Publications

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Displaying 201 - 250 of 2122

2020

March 2020

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 89:557-581 . doi: 10.1146/annurev-biochem-011420-092302
Publication date: March 24, 2020
PMID: 32208767
Structural Basis for EPC1-Mediated Recruitment of MBTD1 into the NuA4/TIP60 Acetyltransferase Complex.
Zhang H, Devoucoux M, Song X, Li L, Ayaz G, Cheng H, Tempel W, Dong C, Loppnau P, Côté J, Min J
Cell Rep 30(12):3996-4002.e4 . doi: 10.1016/j.celrep.2020.03.003
Publication date: March 24, 2020
PMID: 32209463
A Highly Selective Chemical Probe for Activin Receptor-like Kinases ALK4 and ALK5
Hanke T, Wong JF, Berger B-T, Abdi I, Berger LM, Tesch R, Tredup C, Bullock AN, Müller S, Knapp S
ACS Chemical Biology 15:862-870 . doi: 10.1021/acschembio.0c00076
Publication date: March 20, 2020
PMID: 32176847
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. . doi: 10.1021/acschembio.0c00076
Publication date: March 16, 2020
PMID: 32176847
SGC-AAK1-1: A Chemical Probe Targeting AAK1 and BMP2K.
Wells C, Couñago RM, Limas JC, Almeida TL, Cook JG, Drewry DH, Elkins JM, Gileadi O, Kapadia NR, Lorente-Macias A, Pickett JE, Riemen A, Ruela-de-Sousa RR, Willson TM, Zhang C, Zuercher WJ, Zutshi R, Axtman AD
ACS Med Chem Lett 11(3):340-345 . doi: 10.1021/acsmedchemlett.9b00399
Publication date: March 12, 2020
PMID: 32184967
Importance of Quantifying Drug-Target Engagement in Cells
Stefaniak J, Huber KVM
ACS Medicinal Chemistry Letters 11:403-406 . doi: 10.1021/acsmedchemlett.9b00570
Publication date: March 6, 2020
PMID: 32292539
Mutant ACVR1 Arrests Glial Cell Differentiation to Drive Tumorigenesis in Pediatric Gliomas
Fortin J, Tian R, Zarrabi I, Hill G, Williams E, Sanchez-Duffhues G, Thorikay M, Ramachandran P, Siddaway R, Wong JF, Wu A, Apuzzo LN, Haight J, You-Ten A, Snow BE, Wakeham A, Goldhamer DJ, Schramek D, Bullock AN, Dijke PT, Hawkins C, Mak TW
Cancer Cell 37:308-323.e12 . doi: 10.1016/j.ccell.2020.02.002
Publication date: March 5, 2020
PMID: 32142668
Histone H3K27me3 demethylases regulate human Th17 cell development and effector functions by impacting on metabolism.
Cribbs AP, Terlecki-Zaniewicz S, Philpott M, Baardman J, Ahern D, Lindow M, Obad S, Oerum H, Sampey B, Mander PK, Penn H, Wordsworth P, Bowness P, de Winther M, Prinjha RK, Feldmann M, Oppermann U
Proc. Natl. Acad. Sci. U.S.A. . doi: 10.1073/pnas.1919893117
Publication date: March 2, 2020
PMID: 32123118
Crystal structure of the catalytic D2 domain of the AAA+ ATPase p97 reveals a putative helical split-washer-type mechanism for substrate unfolding
Stach L, Morgan RM, Makhlouf L, Douangamath A, von Delft F, Zhang X, Freemont PS
FEBS Letters 594:933-943 . doi: 10.1002/1873-3468.13667
Publication date: March 1, 2020
PMID: 31701538
Effects of epigenetic pathway inhibitors on corticotroph tumour AtT20 cells
LINES K, FILIPPAKOPOULOS P, STEVENSON M, Lockstone H, WRIGHT B, BUCK D, BOUNTRA C, THAKKER RV
Endocrine-Related Cancer 27:163-174 . doi: 10.1530/ERC-19-0448
Publication date: March 1, 2020
PMID: 31935194

February 2020

Re-evaluating the mechanism of action of α,β-unsaturated carbonyl DUB inhibitors b-AP15 and VLX1570: a paradigmatic example of unspecific protein crosslinking with Michael acceptor motif-containing drugs
WARD JA, PINTO FERNANDEZ A, Cornelissen L, BONHAM S, DIAZ SAEZ L, Riant O, HUBER KVM, KESSLER BM, Feron O, Tate EW
Journal of Medicinal Chemistry 63:3756-3762 . doi: 10.1021/acs.jmedchem.0c00144
Publication date: February 28, 2020
PMID:
Re-evaluating the mechanism of action of α,β-unsaturated carbonyl DUB inhibitors b-AP15 and VLX1570: a paradigmatic example of unspecific protein crosslinking with Michael acceptor motif-containing drugs.
Ward JA, Pinto-Fernandez A, Cornelissen L, Bonham S, Díaz-Sáez L, Riant O, Huber KVM, Kessler BM, Feron O, Tate EW
J. Med. Chem. . doi: 10.1021/acs.jmedchem.0c00144
Publication date: February 28, 2020
PMID: 32109059
Mutant ACVR1 Arrests Glial Cell Differentiation to Drive Tumorigenesis in Pediatric Gliomas.
Fortin J, Tian R, Zarrabi I, Hill G, Williams E, Sanchez-Duffhues G, Thorikay M, Ramachandran P, Siddaway R, Wong JF, Wu A, Apuzzo LN, Haight J, You-Ten A, Snow BE, Wakeham A, Goldhamer DJ, Schramek D, Bullock AN, Dijke PT, Hawkins C, Mak TW
Cancer Cell . doi: 10.1016/j.ccell.2020.02.002
Publication date: February 21, 2020
PMID: 32142668
Structure-based view of the druggable genome.
Wang J, Yazdani S, Han A, Schapira M
Drug Discov. Today . doi: 10.1016/j.drudis.2020.02.006
Publication date: February 19, 2020
PMID: 32084498
Development of 2-(4-pyridyl)-benzimidazoles as PKN2 chemical tools to probe cancer.
Scott F, Fala AM, Pennicott LE, Reuillon TD, Massirer KB, Elkins JM, Ward SE
Bioorg. Med. Chem. Lett. 127040 . doi: 10.1016/j.bmcl.2020.127040
Publication date: February 17, 2020
PMID: 32085971
Michelanglo: sculpting protein views on web pages without coding.
Ferla MP, Pagnamenta AT, Damerell D, Taylor JC, Marsden BD
Bioinformatics . doi: 10.1093/bioinformatics/btaa104
Publication date: February 15, 2020
PMID: 32061125
MichelaNglo: sculpting protein views on web pages without coding
Ferla MP, Pagnamenta AT, Damerell D, Taylor JC, Marsden BD
Bioinformatics 36:3268-3270 . doi: 10.1093/bioinformatics/btaa104
Publication date: February 15, 2020
PMID: 32061125
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 11(5):535-549 . doi: 10.18632/oncotarget.27462
Publication date: February 4, 2020
PMID: 32082487

January 2020

In vitro benchmarking of NF-κB inhibitors.
Harrold AP, Cleary MM, Bharathy N, Lathara M, Berlow NE, Foreman NK, Donson AM, Amani V, Zuercher WJ, Keller C
Eur. J. Pharmacol. 172981 . doi: 10.1016/j.ejphar.2020.172981
Publication date: January 31, 2020
PMID: 32014486
Bi-allelic Variants in TKFC Encoding Triokinase/FMN Cyclase Are Associated with Cataracts and Multisystem Disease.
Wortmann SB, Meunier B, Mestek-Boukhibar L, van den Broek F, Maldonado EM, Clement E, Weghuber D, Spenger J, Jaros Z, Taha F, Yue WW, Heales SJ, Davison JE, Mayr JA, Rahman S
Am. J. Hum. Genet. . doi: 10.1016/j.ajhg.2020.01.005
Publication date: January 17, 2020
PMID: 32004446
In Depth Analysis of Kinase Cross Screening Data to Identify CAMKK2 Inhibitory Scaffolds.
O'Byrne SN, Scott JW, Pilotte JR, Santiago ADS, Langendorf CG, Oakhill JS, Eduful BJ, Couñago RM, Wells CI, Zuercher WJ, Willson TM, Drewry DH
Molecules 25(2): . doi: 10.3390/molecules25020325
Publication date: January 13, 2020
PMID: 31941153
Overcoming Fungal Echinocandin Resistance through Inhibition of the Non-essential Stress Kinase Yck2.
Caplan T, Lorente-Macías Á, Stogios PJ, Evdokimova E, Hyde S, Wellington MA, Liston S, Iyer KR, Puumala E, Shekhar-Guturja T, Robbins N, Savchenko A, Krysan DJ, Whitesell L, Zuercher WJ, Cowen LE
Cell Chem Biol . doi: 10.1016/j.chembiol.2019.12.008
Publication date: January 6, 2020
PMID: 31924499
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 . doi: 10.1530/ERC-19-0448
Publication date: January 1, 2020
PMID: 31935194
2019

December 2019

Human MettL3-MettL14 complex is a sequence-specific DNA adenine methyltransferase active on single-strand and unpaired DNA in vitro.
Woodcock CB, Yu D, Hajian T, Li J, Huang Y, Dai N, Corrêa IR, Wu T, Vedadi M, Zhang X, Cheng X
Cell Discov 5:63 . doi: 10.1038/s41421-019-0136-4
Publication date: December 31, 2019
PMID: 31885874
The crystal structure of human forkhead box N1 in complex with DNA reveals the structural basis for forkhead box family specificity.
Newman JA, Aitkenhead H, Gavard AE, Rota IA, Handel AE, Hollander GA, Gileadi O
J. Biol. Chem. . doi: 10.1074/jbc.RA119.010365
Publication date: December 30, 2019
PMID: 31914405
Discovery of a chemical probe for PRDM9.
Allali-Hassani A, Szewczyk MM, Ivanochko D, Organ SL, Bok J, Ho JSY, Gay FPH, Li F, Blazer L, Eram MS, Halabelian L, Dilworth D, Luciani GM, Lima-Fernandes E, Wu Q, Loppnau P, Palmer N, Talib SZA, Brown PJ, Schapira M, Kaldis P, O'Hagan RC, Guccione E, Barsyte-Lovejoy D, Arrowsmith CH, Sanders JM, Kattar SD, Bennett DJ, Nicholson B, Vedadi M
Nat Commun 10(1):5759 . doi: 10.1038/s41467-019-13652-x
Publication date: December 17, 2019
PMID: 31848333
Synthesis and Biological Investigation of (+)-JD1, an Organometallic BET Bromodomain Inhibitor
Hassell-Hart S, Runcie A, Krojer T, Doyle J, Lineham E, Ocasio CA, Neto BAD, Fedorov O, Marsh G, Maple H, Felix R, Banks R, Ciulli A, Picaud S, Filippakopoulos P, Von Delft F, Brennan P, Stewart HJS, Chevassut TJ, Walker M, Austin C, Morley S, Spencer J
Organometallics . doi: 10.1021/acs.organomet.9b00750
Publication date: December 17, 2019
PMID:
Structural Insights into Interaction Mechanisms of Alternative Piperazine-urea YEATS Domain Binders in MLLT1.
Ni X, Heidenreich D, Christott T, Bennett J, Moustakim M, Brennan PE, Fedorov O, Knapp S, Chaikuad A
ACS Med Chem Lett 10(12):1661-1666 . doi: 10.1021/acsmedchemlett.9b00460
Publication date: December 12, 2019
PMID: 31857843
Methyltransferase Inhibitors: Competing with, or Exploiting the Bound Cofactor.
Ferreira de Freitas R, Ivanochko D, Schapira M
Molecules 24(24): . doi: 10.3390/molecules24244492
Publication date: December 8, 2019
PMID: 31817960
Structural consequences of BMPR2 kinase domain mutations causing pulmonary arterial hypertension
BULLOCK A, Chaikuad A, Thangaratnarajah C, VON DELFT F
Scientific Reports 9:18351- . doi: 10.1038/s41598-019-54830-7
Publication date: December 4, 2019
PMID: 31797984
Structural consequences of BMPR2 kinase domain mutations causing pulmonary arterial hypertension.
Chaikuad A, Thangaratnarajah C, von Delft F, Bullock AN
Sci Rep 9(1):18351 . doi: 10.1038/s41598-019-54830-7
Publication date: December 4, 2019
PMID: 31797984
Chemical Probes for Protein Arginine Methyltransferases.
Ming Li AS, Li F, Eram MS, Bolotokova A, Dela Seña CC, Vedadi M
Methods . doi: 10.1016/j.ymeth.2019.11.017
Publication date: December 3, 2019
PMID: 31809836
Lipid Interactions of a Ciliary Membrane TRP Channel: Simulation and Structural Studies of Polycystin-2 (PC2)
WANG Q, COREY RA, Hedger G, Aryal P, GRIEBEN M, NASRALLAH C, Baronina A, PIKE A, Shi J, CARPENTER EP, SANSOM MSP
Structure 28:169-184.e5 . doi: 10.1016/j.str.2019.11.005
Publication date: December 2, 2019
PMID: 31806353

November 2019

Synthetic Peptides as Therapeutic Agents: Lessons Learned From Evolutionary Ancient Peptides and Their Transit Across Blood-Brain Barriers.
Lovejoy DA, Hogg DW, Dodsworth TL, Jurado FR, Read CC, D'Aquila AL, Barsyte-Lovejoy D
Front Endocrinol (Lausanne) 10:730 . doi: 10.3389/fendo.2019.00730
Publication date: November 30, 2019
PMID: 31781029
Lipid Interactions of a Ciliary Membrane TRP Channel: Simulation and Structural Studies of Polycystin-2.
Wang Q, Corey RA, Hedger G, Aryal P, Grieben M, Nasrallah C, Baronina A, Pike ACW, Shi J, Carpenter EP, Sansom MSP
Structure . doi: 10.1016/j.str.2019.11.005
Publication date: November 27, 2019
PMID: 31806353
Development of Macrocycle Kinase Inhibitors for ALK2 Using Fibrodysplasia Ossificans Progressiva-Derived Endothelial Cells.
Sánchez-Duffhues G, Williams E, Benderitter P, Orlova V, van Wijhe M, Garcia de Vinuesa A, Kerr G, Caradec J, Lodder K, de Boer HC, Goumans MJ, Eekhoff EMW, Morales-Piga A, Bachiller-Corral J, Koolwijk P, Bullock AN, Hoflack J, Ten Dijke P
JBMR Plus 3(11):e10230 . doi: 10.1002/jbm4.10230
Publication date: November 27, 2019
PMID: 31768489
The fungal metabolite chaetocin is a sensitizer for pro-apoptotic therapies in glioblastoma.
Ozyerli-Goknar E, Sur-Erdem I, Seker F, Cingöz A, Kayabolen A, Kahya-Yesil Z, Uyulur F, Gezen M, Tolay N, Erman B, Gönen M, Dunford J, Oppermann U, Bagci-Onder T
Cell Death Dis 10(12):894 . doi: 10.1038/s41419-019-2107-y
Publication date: November 26, 2019
PMID: 31772153
Structural Insights into Interaction Mechanisms of Alternative Piperazine-urea YEATS Domain Binders in MLLT1
Ni X, Heidenreich D, Christott T, Bennett J, Moustakim M, Brennan PE, Fedorov O, Knapp S, Chaikuad A
ACS Medicinal Chemistry Letters 10:1661-1666 . doi: 10.1021/acsmedchemlett.9b00460
Publication date: November 25, 2019
PMID: 31857843
Janus kinase inhibition for autoinflammation in patients with DNASE2 deficiency
Hong Y, Capitani M, Murphy C, Pandey S, Cavounidis A, Takeshita H, Nanthapisal S, Yasuda T, Bader-Meunier B, McCreary D, Omoyinmi E, Rao A, Booth C, Gilmour K, Sebire N, Shah N, Klein N, Bullock AN, Eleftheriou D, Uhlig HH, Brogan P
Journal of Allergy and Clinical Immunology 145:701-705.e8 . doi: 10.1016/j.jaci.2019.11.020
Publication date: November 24, 2019
PMID: 31775019
Janus kinase inhibition for autoinflammation in DNASE2 deficiency.
Hong Y, Capitani M, Murphy C, Pandey S, Cavounidis A, Takeshita H, Nanthapisal S, Yasuda T, Bader-Meunier B, McCreary D, Omoyinmi E, Rao A, Booth C, Gilmour K, Sebire N, Shah N, Klein N, Bullock AN, Eleftheriou D, Uhlig HH, Brogan P
J. Allergy Clin. Immunol. . doi: 10.1016/j.jaci.2019.11.020
Publication date: November 24, 2019
PMID: 31775019
HMCES Functions in the Alternative End-Joining Pathway of the DNA DSB Repair during Class Switch Recombination in B Cells.
Shukla V, Halabelian L, Balagere S, Samaniego-Castruita D, Feldman DE, Arrowsmith CH, Rao A, Aravind L
Mol. Cell . doi: 10.1016/j.molcel.2019.10.031
Publication date: November 15, 2019
PMID: 31806351
Binding and structural analyses of potent inhibitors of the human Ca2+/calmodulin dependent protein kinase kinase 2 (CAMKK2) identified from a collection of commercially-available kinase inhibitors.
Profeta GS, Dos Reis CV, Santiago ADS, Godoi PHC, Fala AM, Wells CI, Sartori R, Salmazo APT, Ramos PZ, Massirer KB, Elkins JM, Drewry DH, Gileadi O, Couñago RM
Sci Rep 9(1):16452 . doi: 10.1038/s41598-019-52795-1
Publication date: November 11, 2019
PMID: 31712618
Emerging tools to investigate bromodomain functions
Kougnassoukou Tchara PE, Filippakopoulos P, Lambert JP
Methods . doi: 10.1016/j.ymeth.2019.11.003
Publication date: November 11, 2019
PMID: 31726225
Binding and structural analyses of potent inhibitors of the human Ca<sup>2+</sup>/calmodulin dependent protein kinase kinase 2 (CAMKK2) identified from a collection of commercially-available kinase inhibitors
Profeta GS, Dos Reis CV, Santiago ADS, Godoi PHC, Fala AM, Wells CI, Sartori R, Salmazo APT, Ramos PZ, Massirer KB, Elkins JM, Drewry DH, Gileadi O, Couñago RM
Scientific reports 9:16452- . doi: 10.1038/s41598-019-52795-1
Publication date: November 11, 2019
PMID: 31712618
Emerging tools to investigate bromodomain functions.
Kougnassoukou Tchara PE, Filippakopoulos P, Lambert JP
Methods . doi: 10.1016/j.ymeth.2019.11.003
Publication date: November 11, 2019
PMID: 31726225
A fast iterative synthetic approach towards the identification of novel highly selective p38 MAP kinase inhibitors.
Röhm S, Berger BT, Schröder M, Chaikuad A, Winkel R, Hekking KFW, Benningshof JJC, Mueller G, Tesch R, Kudolo M, Forster M, Laufer SA, Knapp S
J. Med. Chem. . doi: 10.1021/acs.jmedchem.9b01227
Publication date: November 8, 2019
PMID: 31702918
Towards the Development of an In vivo Chemical Probe for Cyclin G Associated Kinase (GAK).
Asquith CRM, Bennett JM, Su L, Laitinen T, Elkins JM, Pickett JE, Wells CI, Li Z, Willson TM, Zuercher WJ
Molecules 24(22): . doi: 10.3390/molecules24224016
Publication date: November 6, 2019
PMID: 31698822
Towards the Development of an In vivo Chemical Probe for Cyclin G Associated Kinase (GAK)
Asquith CRM, Bennett JM, Su L, Laitinen T, Elkins JM, Pickett JE, Wells CI, Li Z, Willson TM, Zuercher WJ
Molecules (Basel, Switzerland) 24:- . doi: 10.3390/molecules24224016
Publication date: November 6, 2019
PMID: 31698822
Multiple direct interactions of TBP with the MYC oncoprotein.
Wei Y, Resetca D, Li Z, Johansson-Åkhe I, Ahlner A, Helander S, Wallenhammar A, Morad V, Raught B, Wallner B, Kokubo T, Tong Y, Penn LZ, Sunnerhagen M
Nat. Struct. Mol. Biol. . doi: 10.1038/s41594-019-0321-z
Publication date: November 4, 2019
PMID: 31686052
Design and analysis of the 4-anilino-quin(az)oline kinase inhibition profiles of GAK/SLK/STK10 using quantitative structure activity relationships.
Asquith CRM, Laitinen T, Bennett JM, Wells CI, Elkins JM, Zuercher WJ, Tizzard G, Poso A
ChemMedChem . doi: 10.1002/cmdc.201900521
Publication date: November 1, 2019
PMID: 31675459

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