Publications

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2024

Autoinhibition of ubiquitin-specific protease 8: insights into domain interactions and mechanisms of regulation.

Caba C, Black M, Liu Y, DaDalt AA, Mallare J, Fan L, Harding RJ, Wang Y, Vacratsis PO, Huang R, Zhuang Z, Tong Y

J Biol Chem. 107727. doi: 10.1016/j.jbc.2024.107727

Publication date: August 28, 2024

PMID: 39214302

A guide to selecting high-performing antibodies for Synaptotagmin-1 (Uniprot ID P21579) for use in western blot, immunoprecipitation, immunofluorescence and flow cytometry.

Biddle MS, Alende C, Fotouhi M, Jones C, Ayoubi R, Southern K, Laflamme C, Virk H

F1000Res. 13:817. doi: 10.12688/f1000research.154034.1

Publication date: August 22, 2024

PMID: 39169954

A chemical screen identifies PRMT5 as a therapeutic vulnerability for paclitaxel-resistant triple-negative breast cancer.

Zhang K, Wei J, Zhang S, Fei L, Guo L, Liu X, Ji Y, Chen W, Ciamponi FE, Chen W, Li M, Zhai J, Fu T, Massirer KB, Yu Y, Lupien M, Wei Y, Arrowsmith CH, Wu Q, Tan W

Cell Chem Biol. doi: 10.1016/j.chembiol.2024.08.003

Publication date: August 21, 2024

PMID: 39232499

Chemical coverage of human biological pathways.

Angela Kwak H, Liu L, Tredup C, Röhm S, Prinos P, Böttcher J, Schapira M

Drug Discov Today. 104144. doi: 10.1016/j.drudis.2024.104144

Publication date: August 21, 2024

PMID: 39179147

Screening of a kinase inhibitor library identified novel targetable kinase pathways in triple-negative breast cancer.

Rinderle CH, Baker CV, Lagarde CB, Nguyen K, Al-Ghadban S, Matossian MD, Hoang VT, Martin EC, Collins-Burow BM, Ali S, Drewry DH, Burow ME, Bunnell BA

Anticancer Drugs. doi: 10.1097/CAD.0000000000001658

Publication date: August 21, 2024

PMID: 39163320

Antibody characterization is critical to enhance reproducibility in biomedical research.

Kahn RA, Virk H, Laflamme C, Houston DW, Polinski NK, Meijers R, Levey AI, Saper CB, Errington TM, Turn RE, Bandrowski A, Trimmer JS, Rego M, Freedman LP, Ferrara F, Bradbury ARM, Cable H, Longworth S

Elife. 13:. doi: 10.7554/eLife.100211

Publication date: August 14, 2024

PMID: 39140332

Benchmarking Methods for PROTAC Ternary Complex Structure Prediction.

Rovers E, Schapira M

J Chem Inf Model. 64(15):6162-6173. doi: 10.1021/acs.jcim.4c00426

Publication date: August 12, 2024

PMID: 39087481

Discovery and Characterization of a Chemical Probe for Cyclin-Dependent Kinase-Like 2.

Bashore FM, Min SM, Chen X, Howell S, Rinderle CH, Morel G, Silvaroli JA, Wells CI, Bunnell BA, Drewry DH, Pabla NS, Ultanir SK, Bullock AN, Axtman AD

ACS Med Chem Lett. 15(8):1325-1333. doi: 10.1021/acsmedchemlett.4c00219

Publication date: August 8, 2024

PMID: 39140040

High-Throughput Screening for LC3/GABARAP Binders Utilizing the Fluorescence Polarization Assay.

Schwalm MP, Dopfer J, Knapp S, Rogov VV

Methods Mol Biol. 2845:203-218. doi: 10.1007/978-1-0716-4067-8_17

Publication date: August 8, 2024

PMID: 39115669

Thermodynamic Characterization of LC3/GABARAP:Ligand Interactions by Isothermal Titration Calorimetry.

Dopfer J, Schwalm MP, Knapp S, Rogov VV

Methods Mol Biol. 2845:219-235. doi: 10.1007/978-1-0716-4067-8_18

Publication date: August 8, 2024

PMID: 39115670

A ligand discovery toolbox for the WWE domain family of human E3 ligases.

Münzker L, Kimani SW, Fowkes MM, Dong A, Zheng H, Li Y, Dasovich M, Zak KM, Leung AKL, Elkins JM, Kessler D, Arrowsmith CH, Halabelian L, Böttcher J

Commun Biol. 7(1):901. doi: 10.1038/s42003-024-06584-w

Publication date: July 24, 2024

PMID: 39048679

A high-throughput approach to identify BRCA1-downregulating compounds to enhance PARP inhibitor sensitivity.

Sellars E, Savguira M, Wu J, Cancelliere S, Jen M, Krishnan R, Hakem A, Barsyte-Lovejoy D, Hakem R, Narod SA, Kotsopoulos J, Salmena L

iScience. 27(7):110180. doi: 10.1016/j.isci.2024.110180

Publication date: July 19, 2024

PMID: 38993666

Back-Pocket Optimization of 2-Aminopyrimidine-Based Macrocycles Leads to Potent EPHA2/GAK Kinase Inhibitors.

Gerninghaus J, Zhubi R, Krämer A, Karim M, Tran DHN, Joerger AC, Schreiber C, Berger LM, Berger BT, Ehret TAL, Elson L, Lenz C, Saxena K, Müller S, Einav S, Knapp S, Hanke T

J Med Chem. doi: 10.1021/acs.jmedchem.4c00411

Publication date: July 19, 2024

PMID: 39028937

Huntingtin is an RNA binding protein and participates in NEAT1-mediated paraspeckles.

Yadav M, Harding RJ, Li T, Xu X, Gall-Duncan T, Khan M, Bardile CF, Sequiera GL, Duan S, Chandrasekaran R, Pan A, Bu J, Yamazaki T, Hirose T, Prinos P, Tippett L, Turner C, Curtis MA, Faull RLM, Pouladi MA, Pearson CE, He HH, Arrowsmith CH

Sci Adv. 10(29):eado5264. doi: 10.1126/sciadv.ado5264

Publication date: July 19, 2024

PMID: 39028820

Discovery of Two Highly Selective Structurally Orthogonal Chemical Probes for Activin Receptor-like Kinases 1 and 2.

Němec V, Remeš M, Beňovský P, Böck MC, Šranková E, Wong JF, Cros J, Williams E, Tse LH, Smil D, Ensan D, Isaac MB, Al-Awar R, Gomolková R, Ursachi VC, Fafílek B, Kahounová Z, Víchová R, Vacek O, Berger BT, Wells CI, Corona CR, Vasta JD, Robers MB, Krejci P, Souček K, Bullock AN, Knapp S, Paruch K

J Med Chem. doi: 10.1021/acs.jmedchem.4c00629

Publication date: July 18, 2024

PMID: 39023313

The identification of high-performing antibodies for Sequestosome-1 for use in Western blot, immunoprecipitation and immunofluorescence.

Ayoubi R, Alshafie W, Shlaifer I, Southern K, McPherson PS, Laflamme C

F1000Res. 12:324. doi: 10.12688/f1000research.132628.2

Publication date: July 15, 2024

PMID: 39006307

Synthesis and evaluation of chemical linchpins for highly selective CK2α targeting.

Greco FA, Krämer A, Wahl L, Elson L, Ehret TAL, Gerninghaus J, Möckel J, Müller S, Hanke T, Knapp S

Eur J Med Chem. 276:116672. doi: 10.1016/j.ejmech.2024.116672

Publication date: July 14, 2024

PMID: 39067440

A guide to selecting high-performing antibodies for Rab1A and Rab1B for use in Western Blot, immunoprecipitation and immunofluorescence.

Ruíz Moleón V, Fotouhi M, Ayoubi R, González Bolívar S, Southern K, McPherson PS, Laflamme C

F1000Res. 12:1578. doi: 10.12688/f1000research.143928.2

Publication date: July 11, 2024

PMID: 38559361

A guide to selecting high-performing antibodies for RNA-binding protein TIA1 for use in Western Blot, immunoprecipitation and immunofluorescence.

Fotouhi M, Worrall D, Ayoubi R, Southern K, McPherson PS, Laflamme C

F1000Res. 12:745. doi: 10.12688/f1000research.133645.2

Publication date: July 11, 2024

PMID: 38638178

Characterization of covalent inhibitors that disrupt the interaction between the tandem SH2 domains of SYK and FCER1G phospho-ITAM.

Bashore FM, Katis VL, Du Y, Sikdar A, Wang D, Bradshaw WJ, Rygiel KA, Leisner TM, Chalk R, Mishra S, Williams CA, Gileadi O, Brennan PE, Wiley JC, Gockley J, Cary GA, Carter GW, Young JE, Pearce KH, Fu H, Axtman AD

PLoS One. 19(2):e0293548. doi: 10.1371/journal.pone.0293548

Publication date: July 11, 2024

PMID: 38359047

Identification of high-performing antibodies for Moesin for use in Western Blot, immunoprecipitation, and immunofluorescence.

Alshafie W, Ayoubi R, Fotouhi M, Southern K, Laflamme C

F1000Res. 12:172. doi: 10.12688/f1000research.130126.3

Publication date: July 11, 2024

PMID: 38106655

Illumination of understudied ciliary kinases.

Flax RG, Rosston P, Rocha C, Anderson B, Capener JL, Durcan TM, Drewry DH, Prinos P, Axtman AD

Front Mol Biosci. 11:1352781. doi: 10.3389/fmolb.2024.1352781

Publication date: July 11, 2024

PMID: 38523660

The identification of high-performing antibodies for Charged multivesicular body protein 2b for use in Western Blot, immunoprecipitation and immunofluorescence.

Alshafie W, Fotouhi M, Ayoubi R, Shlaifer I, Southern K, McPherson PS, Laflamme C

F1000Res. 12:884. doi: 10.12688/f1000research.139755.1

Publication date: July 11, 2024

PMID: 37635943

The identification of high-performing antibodies for Profilin-1 for use in Western blot, immunoprecipitation and immunofluorescence.

Ayoubi R, McDowell I, Fotouhi M, Southern K, McPherson PS, Laflamme C

F1000Res. 12:348. doi: 10.12688/f1000research.132249.1

Publication date: July 11, 2024

PMID: 37576538

The identification of high-performing antibodies for RNA-binding protein FUS for use in Western Blot, immunoprecipitation, and immunofluorescence.

Alshalfie W, Fotouhi M, Ayoubi R, You Z, Southern K, McPherson PS, Laflamme C

F1000Res. 12:376. doi: 10.12688/f1000research.133220.2

Publication date: July 11, 2024

PMID: 37384305

The identification of high-performing antibodies for TDP-43 for use in Western Blot, immunoprecipitation and immunofluorescence.

Worrall D, Ayoubi R, Fotouhi M, Southern K, McPherson PS, Laflamme C

F1000Res. 12:277. doi: 10.12688/f1000research.131852.2

Publication date: July 11, 2024

PMID: 37359785

The identification of high-preforming antibodies for Ubiquilin-2 for use in Western Blot, immunoprecipitation, and immunofluorescence.

McDowell I, Ayoubi R, Fotouhi M, Southern K, McPherson PS, Laflamme C

F1000Res. 12:355. doi: 10.12688/f1000research.131851.1

Publication date: July 11, 2024

PMID: 37359784

A data science roadmap for open science organizations engaged in early-stage drug discovery.

Edfeldt K, Edwards AM, Engkvist O, Günther J, Hartley M, Hulcoop DG, Leach AR, Marsden BD, Menge A, Misquitta L, Müller S, Owen DR, Schütt KT, Skelton N, Steffen A, Tropsha A, Vernet E, Wang Y, Wellnitz J, Willson TM, Clevert DA, Haibe-Kains B, Schiavone LH, Schapira M

Nat Commun. 15(1):5640. doi: 10.1038/s41467-024-49777-x

Publication date: July 5, 2024

PMID: 38965235

tracerDB: a crowdsourced fluorescent tracer database for target engagement analysis.

Dopfer J, Vasta JD, Müller S, Knapp S, Robers MB, Schwalm MP

Nat Commun. 15(1):5646. doi: 10.1038/s41467-024-49896-5

Publication date: July 5, 2024

PMID: 38969708

Recruitment of FBXO22 for targeted degradation of NSD2.

Nie DY, Tabor JR, Li J, Kutera M, St-Germain J, Hanley RP, Wolf E, Paulakonis E, Kenney TMG, Duan S, Shrestha S, Owens DDG, Maitland MER, Pon A, Szewczyk M, Lamberto AJ, Menes M, Li F, Penn LZ, Barsyte-Lovejoy D, Brown NG, Barsotti AM, Stamford AW, Collins JL, Wilson DJ, Raught B, Licht JD, James LI, Arrowsmith CH

Nat Chem Biol. doi: 10.1038/s41589-024-01660-y

Publication date: July 4, 2024

PMID: 38965384

More than an Amide Bioisostere: Discovery of 1,2,4-Triazole-containing Pyrazolo[1,5-a]pyrimidine Host CSNK2 Inhibitors for Combatting β-Coronavirus Replication.

Ong HW, Yang X, Smith JL, Dickmander RJ, Brown JW, Havener TM, Taft-Benz S, Howell S, Sanders MK, Capener JL, Couñago RM, Chang E, Krämer A, Moorman NJ, Heise M, Axtman AD, Drewry DH, Willson TM

J Med Chem. doi: 10.1021/acs.jmedchem.4c00962

Publication date: July 3, 2024

PMID: 38959455

A C-Degron Structure-Based Approach for the Development of Ligands Targeting the E3 Ligase TRIM7.

Muñoz Sosa CJ, Lenz C, Hamann A, Farges F, Dopfer J, Krämer A, Cherkashyna V, Tarnovskiy A, Moroz YS, Proschak E, Němec V, Müller S, Saxena K, Knapp S

ACS Chem Biol. doi: 10.1021/acschembio.4c00301

Publication date: June 27, 2024

PMID: 38934237

Identification of Dihydropyrazolo[1,5-a]pyrazin-4(5H)-ones as Cyclic Products of β-Amidomethyl Vinyl Sulfone Alphavirus Cysteine Protease Inhibitors.

Ghoshal A, Magalhães ÁF, Asressu KH, Hossain MA, Todd MH, Willson TM

Pharmaceuticals (Basel). 17(7):. doi: 10.3390/ph17070836

Publication date: June 26, 2024

PMID: 39065687

Subpocket Similarity-Based Hit Identification for Challenging Targets: Application to the WDR Domain of LRRK2.

Eguida M, Bret G, Sindt F, Li F, Chau I, Ackloo S, Arrowsmith C, Bolotokova A, Ghiabi P, Gibson E, Halabelian L, Houliston S, Harding RJ, Hutchinson A, Loppnau P, Perveen S, Seitova A, Zeng H, Schapira M, Rognan D

J Chem Inf Model. doi: 10.1021/acs.jcim.4c00601

Publication date: June 25, 2024

PMID: 38916159

A designed ankyrin-repeat protein that targets Parkinson's disease-associated LRRK2.

Dederer V, Sanz Murillo M, Karasmanis EP, Hatch KS, Chatterjee D, Preuss F, Abdul Azeez KR, Vu Nguyen L, Galicia C, Dreier B, Plückthun A, Versees W, Mathea S, Leschziner AE, Reck-Peterson SL, Knapp S

J Biol Chem. 107469. doi: 10.1016/j.jbc.2024.107469

Publication date: June 12, 2024

PMID: 38876305

Structural basis of p53 inactivation by cavity-creating cancer mutations and its implications for the development of mutant p53 reactivators.

Balourdas DI, Markl AM, Krämer A, Settanni G, Joerger AC

Cell Death Dis. 15(6):408. doi: 10.1038/s41419-024-06739-x

Publication date: June 11, 2024

PMID: 38862470

The Pan-Canadian Chemical Library: A Mechanism to Open Academic Chemistry to High-Throughput Virtual Screening.

Bedart C, Shimokura G, West FG, Wood TE, Batey RA, Irwin JJ, Schapira M

Sci Data. 11(1):597. doi: 10.1038/s41597-024-03443-5

Publication date: June 6, 2024

PMID: 38844472

Anti-FHL1 autoantibodies in adult patients with myositis: a longitudinal follow-up analysis.

Galindo-Feria AS, Lodin K, Horuluoglu B, Sarrafzadeh-Zargar S, Wigren E, Gräslund S, Danielsson O, Wahren-Herlenius M, Dastmalchi M, Lundberg IE

Rheumatology (Oxford). doi: 10.1093/rheumatology/keae317

Publication date: June 4, 2024

PMID: 38833674

Novel Dihydropteridinone Derivatives As Potent Inhibitors of the Understudied Human Kinases Vaccinia-Related Kinase 1 and Casein Kinase 1δ/ε.

de Souza Gama FH, Dutra LA, Hawgood M, Dos Reis CV, Serafim RAM, Ferreira MA, Teodoro BVM, Takarada JE, Santiago AS, Balourdas DI, Nilsson AS, Urien B, Almeida VM, Gileadi C, Ramos PZ, Salmazo A, Vasconcelos SNS, Cunha MR, Mueller S, Knapp S, Massirer KB, Elkins JM, Gileadi O, Mascarello A, Lemmens BBLG, Guimarães CRW, Azevedo H, Couñago RM

J Med Chem. doi: 10.1021/acs.jmedchem.3c02250

Publication date: May 23, 2024

PMID: 38780468

Splice variants of CK1α and CK1α-like: Comparative analysis of subcellular localization, kinase activity and function in the Wnt signaling pathway.

Gybeľ T, Čada Š, Klementová D, Schwalm MP, Berger BT, Šebesta M, Knapp S, Bryja V

J Biol Chem. 107407. doi: 10.1016/j.jbc.2024.107407

Publication date: May 23, 2024

PMID: 38796065

Structural basis for inhibition of the lysosomal two-pore channel TPC2 by a small molecule antagonist.

Chi G, Jaślan D, Kudrina V, Böck J, Li H, Pike ACW, Rautenberg S, Krogsaeter E, Bohstedt T, Wang D, McKinley G, Fernandez-Cid A, Mukhopadhyay SMM, Burgess-Brown NA, Keller M, Bracher F, Grimm C, Dürr KL

Structure. doi: 10.1016/j.str.2024.05.005

Publication date: May 23, 2024

PMID: 38815576

A chemical probe to modulate human GID4 Pro/N-degron interactions.

Owens DDG, Maitland MER, Khalili Yazdi A, Song X, Reber V, Schwalm MP, Machado RAC, Bauer N, Wang X, Szewczyk MM, Dong C, Dong A, Loppnau P, Calabrese MF, Dowling MS, Lee J, Montgomery JI, O'Connell TN, Subramanyam C, Wang F, Adamson EC, Schapira M, Gstaiger M, Knapp S, Vedadi M, Min J, Lajoie GA, Barsyte-Lovejoy D, Owen DR, Schild-Poulter C, Arrowsmith CH

Nat Chem Biol. doi: 10.1038/s41589-024-01618-0

Publication date: May 21, 2024

PMID: 38773330

STOPLIGHT: A Hit Scoring Calculator.

Wellnitz J, Martin HJ, Anwar Hossain M, Rath M, Fox C, Popov KI, Willson TM, Muratov EN, Tropsha A

J Chem Inf Model. doi: 10.1021/acs.jcim.4c00412

Publication date: May 20, 2024

PMID: 38768560