Alex Bullock trained at the University of Cambridge in biochemistry. His PhD research under the mentorship of Sir Alan Fersht characterised the folding and stability of mutant p53 and stimulated efforts to identify chemical chaperones that rescued mutant p53 activity in cancer cells. He was subsequently awarded a Wellcome Trust International Prize Travelling Research Fellowship, which he began in the group of David Baker at the University of Washington, Seattle. There he established methods to redesign protein-protein interaction specificity using the computer algorithm Rosetta. Alex concluded his fellowship with Sir Peter Ratcliffe at the University of Oxford. He demonstrated the oxygen dependence of the HIF-asparagine hydroxylase that regulates HIF-p300 interaction and performed proteomic studies with the VHL ubiquitin ligase. Alex helped to launch the SGC in 2004 working initially as a team leader on protein kinases with Stefan Knapp. He established the Growth Factor Signalling group in 2008.

 

Research Areas

The Growth Factor Signalling group is interested in the signalling pathways that control cell growth and differentiation and how these might be targeted by small molecule inhibitors to address devastating diseases such as cancer and inflammation. Our work is particularly focussed on the cross talk that regulates protein phosphorylation and ubiquitylation. We aim to understand the molecular structure and function of protein kinases and E3 ubiquitin ligases and to characterize their binding to substrates, regulatory partners and chemical inhibitors. This work involves a multidisciplinary approach using structural, chemical and cell biology as well as many collaborative studies with colleagues across industry and academia. Recent interests include the BMP/TGFβ receptor kinases which control the differentiation of stem cells and tissue morphogenesis. Dysregulation of these pathways is a common event in cancer as well as in many rare developmental disorders. In particular, we are working with FOP Action UK to develop BMP inhibitors for the treatment of fibrodysplasia ossificans progressiva (FOP). We are also interested in Cullin-RING E3 ligases such as KEAP1, which is a potential drug target in neurodegenerative conditions including Huntington’s disease.

Group Members

  • Daniel Pinkas
  • Eleanor Williams
  • Georgina Kerr
  • Sergio Galan
  • Caroline Sanvitale
  • Joshua Bufton
  • Sarah Dixon-Clarke
  • Zhuoyao Chen

Publications

Structural Basis of Intracellular TGF-β Signaling: Receptors and Smads.
Chaikuad, A; Bullock, AN;
Cold Spring Harbor perspectives in biology. 2016 :-. doi:
PMID: 27549117

Covalent targeting of remote cysteine residues to develop CDK12 and CDK13 inhibitors.
Zhang, T; Kwiatkowski, N; Olson, CM; Dixon-Clarke, SE; Abraham, BJ; Greifenberg, AK; Ficarro, SB; Elkins, JM; Liang, Y; Hannett, NM; Manz, T; Hao, M; Bartkowiak, B; Greenleaf, AL; Marto, JA; Geyer, M; Bullock, AN; Young, RA; Gray, NS;
Nature Chemical Biology. 2016 12:876-884. doi:
PMID: 27571479

CIS is a potent checkpoint in NK cell-mediated tumor immunity.
Delconte, RB; Kolesnik, TB; Dagley, LF; Rautela, J; Shi, W; Putz, EM; Stannard, K; Zhang, JG; Teh, C; Firth, M; Ushiki, T; Andoniou, CE; Degli-Esposti, MA; Sharp, PP; Sanvitale, CE; Infusini, G; Liau, NP; Linossi, EM; Burns, CJ; Carotta, S; Gray, DH; Seillet, C; Hutchinson, DS; Belz, GT; Webb, AI; Alexander, WS; Li, SS; Bullock, AN; Babon, JJ; Smyth, MJ; Nicholson, SE; Huntington, ND;
Nature Immunology. 2016 17:816-824. doi:
PMID: 27213690

Inflammatory Signaling by NOD-RIPK2 Is Inhibited by Clinically Relevant Type II Kinase Inhibitors.
Canning, P; Ruan, Q; Schwerd, T; Hrdinka, M; Maki, JL; Saleh, D; Suebsuwong, C; Ray, S; Brennan, PE; Cuny, GD; Uhlig, HH; Gyrd-Hansen, M; Degterev, A; Bullock, AN;
Chemistry and Biology. 2015 22:1174-1184. doi:
PMID: 26320862

ACVR1 mutations in DIPG: lessons learned from FOP.
Taylor, KR; Vinci, M; Bullock, AN; Jones, C;
Cancer Research. 2014 74:4565-4570. doi:
PMID: 25136070

Recurrent activating ACVR1 mutations in diffuse intrinsic pontine glioma
Taylor, KR; Mackay, A; Truffaux, N; Butterfield, YS; Morozova, O; Philippe, C; Castel, D; Grasso, CS; Vinci, M; Carvalho, D; Carcaboso, AM; de Torres, C; Cruz, O; Mora, J; Entz-Werle, N; Ingram, WJ; Monje, M; Hargrave, D; Bullock, AN; Puget, S; Yip, S; Jones, C; Grill, J;
Nature Genetics. 2014 46:457-461. doi: 10.1038/ng.2925
PMID:

Structural and biochemical characterization of the KLHL3-WNK kinase interaction important in blood pressure regulation.
Schumacher, FR; Sorrell, FJ; Alessi, DR; Bullock, AN; Kurz, T;
Biochemical Journal. 2014 460:237-246. doi:
PMID: 24641320

New strategies to inhibit KEAP1 and the Cul3-based E3 ubiquitin ligases.
Canning, P; Bullock, AN;
Biochemical Society Transactions. 2014 42:103-107. doi: 10.1042/BST20130215
PMID: 24450635

The p53 cofactor Strap exhibits an unexpected TPR motif and oligonucleotide-binding (OB)-fold structure.
Adams, CJ; Pike, AC; Maniam, S; Sharpe, TD; Coutts, AS; Knapp, S; La Thangue, NB; Bullock, AN;
Proceedings of the National Academy of Sciences of USA. 2012 109:3778-3783. doi: 10.1073/pnas.1113731109
PMID: 22362889

2016

Covalent targeting of remote cysteine residues to develop CDK12 and CDK13 inhibitors.
Zhang, T; Kwiatkowski, N; Olson, CM; Dixon-Clarke, SE; Abraham, BJ; Greifenberg, AK; Ficarro, SB; Elkins, JM; Liang, Y; Hannett, NM; Manz, T; Hao, M; Bartkowiak, B; Greenleaf, AL; Marto, JA; Geyer, M; Bullock, AN; Young, RA; Gray, NS;
Nature Chemical Biology. 2016 12:876-884. doi:
PMID: 27571479

Structural Basis of Intracellular TGF-β Signaling: Receptors and Smads.
Chaikuad, A; Bullock, AN;
Cold Spring Harbor perspectives in biology. 2016 :-. doi:
PMID: 27549117

Structure-Based Design of Tetrahydroisoquinoline-7-carboxamides as Selective Discoidin Domain Receptor 1 (DDR1) Inhibitors.
Wang, Z; Bian, H; Bartual, SG; Du, W; Luo, J; Zhao, H; Zhang, S; Mo, C; Zhou, Y; Xu, Y; Tu, Z; Ren, X; Lu, X; Brekken, RA; Yao, L; Bullock, AN; Su, J; Ding, K;
Journal of Medicinal Chemistry. 2016 59:5911-5916. doi:
PMID: 27219676

CIS is a potent checkpoint in NK cell-mediated tumor immunity.
Delconte, RB; Kolesnik, TB; Dagley, LF; Rautela, J; Shi, W; Putz, EM; Stannard, K; Zhang, JG; Teh, C; Firth, M; Ushiki, T; Andoniou, CE; Degli-Esposti, MA; Sharp, PP; Sanvitale, CE; Infusini, G; Liau, NP; Linossi, EM; Burns, CJ; Carotta, S; Gray, DH; Seillet, C; Hutchinson, DS; Belz, GT; Webb, AI; Alexander, WS; Li, SS; Bullock, AN; Babon, JJ; Smyth, MJ; Nicholson, SE; Huntington, ND;
Nature Immunology. 2016 17:816-824. doi:
PMID: 27213690

Mutations in Known Monogenic High Bone Mass Loci Only Explain a Small Proportion of High Bone Mass Cases.
Gregson, CL; Wheeler, L; Hardcastle, SA; Appleton, LH; Addison, KA; Brugmans, M; Clark, GR; Ward, KA; Paggiosi, M; Stone, M; Thomas, J; Agarwal, R; Poole, KE; McCloskey, E; Fraser, WD; Williams, E; Bullock, AN; Davey Smith, G; Brown, MA; Tobias, JH; Duncan, EL;
Journal of Bone and Mineral Research. 2016 31:640-649. doi:
PMID: 26348019

2015

Structures of the CDK12/CycK complex with AMP-PNP reveal a flexible C-terminal kinase extension important for ATP binding.
Dixon-Clarke, SE; Elkins, JM; Cheng, SW; Morin, GB; Bullock, AN;
Scientific Reports. 2015 5:17122-. doi:
PMID: 26597175

Targeting RIPK1,2,3 to combat inflammation.
Bullock, AN; Degterev, A;
Oncotarget. 2015 6:34057-34058. doi:
PMID: 26472031

Inflammatory Signaling by NOD-RIPK2 Is Inhibited by Clinically Relevant Type II Kinase Inhibitors.
Canning, P; Ruan, Q; Schwerd, T; Hrdinka, M; Maki, JL; Saleh, D; Suebsuwong, C; Ray, S; Brennan, PE; Cuny, GD; Uhlig, HH; Gyrd-Hansen, M; Degterev, A; Bullock, AN;
Chemistry and Biology. 2015 22:1174-1184. doi:
PMID: 26320862

Structural basis of Keap1 interactions with Nrf2.
Canning, P; Sorrell, FJ; Bullock, AN;
Free Radical Biology and Medicine. 2015 88:101-107. doi:
PMID: 26057936

Clinical Utility Gene Card for: Fibrodysplasia ossificans progressiva.
Bravenboer, N; Micha, D; Triffit, JT; Bullock, AN; Ravazollo, R; Bocciardi, R; di Rocco, M; Netelenbos, JC; Ten Dijke, P; Sánchez-Duffhues, G; Kaplan, FS; Shore, EM; Pignolo, RJ; Seemann, P; Ventura, F; Beaujat, G; Eekhoff, EM; Pals, G;
European Journal of Human Genetics. 2015 23:-. doi:
PMID: 25604857

A small molecule targeting ALK1 prevents Notch cooperativity and inhibits functional angiogenesis.
Kerr, G; Sheldon, H; Chaikuad, A; Alfano, I; von Delft, F; Bullock, AN; Harris, AL;
Angiogenesis. 2015 18:209-217. doi:
PMID: 25557927

Synthesis of Highly Water-Soluble Adamantyl Phosphoinositide Derivatives
Gregory, M; Yin, M-X; McConville, MJ; Williams, E; Bullock, AN; Conway, SJ; Burgess, AW; Catimel, B; Holmes, AB;
Australian Journal of Chemistry: an international journal for chemical science. 2015 68:543-548. doi: 10.1071/CH14543
PMID:

Small molecules dorsomorphin and LDN-193189 inhibit myostatin/GDF8 signaling and promote functional myoblast differentiation.
Horbelt, D; Boergermann, JH; Chaikuad, A; Alfano, I; Williams, E; Lukonin, I; Timmel, T; Bullock, AN; Knaus, P;
Journal of Biological Chemistry. 2015 290:3390-3404. doi:
PMID: 25368322

2014

ACVR1 mutations in DIPG: lessons learned from FOP.
Taylor, KR; Vinci, M; Bullock, AN; Jones, C;
Cancer Research. 2014 74:4565-4570. doi:
PMID: 25136070

Structure-activity relationship of 3,5-diaryl-2-aminopyridine ALK2 inhibitors reveals unaltered binding affinity for fibrodysplasia ossificans progressiva causing mutants.
Mohedas, AH; Wang, Y; Sanvitale, CE; Canning, P; Choi, S; Xing, X; Bullock, AN; Cuny, GD; Yu, PB;
Journal of Medicinal Chemistry. 2014 57:7900-7915. doi:
PMID: 25101911

Recurrent activating ACVR1 mutations in diffuse intrinsic pontine glioma
Taylor, KR; Mackay, A; Truffaux, N; Butterfield, YS; Morozova, O; Philippe, C; Castel, D; Grasso, CS; Vinci, M; Carvalho, D; Carcaboso, AM; de Torres, C; Cruz, O; Mora, J; Entz-Werle, N; Ingram, WJ; Monje, M; Hargrave, D; Bullock, AN; Puget, S; Yip, S; Jones, C; Grill, J;
Nature Genetics. 2014 46:457-461. doi: 10.1038/ng.2925
PMID:

Structural mechanisms determining inhibition of the collagen receptor DDR1 by selective and multi-targeted type II kinase inhibitors.
Canning, P; Tan, L; Chu, K; Lee, SW; Gray, NS; Bullock, AN;
Journal of Molecular Biology. 2014 426:2457-2470. doi:
PMID: 24768818

Structural and biochemical characterization of the KLHL3-WNK kinase interaction important in blood pressure regulation.
Schumacher, FR; Sorrell, FJ; Alessi, DR; Bullock, AN; Kurz, T;
Biochemical Journal. 2014 460:237-246. doi:
PMID: 24641320

Correction to Discovery of a Potent and Selective DDR1 Receptor Tyrosine Kinase Inhibitor.
Kim, HG; Tan, L; Weisberg, EL; Liu, F; Canning, P; Choi, HG; Ezell, S; Zhao, Z; Wu, H; Wang, J; Mandinova, A; Bullock, AN; Liu, Q; Lee, SW; Gray, NS;
ACS Chemical Biology. 2014 9:840-. doi: 10.1021/cb5000949
PMID: 24527812

New strategies to inhibit KEAP1 and the Cul3-based E3 ubiquitin ligases.
Canning, P; Bullock, AN;
Biochemical Society Transactions. 2014 42:103-107. doi: 10.1042/BST20130215
PMID: 24450635

Recurrent activating ACVR1 mutations in diffuse intrinsic pontine glioma.
Taylor, KR; Mackay, A; Truffaux, N; Butterfield, YS; Morozova, O; Philippe, C; Castel, D; Grasso, CS; Vinci, M; Carvalho, D; Carcaboso, AM; de Torres, C; Cruz, O; Mora, J; Entz-Werle, N; Ingram, WJ; Monje, M; Hargrave, D; Bullock, AN; Puget, S; Yip, S; Jones, C; Grill, J;
Nature Genetics. 2014 46:457-461. doi:
PMID: 24705252

2013

Discovery of a potent and selective DDR1 receptor tyrosine kinase inhibitor.
Kim, HG; Tan, L; Weisberg, EL; Liu, F; Canning, P; Choi, HG; Ezell, SA; Wu, H; Zhao, Z; Wang, J; Mandinova, A; Griffin, JD; Bullock, AN; Liu, Q; Lee, SW; Gray, NS;
ACS Chemical Biology. 2013 8:2145-2150. doi: 10.1021/cb400430t
PMID: 23899692

Molecular architecture of the ankyrin SOCS box family of Cul5-dependent E3 ubiquitin ligases.
Muniz, JR; Guo, K; Kershaw, NJ; Ayinampudi, V; von Delft, F; Babon, JJ; Bullock, AN;
Journal of Molecular Biology. 2013 425:3166-3177. doi: 10.1016/j.jmb.2013.06.015
PMID: 23806657

Constitutively active ALK2 receptor mutants require type II receptor cooperation.
Bagarova, J; Vonner, AJ; Armstrong, KA; Börgermann, J; Lai, CS; Deng, DY; Beppu, H; Alfano, I; Filippakopoulos, P; Morrell, NW; Bullock, AN; Knaus, P; Mishina, Y; Yu, PB;
Molecular and Cellular Biology. 2013 33:2413-2424. doi: 10.1128/MCB.01595-12
PMID: 23572558

Development of an ALK2-biased BMP type I receptor kinase inhibitor.
Mohedas, AH; Xing, X; Armstrong, KA; Bullock, AN; Cuny, GD; Yu, PB;
ACS Chemical Biology. 2013 8:1291-1302. doi: 10.1021/cb300655w
PMID: 23547776

Structural basis for Cul3 protein assembly with the BTB-Kelch family of E3 ubiquitin ligases.
Canning, P; Cooper, CD; Krojer, T; Murray, JW; Pike, AC; Chaikuad, A; Keates, T; Thangaratnarajah, C; Hojzan, V; Ayinampudi, V; Marsden, BD; Gileadi, O; Knapp, S; von Delft, F; Bullock, AN;
Journal of Biological Chemistry. 2013 288:7803-7814. doi: 10.1074/jbc.M112.437996
PMID: 23349464

A new class of small molecule inhibitor of BMP signaling.
Sanvitale, CE; Kerr, G; Chaikuad, A; Ramel, MC; Mohedas, AH; Reichert, S; Wang, Y; Triffitt, JT; Cuny, GD; Yu, PB; Hill, CS; Bullock, AN;
PLoS One. 2013 8:e62721-. doi: 10.1371/journal.pone.0062721
PMID: 23646137

The structural basis of ZMPSTE24-dependent laminopathies
Quigley, A; Dong, YY; Pike, ACW; Dong, L; Shrestha, L; Berridge, G; Stansfeld, PJ; Sansom, MSP; Edwards, AM; Bountra, C; Von Delft, F; Bullock, AN; Burgess-Brown, NA; Carpenter, EP;
Science. 2013 340:1604-1607. doi: 10.1126/science.1231513
PMID:

Suppressor of Cytokine Signaling (SOCS) 5 utilises distinct domains for regulation of JAK1 and interaction with the adaptor protein Shc-1.
Linossi, EM; Chandrashekaran, IR; Kolesnik, TB; Murphy, JM; Webb, AI; Willson, TA; Kedzierski, L; Bullock, AN; Babon, JJ; Norton, RS; Nicola, NA; Nicholson, SE;
PLoS One. 2013 8:e70536-. doi: 10.1371/journal.pone.0070536
PMID: 23990909

2012

Structure of the bone morphogenetic protein receptor ALK2 and implications for fibrodysplasia ossificans progressiva.
Chaikuad, A; Alfano, I; Kerr, G; Sanvitale, CE; Boergermann, JH; Triffitt, JT; von Delft, F; Knapp, S; Knaus, P; Bullock, AN;
Journal of Biological Chemistry. 2012 287:36990-36998. doi: 10.1074/jbc.M112.365932
PMID: 22977237

Structural basis for ASPP2 recognition by the tumor suppressor p73.
Canning, P; von Delft, F; Bullock, AN;
Journal of Molecular Biology. 2012 423:515-527. doi: 10.1016/j.jmb.2012.08.005
PMID: 22917970

The p53 cofactor Strap exhibits an unexpected TPR motif and oligonucleotide-binding (OB)-fold structure.
Adams, CJ; Pike, AC; Maniam, S; Sharpe, TD; Coutts, AS; Knapp, S; La Thangue, NB; Bullock, AN;
Proceedings of the National Academy of Sciences of USA. 2012 109:3778-3783. doi: 10.1073/pnas.1113731109
PMID: 22362889

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

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

A novel ACVR1 mutation in the glycine/serine-rich domain found in the most benign case of a fibrodysplasia ossificans progressiva variant reported to date.
Gregson, CL; Hollingworth, P; Williams, M; Petrie, KA; Bullock, AN; Brown, MA; Tobias, JH; Triffitt, JT;
Bone. 2011 48:654-658. doi: 10.1016/j.bone.2010.10.164
PMID: 21044902

Structural basis for c-KIT inhibition by the suppressor of cytokine signaling 6 (SOCS6) ubiquitin ligase.
Zadjali, F; Pike, AC; Vesterlund, M; Sun, J; Wu, C; Li, SS; Rönnstrand, L; Knapp, S; Bullock, AN; Flores-Morales, A;
Journal of Biological Chemistry. 2011 286:480-490. doi: 10.1074/jbc.M110.173526
PMID: 21030588

2010

Structural basis for Par-4 recognition by the SPRY domain- and SOCS box-containing proteins SPSB1, SPSB2, and SPSB4.
Filippakopoulos, P; Low, A; Sharpe, TD; Uppenberg, J; Yao, S; Kuang, Z; Savitsky, P; Lewis, RS; Nicholson, SE; Norton, RS; Bullock, AN;
Journal of Molecular Biology. 2010 401:389-402. doi: 10.1016/j.jmb.2010.06.017
PMID: 20561531

New potent dual inhibitors of CK2 and Pim kinases: discovery and structural insights.
López-Ramos, M; Prudent, R; Moucadel, V; Sautel, CF; Barette, C; Lafanechère, L; Mouawad, L; Grierson, D; Schmidt, F; Florent, JC; Filippakopoulos, P; Bullock, AN; Knapp, S; Reiser, JB; Cochet, C;
The FASEB Journal. 2010 24:3171-3185. doi: 10.1096/fj.09-143743
PMID: 20400536

2009

Conformational stability and activity of p73 require a second helix in the tetramerization domain.
Coutandin, D; Löhr, F; Niesen, FH; Ikeya, T; Weber, TA; Schäfer, B; Zielonka, EM; Bullock, AN; Yang, A; Güntert, P; Knapp, S; McKeon, F; Ou, HD; Dötsch, V;
Cell Death and Differentiation. 2009 16:1582-1589. doi: 10.1038/cdd.2009.139
PMID: 19763140

Synthesis, kinase inhibitory potencies, and in vitro antiproliferative evaluation of new Pim kinase inhibitors.
Akué-Gédu, R; Rossignol, E; Azzaro, S; Knapp, S; Filippakopoulos, P; Bullock, AN; Bain, J; Cohen, P; Prudhomme, M; Anizon, F; Moreau, P;
Journal of Medicinal Chemistry. 2009 52:6369-6381. doi: 10.1021/jm901018f
PMID: 19788246

Dissection of PIM serine/threonine kinases in FLT3-ITD-induced leukemogenesis reveals PIM1 as regulator of CXCL12-CXCR4-mediated homing and migration.
Grundler, R; Brault, L; Gasser, C; Bullock, AN; Dechow, T; Woetzel, S; Pogacic, V; Villa, A; Ehret, S; Berridge, G; Spoo, A; Dierks, C; Biondi, A; Knapp, S; Duyster, J; Schwaller, J;
Journal of Experimental Medicine. 2009 206:1957-1970. doi: 10.1084/jem.20082074
PMID: 19687226

STUDYING THE ROLE OF PIM KINASES IN FLT3-ITD-INDUCED LEUKEMIA REVEALED PIM1 AS REGULATOR OF CXCL12/CXCR4-MEDIATED HOMING AND MIGRATION
Brault, L; Grundler, R; Gasser, C; Bullock, AN; Ehret, S; Spoo, A; Dierks, C; Biondi, A; Knapp, S; Duyster, J; Schwaller, J;
Haematologica: the hematology journal. 2009 94:448-449. doi:
PMID:

Kinase domain insertions define distinct roles of CLK kinases in SR protein phosphorylation.
Bullock, AN; Das, S; Debreczeni, JE; Rellos, P; Fedorov, O; Niesen, FH; Guo, K; Papagrigoriou, E; Amos, AL; Cho, S; Turk, BE; Ghosh, G; Knapp, S;
Structure. 2009 17:352-362. doi:
PMID: 19278650

Crystal structure of the PIM2 kinase in complex with an organoruthenium inhibitor.
Bullock, AN; Russo, S; Amos, A; Pagano, N; Bregman, H; Debreczeni, JE; Lee, WH; von Delft, F; Meggers, E; Knapp, S;
PLoS One. 2009 4:e7112-. doi: 10.1371/journal.pone.0007112
PMID: 19841674

Novel mutations in ACVR1 result in atypical features in two fibrodysplasia ossificans progressiva patients.
Petrie, KA; Lee, WH; Bullock, AN; Pointon, JJ; Smith, R; Russell, RG; Brown, MA; Wordsworth, BP; Triffitt, JT;
PLoS One. 2009 4:e5005-. doi: 10.1371/journal.pone.0005005
PMID: 19330033

2008

The structure of P-TEFb (CDK9/cyclin T1), its complex with flavopiridol and regulation by phosphorylation.
Baumli, S; Lolli, G; Lowe, ED; Troiani, S; Rusconi, L; Bullock, AN; Debreczeni, JE; Knapp, S; Johnson, LN;
The EMBO Journal. 2008 27:1907-1918. doi: 10.1038/emboj.2008.121
PMID: 18566585

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;
Proceedings of the National Academy of Sciences of USA. 2007 104:20523-20528. doi:
PMID: 18077363

Structural analysis identifies imidazo[1,2-b]pyridazines as PIM kinase inhibitors with in vitro antileukemic activity.
Pogacic, V; Bullock, AN; Fedorov, O; Filippakopoulos, P; Gasser, C; Biondi, A; Meyer-Monard, S; Knapp, S; Schwaller, J;
Cancer Research. 2007 67:6916-6924. doi:
PMID: 17638903

Interaction of hydroxylated collagen IV with the von-Hippel-Lindau tumor suppressor.
Masson, N; Grosfeld A, ; Kessler B, ; Ratcliffe PJ, ;
Journal of Biological Chemistry. 2007 282:13264-13269. doi: 10.1074/jbc.M611648200
PMID: 17339318

2006

Ruthenium half-sandwich complexes bound to protein kinase Pim-1.
Debreczeni, JE; Bullock, AN; Atilla, GE; Williams, DS; Bregman, H; Knapp, S; Meggers, E;
Angewandte Chemie International Edition. 2006 45:1580-1585. doi: 10.1002/anie.200503468
PMID: 16381041

2005

Structure and substrate specificity of the Pim-1 kinase.
Bullock, AN; Debreczeni, J; Amos, AL; Knapp, S; Turk, BE;
Journal of Biological Chemistry. 2005 280:41675-41682. doi: 10.1074/jbc.M510711200
PMID: 16227208

Structural basis of inhibitor specificity of the human protooncogene proviral insertion site in moloney murine leukemia virus (PIM-1) kinase.
Bullock, AN; Debreczeni, JE; Fedorov, OY; Nelson, A; Marsden, BD; Knapp, S;
Journal of Medicinal Chemistry. 2005 48:7604-7614. doi:
PMID: 16302800

2004

Computational redesign of protein-protein interaction specificity
Kortemme, T; Joachimiak, LA; Bullock, AN; Schuler, AD; Stoddard, BL; Baker, D;
Nature Structural and Molecular Biology. 2004 11:371-379. doi: 10.1038/nsmb749
PMID: 15034550

2002

Hypoxia-inducible factor (HIF) asparagine hydroxylase is identical to factor inhibiting HIF (FIH) and is related to the cupin structural family.
Hewitson, KS; McNeill, LA; Riordan, MV; Tian, YM; Bullock, AN; Welford, RW; Elkins, JM; Oldham, NJ; Bhattacharya, S; Gleadle, JM; Ratcliffe, PJ; Pugh, CW; Schofield, CJ;
Journal of Biological Chemistry. 2002 277:26351-26355. doi: 10.1074/jbc.C200273200
PMID: 12042299

2001

Rescuing the function of mutant p53.
Bullock, AN; Fersht, AR;
Nature Reviews: Cancer. 2001 1:68-76. doi: 10.1038/35094077
PMID: 11900253

2000

1997

Thermodynamic stability of wild-type and mutant p53 core domain.
Bullock, AN; Henckel, J; DeDecker, BS; Johnson, CM; Nikolova, PV; Proctor, MR; Lane, DP; Fersht, AR;
Proceedings of the National Academy of Sciences of USA. 1997 94:14338-14342. doi:
PMID: 9405613

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