Publications

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2019

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

Carvalho D, Taylor KR, Olaciregui NG, Molinari V, Clarke M, Mackay A, Ruddle R, Henley A, Valenti M, Hayes A, Brandon AH, Eccles SA, Raynaud F, Boudhar A, Monje M, Popov S, Moore AS, Mora J, Cruz O, Vinci M, Brennan PE, Bullock AN, Carcaboso AM, Jones C

Commun Biol. 2(1):156. doi: 10.1038/s42003-019-0420-8

Publication date: May 9, 2019

PMID: 31925004

Rapid covalent-probe discovery by electrophile-fragment screening.

Resnick E, Bradley A, Gan J, Douangamath A, Krojer T, Sethi R, Geurink PP, Aimon A, Amitai G, Bellini D, Bennett J, Fairhead M, Fedorov O, Gabizon R, Gan J, Guo J, Plotnikov A, Reznik N, Ruda GF, Díaz-Sáez L, Straub VM, Szommer T, Velupillai S, Zaidman D, Zhang Y, Coker AR, Dowson CG, Barr H, Wang C, Huber KVM, Brennan PE, Ovaa H, von Delft F, London N

J. Am. Chem. Soc.. doi: 10.1021/jacs.9b02822

Publication date: May 7, 2019

PMID: 31060360

Structure and function of eTudor domain containing TDRD proteins.

Gan B, Chen S, Liu H, Min J, Liu K

Crit. Rev. Biochem. Mol. Biol.. 1-14. doi: 10.1080/10409238.2019.1603199

Publication date: May 3, 2019

PMID: 31046474

A Perspective on Extreme Open Science: Companies Sharing Compounds without Restriction.

Drewry DH, Wells CI, Zuercher WJ, Willson TM

SLAS Discov. 2472555219838210. doi: 10.1177/2472555219838210

Publication date: April 29, 2019

PMID: 31034310

Construction of a Shape-Diverse Fragment Set: Design, Synthesis and Screen against Aurora-A Kinase.

Zhang R, McIntyre PJ, Collins PM, Foley DJ, Arter C, von Delft F, Bayliss R, Warriner S, Nelson A

Chemistry. doi: 10.1002/chem.201900815

Publication date: April 26, 2019

PMID: 31026091

Crosstalk between RNA Pol II C-Terminal Domain Acetylation and Phosphorylation via RPRD Proteins.

Ali I, Ruiz DG, Ni Z, Johnson JR, Zhang H, Li PC, Khalid MM, Conrad RJ, Guo X, Min J, Greenblatt J, Jacobson M, Krogan NJ, Ott M

Mol. Cell. doi: 10.1016/j.molcel.2019.04.008

Publication date: April 26, 2019

PMID: 31054975

Crystal structure of human RIOK2 bound to a specific inhibitor.

Wang J, Varin T, Vieth M, Elkins JM

Open Biol. 9(4):190037. doi: 10.1098/rsob.190037

Publication date: April 26, 2019

PMID: 30991936

Discovery of selective activators of PRC2 mutant EED-I363M.

Suh JL, Barnash KD, Abramyan TM, Li F, The J, Engelberg IA, Vedadi M, Brown PJ, Kireev DB, Arrowsmith CH, James LI, Frye SV

Sci Rep. 9(1):6524. doi: 10.1038/s41598-019-43005-z

Publication date: April 25, 2019

PMID: 31024026

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. 10(1):1915. doi: 10.1038/s41467-019-09672-2

Publication date: April 23, 2019

PMID: 31015424

Design of a Cyclin G Associated Kinase (GAK)/Epidermal Growth Factor Receptor (EGFR) Inhibitor Set to Interrogate the Relationship of EGFR and GAK in Chordoma.

Asquith CRM, Naegeli KM, East MP, Laitinen T, Havener TM, Wells CI, Johnson GL, Drewry DH, Zuercher WJ, Morris DC

J. Med. Chem.. doi: 10.1021/acs.jmedchem.9b00350

Publication date: April 19, 2019

PMID: 30973735

Discovery of Pyrrolo[3,2-d]pyrimidin-4-one Derivatives as a New Class of Potent and Cell Active Inhibitors of P300/CBP-Associated Factor Bromodomain.

Huang LY, Li H, Li LL, Niu L, Seupel R, Wu C, Cheng W, Chen C, Ding B, Brennan PE, Yang S

J. Med. Chem.. doi: 10.1021/acs.jmedchem.9b00096

Publication date: April 18, 2019

PMID: 30998845

Structural analyses reveal that MBD3 is a methylated-CG binder.

Liu K, Lei M, Wu Z, Gan B, Cheng H, Li Y, Min J

FEBS J.. doi: 10.1111/febs.14850

Publication date: April 13, 2019

PMID: 30980593

Structural insights into the modulatory role of the accessory protein WYL1 in the Type VI-D CRISPR-Cas system.

Zhang H, Dong C, Li L, Wasney GA, Min J

Nucleic Acids Res.. doi: 10.1093/nar/gkz269

Publication date: April 12, 2019

PMID: 30976796

Chromokinesins NOD and KID Use Distinct ATPase Mechanisms and Microtubule Interactions to Perform a Similar Function.

Walker BC, Tempel W, Zhu H, Park HW, Cochran JC

Biochemistry. doi: 10.1021/acs.biochem.9b00011

Publication date: April 11, 2019

PMID: 30973712

A Tail-Based Mechanism Drives Nucleosome Demethylation by the LSD2/NPAC Multimeric Complex.

Marabelli C, Marrocco B, Pilotto S, Chittori S, Picaud S, Marchese S, Ciossani G, Forneris F, Filippakopoulos P, Schoehn G, Rhodes D, Subramaniam S, Mattevi A

Cell Rep. 27(2):387-399.e7. doi: 10.1016/j.celrep.2019.03.061

Publication date: April 9, 2019

PMID: 30970244

Bromodomain inhibition of the coactivators CBP/EP300 facilitate cellular reprogramming.

Ebrahimi A, Sevinç K, Gürhan Sevinç G, Cribbs AP, Philpott M, Uyulur F, Morova T, Dunford JE, Göklemez S, Arı Ş, Oppermann U, Önder TT

Nat. Chem. Biol.. doi: 10.1038/s41589-019-0264-z

Publication date: April 8, 2019

PMID: 30962627

A Parsimonious Mechanism of Sugar Dehydration by Human GDP-Mannose-4,6-dehydratase.

Pfeiffer M, Johansson C, Krojer T, Kavanagh KL, Oppermann U, Nidetzky B

ACS Catal. 9(4):2962-2968. doi: 10.1021/acscatal.9b00064

Publication date: April 5, 2019

PMID: 30984471

Substrate reduction therapy for inborn errors of metabolism.

Yue WW, Mackinnon S, Bezerra GA

Emerg Top Life Sci. 3(1):63-73. doi: 10.1042/ETLS20180058

Publication date: March 29, 2019

PMID: 33523197

Targeting bivalency de-represses Indian Hedgehog and inhibits self-renewal of colorectal cancer-initiating cells.

Lima-Fernandes E, Murison A, da Silva Medina T, Wang Y, Ma A, Leung C, Luciani GM, Haynes J, Pollett A, Zeller C, Duan S, Kreso A, Barsyte-Lovejoy D, Wouters BG, Jin J, Carvalho DD, Lupien M, Arrowsmith CH, O'Brien CA

Nat Commun. 10(1):1436. doi: 10.1038/s41467-019-09309-4

Publication date: March 29, 2019

PMID: 30926792

Crystal structure and activity-based labeling reveal the mechanisms for linkage-specific substrate recognition by deubiquitinase USP9X.

Paudel P, Zhang Q, Leung C, Greenberg HC, Guo Y, Chern YH, Dong A, Li Y, Vedadi M, Zhuang Z, Tong Y

Proc. Natl. Acad. Sci. U.S.A.. doi: 10.1073/pnas.1815027116

Publication date: March 26, 2019

PMID: 30914461

AKT drives SOX2 overexpression and cancer cell stemness in esophageal cancer by protecting SOX2 from UBR5-mediated degradation.

Wang Z, Kang L, Zhang H, Huang Y, Fang L, Li M, Brown PJ, Arrowsmith CH, Li J, Wong J

Oncogene. doi: 10.1038/s41388-019-0790-x

Publication date: March 20, 2019

PMID: 30894683

Leveraging Compound Promiscuity to Identify Targetable Cysteines within the Kinome.

Rao S, Gurbani D, Du G, Everley RA, Browne CM, Chaikuad A, Li T, Schröder M, Gondi S, Ficarro SB, Sim T, Kim ND, Berberich MJ, Knapp S, Marto JA, Westover KD, Sorger PK, Gray NS

Cell Chem Biol. doi: 10.1016/j.chembiol.2019.02.021

Publication date: March 18, 2019

PMID: 30982749

Targeting the Small GTPase Superfamily through their Regulatory Proteins.

Gray JL, von Delft F, Brennan P

Angew. Chem. Int. Ed. Engl.. doi: 10.1002/anie.201900585

Publication date: March 14, 2019

PMID: 30869179

Divergent roles of prostacyclin and PGE2 in human tendinopathy.

Bergqvist F, Carr AJ, Wheway K, Watkins B, Oppermann U, Jakobsson PJ, Dakin SG

Arthritis Res. Ther.. 21(1):74. doi: 10.1186/s13075-019-1855-5

Publication date: March 13, 2019

PMID: 30867043

Solution structures and biophysical analysis of full-length group A PAKs reveal they are monomeric and auto-inhibited in cis.

Sorrell FJ, Kilian LM, Elkins JM

Biochem. J.. doi: 10.1042/BCJ20180867

Publication date: March 11, 2019

PMID: 30858169

Lrig2 and Hpse2, mutated in urofacial syndrome, pattern nerves in the urinary bladder.

Roberts NA, Hilton EN, Lopes FM, Singh S, Randles MJ, Gardiner NJ, Chopra K, Coletta R, Bajwa Z, Hall RJ, Yue WW, Schaefer F, Weber S, Henriksson R, Stuart HM, Hedman H, Newman WG, Woolf AS

Kidney Int.. doi: 10.1016/j.kint.2018.11.040

Publication date: March 8, 2019

PMID: 30885509

Role of protein structure in variant annotation: structural insight of mutations causing 6-pyruvoyl-tetrahydropterin synthase deficiency.

Muniz JRC, Szeto NW, Frise R, Lee WH, Wang XS, Thöny B, Himmelreich N, Blau N, Hsiao KJ, Liu TT, Gileadi O, Oppermann U, Von Delft F, Yue WW, Tang NL

Pathology. doi: 10.1016/j.pathol.2018.11.011

Publication date: March 7, 2019

PMID: 30853107

Design and characterization of mutant and wild-type huntingtin proteins produced from a toolkit of scalable eukaryotic expression systems.

Harding RJ, Loppnau P, Ackloo S, Lemak A, Hutchinson A, Hunt B, Holehouse AS, Ho JC, Fan L, Toledo-Sherman L, Seitova A, Arrowsmith CH

J. Biol. Chem.. doi: 10.1074/jbc.RA118.007204

Publication date: March 6, 2019

PMID: 30842263

Organizational innovation for developing new medicines that target aging and age-related conditions.

Ford GA, Lord JM, Ferguson MA, Bountra C, Le Couteur DG

J. Gerontol. A Biol. Sci. Med. Sci.. doi: 10.1093/gerona/glz062

Publication date: March 6, 2019

PMID: 30838376

RNA interference may result in unexpected phenotypes in Caenorhabditis elegans.

De-Souza EA, Camara H, Salgueiro WG, Moro RP, Knittel TL, Tonon G, Pinto S, Pinca APF, Antebi A, Pasquinelli AE, Massirer KB, Mori MA

Nucleic Acids Res.. doi: 10.1093/nar/gkz154

Publication date: March 6, 2019

PMID: 30838421

A pharmacological master key mechanism that unlocks the selectivity filter gate in K+ channels.

Schewe M, Sun H, Mert Ü, Mackenzie A, Pike ACW, Schulz F, Constantin C, Vowinkel KS, Conrad LJ, Kiper AK, Gonzalez W, Musinszki M, Tegtmeier M, Pryde DC, Belabed H, Nazare M, de Groot BL, Decher N, Fakler B, Carpenter EP, Tucker SJ, Baukrowitz T

Science. 363(6429):875-880. doi: 10.1126/science.aav0569

Publication date: February 22, 2019

PMID: 30792303

Designing Dual Inhibitors of Anaplastic Lymphoma Kinase (ALK) and Bromodomain-4 (BRD4) by Tuning Kinase Selectivity.

Watts E, Heidenreich D, Tucker E, Raab M, Strebhardt K, Chesler L, Knapp S, Bellenie B, Hoelder S

J. Med. Chem.. doi: 10.1021/acs.jmedchem.8b01947

Publication date: February 21, 2019

PMID: 30789735

Structural insights into SETD3-mediated histidine methylation on β-actin.

Guo Q, Liao S, Kwiatkowski S, Tomaka W, Yu H, Wu G, Tu X, Min J, Drozak J, Xu C

Elife. 8:. doi: 10.7554/eLife.43676

Publication date: February 20, 2019

PMID: 30785395

Teneurin C-Terminal Associated Peptide (TCAP)-1 and Latrophilin Interaction in HEK293 Cells: Evidence for Modulation of Intercellular Adhesion.

Husić M, Barsyte-Lovejoy D, Lovejoy DA

Front Endocrinol (Lausanne). 10:22. doi: 10.3389/fendo.2019.00022

Publication date: February 19, 2019

PMID: 30774623

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.. doi: 10.1021/acs.jmedchem.8b01213

Publication date: February 15, 2019

PMID: 30768268

Response to: 'Potential roles for tenascin in (very) early diagnosis and treatment of rheumatoid arthritis' by Cutolo et al.

Aungier S, Cartwright AJ, Schwenzer A, Marshall J, Dyson MR, Slavny P, Parthiban K, Karatt-Vellatt A, Sahbudin I, Culbert E, Hextall P, Clanchy FI, Williams R, Marsden BD, Raza K, Filer A, Buckley CD, McCafferty J, Midwood KS

Ann. Rheum. Dis.. doi: 10.1136/annrheumdis-2019-215108

Publication date: February 12, 2019

PMID: 30755416

Ideation and implementation of an open science drug discovery business model - M4K Pharma.

Morgan MR, Roberts OG, Edwards AM

Wellcome Open Res. 3:154. doi: 10.12688/wellcomeopenres.14947.1

Publication date: February 2, 2019

PMID: 30705971

4'-Phosphopantetheine and long acyl chain-dependent interactions are integral to human mitochondrial acyl carrier protein function.

Majmudar JD, Feng X, Fox NG, Nabhan JF, Towle T, Ma T, Gooch R, Bulawa C, Yue WW, Martelli A

Medchemcomm. 10(2):209-220. doi: 10.1039/c8md00489g

Publication date: February 1, 2019

PMID: 30881609

Open notebook science can maximize impact for rare disease projects.

Harding RJ

PLoS Biol. 17(1):e3000120. doi: 10.1371/journal.pbio.3000120

Publication date: January 29, 2019

PMID: 30689629

New pyrido[3,4-g]quinazoline derivatives as CLK1 and DYRK1A inhibitors: synthesis, biological evaluation and binding mode analysis.

Tazarki H, Zeinyeh W, Esvan YJ, Knapp S, Chatterjee D, Schröder M, Joerger AC, Khiari J, Josselin B, Baratte B, Bach S, Ruchaud S, Anizon F, Giraud F, Moreau P

Eur J Med Chem. 166:304-317. doi: 10.1016/j.ejmech.2019.01.052

Publication date: January 26, 2019

PMID: 30731399

Structural basis for species-selective targeting of Hsp90 in a pathogenic fungus.

Whitesell L, Robbins N, Huang DS, McLellan CA, Shekhar-Guturja T, LeBlanc EV, Nation CS, Hui R, Hutchinson A, Collins C, Chatterjee S, Trilles R, Xie JL, Krysan DJ, Lindquist S, Porco JA, Tatu U, Brown LE, Pizarro J, Cowen LE

Nat Commun. 10(1):402. doi: 10.1038/s41467-018-08248-w

Publication date: January 24, 2019

PMID: 30679438

Genetic, structural, and functional analysis of pathogenic variations causing methylmalonyl-CoA epimerase deficiency.

Heuberger K, Bailey HJ, Burda P, Chaikuad A, Krysztofinska E, Suormala T, Bürer C, Lutz S, Fowler B, Froese DS, Yue WW, Baumgartner MR

Biochim Biophys Acta Mol Basis Dis. doi: 10.1016/j.bbadis.2019.01.021

Publication date: January 22, 2019

PMID: 30682498

Identification of a novel biomarker for pyridoxine-dependent epilepsy: Implications for newborn screening.

Wempe MF, Kumar A, Kumar V, Choi YJ, Swanson MA, Friederich MW, Hyland K, Yue WW, Van Hove JLK, Coughlin CR

J. Inherit. Metab. Dis.. doi: 10.1002/jimd.12059

Publication date: January 21, 2019

PMID: 30663059

A chemical biology toolbox to study protein methyltransferases and epigenetic signaling.

Scheer S, Ackloo S, Medina TS, Schapira M, Li F, Ward JA, Lewis AM, Northrop JP, Richardson PL, Kaniskan HÜ, Shen Y, Liu J, Smil D, McLeod D, Zepeda-Velazquez CA, Luo M, Jin J, Barsyte-Lovejoy D, Huber KVM, De Carvalho DD, Vedadi M, Zaph C, Brown PJ, Arrowsmith CH

Nat Commun. 10(1):19. doi: 10.1038/s41467-018-07905-4

Publication date: January 3, 2019

PMID: 30604761

Structural insights into trans-histone regulation of H3K4 methylation by unique histone H4 binding of MLL3/4.

Liu Y, Qin S, Chen TY, Lei M, Dhar SS, Ho JC, Dong A, Loppnau P, Li Y, Lee MG, Min J

Nat Commun. 10(1):36. doi: 10.1038/s41467-018-07906-3

Publication date: January 3, 2019

PMID: 30604749

UbiHub: a data hub for the explorers of ubiquitination pathways.

Liu L, Damerell DR, Koukouflis L, Tong Y, Marsden BD, Schapira M

Bioinformatics. doi: 10.1093/bioinformatics/bty1067

Publication date: January 2, 2019

PMID: 30601939

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. 26(1):79-93.e8. doi: 10.1016/j.celrep.2018.12.023

Publication date: January 2, 2019

PMID: 30605688

2018

An Activity-Based Probe Targeting Non-Catalytic, Highly Conserved Amino Acid Residues within Bromodomains.

D'Ascenzio M, Pugh KM, Konietzny R, Berridge G, Tallant C, Hashem S, Monteiro O, Thomas JR, Schirle M, Knapp S, Marsden B, Fedorov O, Bountra C, Kessler BM, Brennan PE

Angew. Chem. Int. Ed. Engl.. doi: 10.1002/anie.201807825

Publication date: December 27, 2018

PMID: 30589164

Single-Molecule Protein Phosphorylation and Dephosphorylation by Nanopore Enzymology.

Harrington L, Alexander LT, Knapp S, Bayley H

ACS Nano. doi: 10.1021/acsnano.8b07697

Publication date: December 27, 2018

PMID: 30588793

Furo[3,2-b]pyridine: A Privileged Scaffold for Highly Selective Kinase Inhibitors and Effective Modulators of the Hedgehog Pathway.

Němec V, Hylsová M, Maier L, Flegel J, Sievers S, Ziegler S, Schroeder M, Berger BT, Chaikuad A, Valčíková B, Uldrijan S, Drápela S, Souček K, Waldmann H, Knapp S, Paruch K

Angew. Chem. Int. Ed. Engl.. doi: 10.1002/anie.201810312

Publication date: December 20, 2018

PMID: 30569600

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