, Mok NY, Le Bihan YV, Dempster S, Boxall KJ, Jeganathan F, Hatch SB, Savitsky P, Velupillai S, Krojer T, England KS, Sejberg J, Thai C, Donovan A, Pal A, Scozzafava G, Bennett JM, Kawamura A, Johansson C, Szykowska A, Gileadi C, Burgess-Brown NA, von Delft F, Oppermann U, Walters Z, Shipley J, Raynaud FI, Westaway SM, Prinjha RK, Fedorov O, Burke R, Schofield CJ, Westwood IM, Bountra C, Müller S, van Montfort RL, Brennan PE, Blagg J
J. Med. Chem.. 7.1.2016 . doi: 10.1021/acs.jmedchem.5b01635
PMID: 26741168

Structure-based identification of inhibitory fragments targeting the p300/CBP-associated factor bromodomain.
Chaikuad A, Lang S, Brennan PE, Temperini C, Fedorov O, Hollander J, Nachane R, Abell C, Müller S, Siegal G, Knapp S
J. Med. Chem.. 5.1.2016 . doi: 10.1021/acs.jmedchem.5b01719
PMID: 26731131

2015

Selective targeting of the BRG/PB1 bromodomains impairs embryonic and trophoblast stem cell maintenance.
Fedorov O, Castex J, Tallant C, Owen DR, Martin S, Aldeghi M, Monteiro O, Filippakopoulos P, Picaud S, Trzupek JD, Gerstenberger BS, Bountra C, Willmann D, Wells C, Philpott M, Rogers C, Biggin PC, Brennan PE, Bunnage ME, Schüle R, Günther T, Knapp S, Müller S
Sci Adv. 13.11.2015 1(10):e1500723. doi: 10.1126/sciadv.1500723
PMID: 26702435

Generation of a selective small molecule inhibitor of the CBP/p300 bromodomain for leukemia therapy.
Picaud S, Fedorov O, Thanasopoulou A, Leonards K, Jones K, Meier J, Olzscha H, Monteiro O, Martin S, Philpott M, Tumber A, Filippakopoulos P, Yapp C, Wells C, Hing Che K, Bannister A, Robson S, Kumar U, Parr N, Lee K, Lugo D, Jeffrey P, Taylor S, Vecellio ML, Bountra C, Brennan P, O'Mahony A, Velichko S, Muller S, Hay D, Daniels DL, Urh M, La Thangue NB, Kouzarides T, Prinjha R, Schwaller J, Knapp S
Cancer Res.. 9.11.2015 . doi: 10.1158/0008-5472.CAN-15-0236
PMID: 26552700

Comprehensive characterization of the Published Kinase Inhibitor Set.
Elkins JM, Fedele V, Szklarz M, Abdul Azeez KR, Salah E, Mikolajczyk J, Romanov S, Sepetov N, Huang XP, Roth BL, Al Haj Zen A, Fourches D, Muratov E, Tropsha A, Morris J, Teicher BA, Kunkel M, Polley E, Lackey KE, Atkinson FL, Overington JP, Bamborough P, Müller S, Price DJ, Willson TM, Drewry DH, Knapp S, Zuercher WJ
Nat. Biotechnol.. 26.10.2015 . doi: 10.1038/nbt.3374
PMID: 26501955

The ins and outs of selective kinase inhibitor development.
Müller S, Chaikuad A, Gray NS, Knapp S
Nat. Chem. Biol.. 20.10.2015 11(11):818-21. doi: 10.1038/nchembio.1938
PMID: 26485069

Open access chemical probes for epigenetic targets.
Brown PJ, Müller S
Future Med Chem. 23.9.2015 . doi: 10.4155/fmc.15.127
PMID: 26397018

CBP30, a selective CBP/p300 bromodomain inhibitor, suppresses human Th17 responses.
Hammitzsch A, Tallant C, Fedorov O, O'Mahony A, Brennan PE, Hay DA, Martinez FO, Al-Mossawi MH, de Wit J, Vecellio M, Wells C, Wordsworth P, Müller S, Knapp S, Bowness P
Proc. Natl. Acad. Sci. U.S.A.. 10.8.2015 . doi: 10.1073/pnas.1501956112
PMID: 26261308

The promise and peril of chemical probes.
Arrowsmith CH, Audia JE, Austin C, Baell J, Bennett J, Blagg J, Bountra C, Brennan PE, Brown PJ, Bunnage ME, Buser-Doepner C, Campbell RM, Carter AJ, Cohen P, Copeland RA, Cravatt B, Dahlin JL, Dhanak D, Edwards AM, Frye SV, Gray N, Grimshaw CE, Hepworth D, Howe T, Huber KV, Jin J, Knapp S, Kotz JD, Kruger RG, Lowe D, Mader MM, Marsden B, Mueller-Fahrnow A, Müller S, O'Hagan RC, Overington JP, Owen DR, Rosenberg SH, Roth B, Ross R, Schapira M, Schreiber SL, Shoichet B, Sundström M, Superti-Furga G, Taunton J, Toledo-Sherman L, Walpole C, Walters MA, Willson TM, Workman P, Young RN, Zuercher WJ
Nat. Chem. Biol.. 21.7.2015 11(8):536-41. doi: 10.1038/nchembio.1867
PMID: 26196764

Discovery of a Chemical Tool Inhibitor Targeting the Bromodomains of TRIM24 and BRPF.
Bennett JM, Fedorov O, Tallant C, Monteiro OP, Meier J, Gamble V, Savitski P, Nunez-Alonso GA, Haendler B, Rogers C, Brennan PE, Müller S, Knapp S
J. Med. Chem.. 14.5.2015 . doi: 10.1021/acs.jmedchem.5b00458
PMID: 25974391

LP99: Discovery and Synthesis of the First Selective BRD7/9 Bromodomain Inhibitor.
Clark PG, Vieira LC, Tallant C, Fedorov O, Singleton DC, Rogers CM, Monteiro OP, Bennett JM, Baronio R, Müller S, Daniels DL, Méndez J, Knapp S, Brennan PE, Dixon DJ
Angew. Chem. Int. Ed. Engl.. 13.4.2015 . doi: 10.1002/anie.201501394
PMID: 25864491

Discovery and characterization of GSK2801, a selective chemical probe for the bromodomains BAZ2A and BAZ2B.
Chen P, Chaikuad A, Bamborough P, Bantscheff M, Bountra C, Chung CW, Fedorov O, Grandi P, Jung D, Lesniak R, Lindon M, Müller S, Philpott M, Prinjha RK, Rogers CM, Selenski C, Tallant C, Werner T, Willson TM, Knapp S, Drewry DH
J. Med. Chem.. 23.3.2015 . doi: 10.1021/acs.jmedchem.5b00209
PMID: 25799074

Structure Enabled Design of BAZ2-ICR, A Chemical Probe Targeting the Bromodomains of BAZ2A and BAZ2B.
Drouin L, McGrath S, Vidler LR, Chaikuad A, Monteiro O, Tallant C, Philpott M, Rogers C, Fedorov O, Liu M, Akhtar W, Hayes A, Raynaud F, Müller S, Knapp S, Hoelder S
J. Med. Chem.. 26.2.2015 . doi: 10.1021/jm501963e
PMID: 25719566

2014

Corrigendum: Dual kinase-bromodomain inhibitors for rationally designed polypharmacology.
Ciceri P, Müller S, O'Mahony A, Fedorov O, Filippakopoulos P, Hunt JP, Lasater EA, Pallares G, Picaud S, Wells C, Martin S, Wodicka LM, Shah NP, Treiber DK, Knapp S
Nat. Chem. Biol.. 18.7.2014 10(8):692. doi:
PMID: 25036311

Assessing cellular efficacy of bromodomain inhibitors using fluorescence recovery after photobleaching.
Philpott M, Rogers CM, Yapp C, Wells C, Lambert JP, Strain-Damerell C, Burgess-Brown NA, Gingras AC, Knapp S, Müller S
Epigenetics Chromatin. 13.7.2014 7:14. doi: 10.1186/1756-8935-7-14
PMID: 25097667

Discovery and Optimization of Small-Molecule Ligands for the CBP/p300 Bromodomains.
Hay DA, Fedorov O, Martin S, Singleton DC, Tallant C, Wells C, Picaud S, Philpott M, Monteiro OP, Rogers CM, Conway SJ, Rooney TP, Tumber A, Yapp C, Filippakopoulos P, Bunnage ME, Müller S, Knapp S, Schofield CJ, Brennan PE
J. Am. Chem. Soc.. 2.7.2014 136(26):9308-19. doi: 10.1021/ja412434f
PMID: 24946055

A Series of Potent CREBBP Bromodomain Ligands Reveals an Induced-Fit Pocket Stabilized by a Cation-π Interaction.
Rooney TP, Filippakopoulos P, Fedorov O, Picaud S, Cortopassi WA, Hay DA, Martin S, Tumber A, Rogers CM, Philpott M, Wang M, Thompson AL, Heightman TD, Pryde DC, Cook A, Paton RS, Müller S, Knapp S, Brennan PE, Conway SJ
Angew. Chem. Int. Ed. Engl.. 12.5.2014 . doi: 10.1002/anie.201402750
PMID: 24821300

Dual kinase-bromodomain inhibitors for rationally designed polypharmacology.
Ciceri P, Müller S, O'Mahony A, Fedorov O, Filippakopoulos P, Hunt JP, Lasater EA, Pallares G, Picaud S, Wells C, Martin S, Wodicka LM, Shah NP, Treiber DK, Knapp S
Nat. Chem. Biol.. 2.3.2014 10(4):305-12. doi: 10.1038/nchembio.1471
PMID: 24584101

Structure of Cyclin G associated kinase (GAK) Trapped in different Conformations using Nanobodies.
Chaikuad A, Keates T, Vincke C, Kaufholz M, Zenn M, Zimmermann B, Gutiérrez C, Zhang RG, Hatzos-Skintges C, Joachimiak A, Muyldermans S, Herberg FW, Knapp S, Müller S
Biochem. J.. 17.1.2014 . doi: 10.1042/BJ20131399
PMID: 24438162

2013

[1,2,4]Triazolo[4,3-a]phthalazines: inhibitors of diverse bromodomains.
Fedorov O, Lingard H, Wells C, Monteiro OP, Picaud S, Keates T, Yapp C, Philpott M, Martin SJ, Felletar I, Marsden B, Filippakopoulos P, Muller-Knapp S, Knapp S, Brennan PE
J. Med. Chem.. 8.12.2013 . doi: 10.1021/jm401568s
PMID: 24313754

RVX-208, an inhibitor of BET transcriptional regulators with selectivity for the second bromodomain.
Picaud S, Wells C, Felletar I, Brotherton D, Martin S, Savitsky P, Diez-Dacal B, Philpott M, Bountra C, Lingard H, Fedorov O, Müller S, Brennan PE, Knapp S, Filippakopoulos P
Proc. Natl. Acad. Sci. U.S.A.. 18.11.2013 . doi: 10.1073/pnas.1310658110
PMID: 24248379

5-Carboxy-8-hydroxyquinoline is a Broad Spectrum 2-Oxoglutarate Oxygenase Inhibitor which Causes Iron Translocation.
Hopkinson RJ, Tumber A, Yapp C, Chowdhury R, Aik W, Che KH, Li XS, Kristensen JB, King ON, Chan MC, Yeoh KK, Choi H, Walport LJ, Thinnes CC, Bush JT, Lejeune C, Rydzik AM, Rose NR, Bagg EA, McDonough MA, Krojer T, Yue WW, Ng SS, Olsen L, Brennan PE, Oppermann U, Muller-Knapp S, Klose RJ, Ratcliffe PJ, Schofield CJ, Kawamura A
Chem Sci. 1.8.2013 4(8):3110-3117. doi: 10.1039/C3SC51122G
PMID: 26682036

PFI-1, a Highly Selective Protein Interaction Inhibitor, Targeting BET Bromodomains.
Picaud S, Da Costa D, Thanasopoulou A, Filippakopoulos P, Fish PV, Philpott M, Fedorov O, Brennan P, Bunnage ME, Owen DR, Bradner JE, Taniere P, O'Sullivan B, Müller S, Schwaller J, Stankovic T, Knapp S
Cancer Res.. 1.6.2013 73(11):3336-3346. doi: 10.1158/0008-5472.CAN-12-3292
PMID: 23576556

Inhibition of BET Bromodomain Targets Genetically Diverse Glioblastoma.
Cheng Z, Gong Y, Ma Y, Lu K, Lu X, Pierce LA, Thompson RC, Muller S, Knapp S, Wang J
Clin. Cancer Res.. 26.3.2013 . doi: 10.1158/1078-0432.CCR-12-3066
PMID: 23403638

2012

Plant growth regulator daminozide is a selective inhibitor of human KDM2/7 histone demethylases.
Rose NR, Woon EC, Tumber A, Walport LJ, Chowdhury R, Li XS, King ON, Lejeune C, Ng SS, Krojer T, Chan MC, Rydzik AM, Hopkinson RJ, Che KH, Daniel M, Strain-Damerell C, Gileadi C, Kochan G, Leung IK, Dunford J, Yeoh KK, Ratcliffe PJ, Burgess-Brown N, von Delft F, Muller S, Marsden B, Brennan PE, McDonough MA, Oppermann U, Klose RJ, Schofield CJ, Kawamura A
J. Med. Chem.. 26.7.2012 55(14):6639-43. doi: 10.1021/jm300677j
PMID: 22724510

Expressing the human proteome for affinity proteomics: optimising expression of soluble protein domains and in vivo biotinylation.
Keates T, Cooper CD, Savitsky P, Allerston CK, Phillips C, Hammarström M, Daga N, Berridge G, Mahajan P, Burgess-Brown NA, Müller S, Gräslund S, Gileadi O
N Biotechnol. 15.6.2012 29(5):515-25. doi: 10.1016/j.nbt.2011.10.007
PMID: 22027370

Histone recognition and large-scale structural analysis of the human bromodomain family.
Filippakopoulos P, Picaud S, Mangos M, Keates T, Lambert JP, Barsyte-Lovejoy D, Felletar I, Volkmer R, Müller S, Pawson T, Gingras AC, Arrowsmith CH, Knapp S
Cell. 30.3.2012 149(1):214-31. doi: 10.1016/j.cell.2012.02.013
PMID: 22464331

2011

Bromodomains as therapeutic targets.
Muller S, Filippakopoulos P, Knapp S
Expert Rev Mol Med. 22.9.2011 13:e29. doi: 10.1017/S1462399411001992
PMID: 21933453

Structural basis of fumarate hydratase deficiency.
Picaud S, Kavanagh KL, Yue WW, Lee WH, Muller-Knapp S, Gileadi O, Sacchettini J, Oppermann U
J. Inherit. Metab. Dis.. 29.3.2011 34(3):671-6. doi: 10.1007/s10545-011-9294-8
PMID: 21445611

2010

Targeting kinases for the treatment of inflammatory diseases.
Müller S, Knapp S
Expert Opin Drug Discov. 15.7.2010 5(9):867-81. doi: 10.1517/17460441.2010.504203
PMID: 22823261

HMGB1 protein inhibitors and/or antagonists for the treatment of vascular diseases.
Muller-Knapp, S; Bianchi, ME; Bonaldi, T; Scaffidi, P; Degryse, B;
. 8 July 2010 :-. doi: US-2010172896-A1
PMID:

The (un)targeted cancer kinome.
Fedorov O, Müller S, Knapp S
Nat. Chem. Biol.. 16.2.2010 6(3):166-169. doi: 10.1038/nchembio.297
PMID: 20154661

Open-access public-private partnerships to enable drug discovery--new approaches.
Müller S, Weigelt J
IDrugs. 3.2010 13(3):175-80. doi:
PMID: 20191434

2009

SH2 domains: modulators of nonreceptor tyrosine kinase activity.
Filippakopoulos P, Müller S, Knapp S
Curr. Opin. Struct. Biol.. 18.11.2009 19(6):643-9. doi: 10.1016/j.sbi.2009.10.001
PMID: 19926274

Large-scale structural analysis of the classical human protein tyrosine phosphatome.
Barr AJ, Ugochukwu E, Lee WH, King ON, Filippakopoulos P, Alfano I, Savitsky P, Burgess-Brown NA, Müller S, Knapp S
Cell. 23.1.2009 136(2):352-63. doi: 10.1016/j.cell.2008.11.038
PMID: 19167335

2007

A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases.
Fedorov O, Marsden B, Pogacic V, Rellos P, Müller S, Bullock AN, Schwaller J, Sundström M, Knapp S
Proc. Natl. Acad. Sci. U.S.A.. 18.12.2007 104(51):20523-8. doi: 10.1073/pnas.0708800104
PMID: 18077363

Structural and functional characterization of the human protein kinase ASK1.
Bunkoczi G, Salah E, Filippakopoulos P, Fedorov O, Müller S, Sobott F, Parker SA, Zhang H, Min W, Turk BE, Knapp S
Structure. 17.10.2007 15(10):1215-26. doi: 10.1016/j.str.2007.08.011
PMID: 17937911

The scientific impact of the Structural Genomics Consortium: a protein family and ligand-centered approach to medically-relevant human proteins.
Gileadi O, Knapp S, Lee WH, Marsden BD, Müller S, Niesen FH, Kavanagh KL, Ball LJ, von Delft F, Doyle DA, Oppermann UC, Sundström M
J. Struct. Funct. Genomics. 12.10.2007 8(2-3):107-19. doi: 10.1007/s10969-007-9027-2
PMID: 17932789

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