A. Bullock

M. Brown, E. McCloskey, G. Davey Smith, 2015, Journal of bone and mineral research : the official journal of the American Society for Bone and Mineral Research.

Crystal Structure of the PIM2 Kinase in Complex with an Organoruthenium Inhibitor

S. Knapp, F. von Delft, J. Debreczeni, 2009, PloS one.

Development of a Selective Dual Discoidin Domain Receptor (DDR)/p38 Kinase Chemical Probe.

S. Knapp, S. Müller, A. Bullock, 2021, Journal of medicinal chemistry.

Suppressor of Cytokine Signaling (SOCS) 5 Utilises Distinct Domains for Regulation of JAK1 and Interaction with the Adaptor Protein Shc-1

R. Norton, A. Bullock, L. Kedzierski, 2013, PloS one.

Protocol paper: a multi-center, double-blinded, randomized, 6-month, placebo-controlled study followed by 12-month open label extension to evaluate the safety and efficacy of Saracatinib in Fibrodysplasia Ossificans Progressiva (STOPFOP)

N. V. van Schoor, A. Bullock, Annette von Delft, 2022, BMC Musculoskeletal Disorders.

Small molecule inhibitors reveal an indispensable scaffolding role of RIPK2 in NOD2 signaling

Jennifer A. Ward, A. Degterev, A. Bullock, 2018, The EMBO journal.

Development of Macrocycle Kinase Inhibitors for ALK2 Using Fibrodysplasia Ossificans Progressiva‐Derived Endothelial Cells

M. Goumans, A. Bullock, P. Koolwijk, 2019, JBMR plus.

Crystal structure of human CUL3 N-terminal domain bound to KEAP1 BTB and 3-box

C. Bountra, C. Arrowsmith, A. Bullock, 2017 .

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.

M. Brown, A. Bullock, C. Gregson, 2011, Bone.

Small molecule inhibitors reveal an indispensable scaffolding role of RIPK 2 in NOD 2 signaling

Jennifer A. Ward, A. Degterev, A. Bullock, 2018 .

Constitutively Active ALK2 Receptor Mutants Require Type II Receptor Cooperation

Y. Mishina, A. Bullock, H. Beppu, 2013, Molecular and Cellular Biology.

Targeted protein degradation: expanding the toolbox

Matthieu Schapira, Matthew F. Calabrese, Alex N. Bullock, 2019, Nature Reviews Drug Discovery.

Structural Basis for Par-4 Recognition by the SPRY Domain- and SOCS Box-Containing Proteins SPSB1, SPSB2, and SPSB4

T. Sharpe, R. Norton, A. Bullock, 2010, Journal of molecular biology.

Structure of the kinase domain of human RIPK2 in complex with ponatinib

C. Bountra, C. Arrowsmith, A. Bullock, 2013 .

Specific CLK Inhibitors from a Novel Chemotype for Regulation of Alternative Splicing

Damian Szklarczyk, Doriano Fabbro, Stefan Knapp, 2011, Chemistry & biology.

Ubiquitin ligases: guardians of mammalian development

Kenneth M. Yamada, A. Bullock, Zhuoyao Chen, 2022, Nature Reviews Molecular Cell Biology.

7,8-Dichloro-1-oxo-β-carbolines as a Versatile Scaffold for the Development of Potent and Selective Kinase Inhibitors with Unusual Binding Modes

Doriano Fabbro, Stefan Knapp, Jörg Trappe, 2011, Journal of medicinal chemistry.

Synthesis, kinase inhibitory potencies, and in vitro antiproliferative evaluation of new Pim kinase inhibitors.

Stefan Knapp, Panagis Filippakopoulos, Jenny Bain, 2009, Journal of medicinal chemistry.

CIS is a potent checkpoint in NK cell–mediated tumor immunity

Laura F. Dagley, S. Li, W. Shi, 2016, Nature Immunology.

Development of an ALK2-biased BMP type I receptor kinase inhibitor.

A. Bullock, G. Cuny, Agustin H. Mohedas, 2013, ACS chemical biology.

The structure of P‐TEFb (CDK9/cyclin T1), its complex with flavopiridol and regulation by phosphorylation

L. Johnson, S. Knapp, J. Debreczeni, 2008, The EMBO journal.

ACVR1 mutations in DIPG: lessons learned from FOP.

Chris Jones, Maria Vinci, Chris Jones, 2014, Cancer research.

MEDB-62. Disease-associated KBTBD4 mutations in medulloblastoma elicit neomorphic ubiquitylation activity to promote CoREST degradation

A. Bullock, I. Vendrell, L. Busino, 2022, Cell Death & Differentiation.

Mutant ACVR1 Arrests Glial Cell Differentiation to Drive Tumorigenesis in Pediatric Gliomas

T. Mak, C. Hawkins, A. Bullock, 2020, Cancer cell.

Fostering open collaboration in drug development for paediatric brain tumours

A. Bullock, E. Williams, J. Wong, 2019, Biochemical Society transactions.

ALK2 inhibitors display beneficial effects in preclinical models of ACVR1 mutant diffuse intrinsic pontine glioma

M. Monje, J. Mora, Chris Jones, 2019, Communications Biology.

Structure–Activity Relationship of 3,5-Diaryl-2-aminopyridine ALK2 Inhibitors Reveals Unaltered Binding Affinity for Fibrodysplasia Ossificans Progressiva Causing Mutants

A. Bullock, G. Cuny, Agustin H. Mohedas, 2014, Journal of medicinal chemistry.

A New Class of Small Molecule Inhibitor of BMP Signaling

A. Bullock, C. Hill, A. Chaikuad, 2013, PloS one.

ALK2 inhibitors display beneficial effects in preclinical models of ACVR1 mutant diffuse intrinsic pontine glioma

M. Monje, J. Mora, Chris Jones, 2019, Communications Biology.

A small molecule targeting ALK1 prevents Notch cooperativity and inhibits functional angiogenesis

A. Harris, F. von Delft, A. Bullock, 2015, Angiogenesis.

A Potent and Selective CDKL5/GSK3 Chemical Probe is Neuroprotective

H. Wichterle, D. Drewry, C. Wells, 2023, bioRxiv.

Structure and inhibitor specificity of the PCTAIRE-family kinase CDK16

T. Sharpe, A. Bullock, K. Sakamoto, 2017, The Biochemical journal.

Challenges and Opportunities for Drug Repositioning in Fibrodysplasia Ossificans Progressiva

M. Goumans, A. Bullock, F. Ventura, 2021, Biomedicines.

Saracatinib is an efficacious clinical candidate for fibrodysplasia ossificans progressiva

Wei Zheng, E. Place, A. Bullock, 2020, bioRxiv.

Structural basis for the potent and selective binding of LDN-212854 to the BMP receptor kinase ALK2

A. Bullock, E. Williams, 2017, Bone.

Structural Basis of Intracellular TGF-β Signaling: Receptors and Smads.

A. Bullock, A. Chaikuad, 2016, Cold Spring Harbor perspectives in biology.

Structural complexity in the KCTD family of Cullin3-dependent E3 ubiquitin ligases

A. Bullock, R. Chalk, D. Pinkas, 2017, The Biochemical journal.

New strategies to inhibit KEAP1 and the Cul3-based E3 ubiquitin ligases

A. Bullock, P. Canning, 2014, Biochemical Society transactions.

Molecular Architecture of the Ankyrin SOCS Box Family of Cul5-Dependent E3 Ubiquitin Ligases

F. von Delft, A. Bullock, K. Guo, 2013, Journal of molecular biology.

Discovery of a Potent and Selective DDR1 Receptor Tyrosine Kinase Inhibitor

Sam W. Lee, N. Gray, Qingsong Liu, 2013, ACS chemical biology.

Discovery of a Potent and Selective DDR 1 Receptor Tyrosine Kinase Inhibitor

Sam W. Lee, N. Gray, Qingsong Liu, 2013 .

Crystal Structure of the KELCH domain of human KEAP1

C. Bountra, F. von Delft, C. Arrowsmith, 2019 .

Lessons from LIMK1 enzymology and their impact on inhibitor design

S. Knapp, E. Salah, A. Bullock, 2019, The Biochemical journal.

Structure and Substrate Specificity of the Pim-1 Kinase*

S. Knapp, B. Turk, J. Debreczeni, 2005, Journal of Biological Chemistry.

New potent dual inhibitors of CK2 and Pim kinases: discovery and structural insights

S. Knapp, L. Mouawad, A. Bullock, 2010, FASEB journal : official publication of the Federation of American Societies for Experimental Biology.

2-Amino-2,3-dihydro-1H-indene-5-carboxamide-Based Discoidin Domain Receptor 1 (DDR1) Inhibitors: Design, Synthesis, and in Vivo Antipancreatic Cancer Efficacy

A. Bullock, R. Brekken, Xiaoyun Lu, 2019, Journal of medicinal chemistry.

The SGC beyond structural genomics: redefining the role of 3D structures by coupling genomic stratification with fragment-based discovery

Brian D. Marsden, Wen Hwa Lee, Frank von Delft, 2017, Essays in biochemistry.

Structural Mechanisms Determining Inhibition of the Collagen Receptor DDR1 by Selective and Multi-Targeted Type II Kinase Inhibitors

Kiki Chu, Peter Canning, Nathanael S. Gray, 2014, Journal of molecular biology.

Structure-Based Design of Tetrahydroisoquinoline-7-carboxamides as Selective Discoidin Domain Receptor 1 (DDR1) Inhibitors

Yong Xu, A. Bullock, L. Yao, 2016, Journal of medicinal chemistry.

Structural Basis for c-KIT Inhibition by the Suppressor of Cytokine Signaling 6 (SOCS6) Ubiquitin Ligase*

S. Knapp, S. Li, A. Bullock, 2010, The Journal of Biological Chemistry.

University of Dundee Structural and biochemical characterization of the KLHL 3-WNK kinase interaction important in blood pressure regulation

D. Alessi, A. Bullock, Frances-Rose Schumacher, 2014 .

The Structural Basis of ZMPSTE24-Dependent Laminopathies

C. Bountra, C. Bountra, F. von Delft, 2013, Science.

Structural analysis identifies imidazo[1,2-b]pyridazines as PIM kinase inhibitors with in vitro antileukemic activity.

S. Knapp, O. Fedorov, A. Bullock, 2007, Cancer research.

Inflammatory Signaling by NOD-RIPK2 Is Inhibited by Clinically Relevant Type II Kinase Inhibitors

A. Degterev, A. Bullock, S. Ray, 2015, Chemistry & biology.

DFG-1 residue controls inhibitor binding mode and affinity providing a basis for rational design of kinase inhibitor selectivity.

S. Knapp, O. Fedorov, A. Bullock, 2020, Journal of medicinal chemistry.

Human Kelch-like protein 20 (KLHL20) A Target Enabling Package (TEP)

O. Fedorov, A. Bullock, P. Brennan, 2020 .

Structural Basis for Recruitment of DAPK1 to the KLHL20 E3 Ligase

A. Bullock, P. Filippakopoulos, S. Picaud, 2018, bioRxiv.

Receptor-interacting protein kinase 2 (RIPK2) and nucleotide-binding oligomerization domain (NOD) cell signaling inhibitors based on a 3,5-diphenyl-2-aminopyridine scaffold.

A. Degterev, A. Bullock, L. Schlicher, 2020, European journal of medicinal chemistry.

Structural Basis for ASPP2 Recognition by the Tumor Suppressor p73

F. von Delft, A. Bullock, P. Canning, 2012, Journal of molecular biology.

Selection and structural characterization of anti-TREM2 scFvs that reduce levels of shed ectodomain

S. Gräslund, A. Bullock, S. Mukhopadhyay, 2021, Structure.

Selection and structural characterisation of anti-TREM2 scFvs that reduce levels of shed ectodomain

S. Gräslund, A. Bullock, S. Mukhopadhyay, 2021, bioRxiv.

Structural basis for Cul3 protein assembly with the BTB-Kelch family of E3 ubiquitin ligases.

S. Knapp, F. von Delft, O. Gileadi, 2013, The Journal of Biological Chemistry.

Crystal structure of the SOCS2–elongin C–elongin B complex defines a prototypical SOCS box ubiquitin ligase

Stefan Knapp, Aled M. Edwards, S. Knapp, 2006, Proceedings of the National Academy of Sciences of the United States of America.

Clinical Utility Gene Card for: Fibrodysplasia ossificans progressiva

G. Pals, A. Bullock, F. Ventura, 2015, European Journal of Human Genetics.

Small Molecules Dorsomorphin and LDN-193189 Inhibit Myostatin/GDF8 Signaling and Promote Functional Myoblast Differentiation*

A. Bullock, D. Horbelt, P. Knaus, 2014, The Journal of Biological Chemistry.

Dissection of PIM serine/threonine kinases in FLT3-ITD–induced leukemogenesis reveals PIM1 as regulator of CXCL12–CXCR4-mediated homing and migration

Stefan Knapp, Andrea Biondi, Antonello Villa, 2009, The Journal of experimental medicine.

Structure of the SOCS4-ElonginB/C Complex Reveals a Distinct SOCS Box Interface and the Molecular Basis for SOCS-Dependent EGFR Degradation

Stefan Knapp, Zhou Songyang, S. Knapp, 2007, Structure.

Human AGR2 Deficiency Causes Mucus Barrier Dysfunction and Infantile Inflammatory Bowel Disease

A. Bullock, H. Uhlig, A. Al-Shaibi, 2021, Cellular and molecular gastroenterology and hepatology.

The p53 cofactor Strap exhibits an unexpected TPR motif and oligonucleotide-binding (OB)–fold structure

S. Knapp, T. Sharpe, A. Bullock, 2012, Proceedings of the National Academy of Sciences.

Ruthenium half-sandwich complexes bound to protein kinase Pim-1.

S. Knapp, J. Debreczeni, A. Bullock, 2006, Angewandte Chemie.

Janus kinase inhibition for autoinflammation in DNASE2 deficiency.

N. Sebire, A. Bullock, H. Uhlig, 2019, The Journal of allergy and clinical immunology.

Novel Quinazolinone Inhibitors of ALK2 Flip between Alternate Binding Modes: Structure–Activity Relationship, Structural Characterization, Kinase Profiling, and Cellular Proof of Concept

A. Bullock, S. Hoelder, S. Vázquez, 2018, Journal of medicinal chemistry.

Structural and biochemical characterization establishes a detailed understanding of KEAP1-CUL3 complex assembly

A. Bullock, R. Adamson, N. C. Payne, 2023, bioRxiv.

Structures of ABCB10, a human ATP-binding cassette transporter in apo- and nucleotide-bound states

A. Barr, C. Bountra, F. von Delft, 2013, Proceedings of the National Academy of Sciences.

Discovery and characterization of a specific inhibitor of serine-threonine kinase cyclin-dependent kinase-like 5 (CDKL5) demonstrates role in hippocampal CA1 physiology

D. Drewry, C. Wells, A. Axtman, 2023, eLife.

Target 2035 – update on the quest for a probe for every protein

G. A. Bezerra, T. Willson, G. Superti-Furga, 2021, RSC medicinal chemistry.

Structural consequences of BMPR2 kinase domain mutations causing pulmonary arterial hypertension

F. von Delft, A. Bullock, A. Chaikuad, 2019, Scientific Reports.

Activation loop targeting strategy for design of receptor-interacting protein kinase 2 (RIPK2) inhibitors

A. Degterev, A. Bullock, S. Ray, 2018, Bioorganic & medicinal chemistry letters.

Design, Synthesis, and Biological Evaluation of 3-(Imidazo[1,2-a]pyrazin-3-ylethynyl)-4-isopropyl-N-(3-((4-methylpiperazin-1-yl)methyl)-5-(trifluoromethyl)phenyl)benzamide as a Dual Inhibitor of Discoidin Domain Receptors 1 and 2

A. Bullock, R. Brekken, Tingting Xu, 2018, Journal of medicinal chemistry.

Tetrahydroisoquinoline-7-carboxamide Derivatives as New Selective Discoidin Domain Receptor 1 (DDR1) Inhibitors.

A. Bullock, R. Brekken, Xiaoyun Lu, 2017, ACS medicinal chemistry letters.

Identification of a PGXPP degron motif in dishevelled and structural basis for its binding to the E3 ligase KLHL12

A. Bullock, M. Vedadi, P. Filippakopoulos, 2020, bioRxiv.

Structures of the CDK12/CycK complex with AMP-PNP reveal a flexible C-terminal kinase extension important for ATP binding

G. Morin, J. Elkins, A. Bullock, 2015, Scientific Reports.

Target 2035 – an update on private sector contributions

T. Willson, S. Knapp, U. Lessel, 2023, RSC medicinal chemistry.

Human Receptor-Interacting Serine / Threonine-Protein Kinase 2 ( RIPK 2 ) A Target Enabling Package ( TEP )

Jennifer A. Ward, S. Knapp, A. Degterev, 2020 .

Discovery of a Potent and Selective CDKL5/GSK3 Chemical Probe That Is Neuroprotective

H. Wichterle, D. Drewry, C. Wells, 2023, ACS chemical neuroscience.

CRYSTAL STRUCTURE OF THE HUMAN PIM1 IN COMPLEX WITH A RUTHENIUM ORGANOMETALLIC LIGAND RU1

S. Knapp, C. Arrowsmith, J. Weigelt, 2005 .

Structural and biochemical characterization of the KLHL3–WNK kinase interaction important in blood pressure regulation

D. Alessi, A. Bullock, Frances-Rose Schumacher, 2014, The Biochemical journal.

Crystal Structure-Guided Design of Bisubstrate Inhibitors and Photoluminescent Probes for Protein Kinases of the PIM Family

S. Knapp, A. Bullock, A. Chaikuad, 2021, Molecules.

1 The FAM 83 family of proteins are anchors for Casein Kinase 1 isoforms through 1 the DUF 1669 domain 2 3

A. Bullock, D. Campbell, R. Gourlay, 2017 .

Discovery and characterization of a specific inhibitor of serine-threonine kinase cyclin dependent kinase-like 5 (CDKL5) demonstrates role in hippocampal CA1 physiology

D. Drewry, C. Wells, A. Axtman, 2023, bioRxiv.

ALK2 inhibitors display beneficial effects in preclinical models of ACVR1 mutant diffuse intrinsic pontine glioma

M. Monje, J. Mora, Chris Jones, 2019, Communications Biology.

Human LIM Domain Kinase 1 (LIMK1), Kinase Domain A Target Enabling Package (TEP)

S. Knapp, E. Salah, A. Hata, 2020 .

Structural basis for Cul3 protein assembly with the BTB-Kelch family of E3 ubiquitin ligases.

S. Knapp, F. von Delft, O. Gileadi, 2013, The Journal of Biological Chemistry.

Sequence and structural variations determining the recruitment of WNK kinases to the KLHL3 E3 ligase

D. Alessi, A. Bullock, R. Fischer, 2020, bioRxiv.

New potent dual inhibitors of CK2 and Pim kinases: discovery and structural insights

S. Knapp, L. Mouawad, A. Bullock, 2010, FASEB journal : official publication of the Federation of American Societies for Experimental Biology.

Covalent targeting of remote cysteine residues to develop CDK12 and 13 inhibitors

Richard A. Young, N. Hannett, N. Gray, 2016 .

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.

M. Brown, A. Bullock, C. Gregson, 2011, Bone.

Target highlights in CASP13: experimental target structures through the eyes of their authors. Proteins: Structure,

Gutsche, K. Fidelis, G. Phillips, 2019 .

ALK2 Receptor Kinase Association with FKBP12.6 Is Structurally Conserved with the ALK2-FKBP12 Complex

A. Bullock, G. Kerr, E. Williams, 2021, Biomedicines.

PRMT5 inhibition shows in vitro efficacy against H3K27M-altered diffuse midline glioma, but does not extend survival in vivo

A. Cribbs, A. Bullock, A. Carcaboso, 2024, Scientific reports.