Publications

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Displaying 1 - 50 of 2452

2024

June 2024

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: June 7, 2024
PMID: 37635943
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: June 7, 2024
PMID: 38638178
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: June 7, 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: June 7, 2024
PMID: 37384305
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: June 7, 2024
PMID: 38523660
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: June 7, 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: June 7, 2024
PMID: 37359784
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: June 7, 2024
PMID: 38359047
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: June 7, 2024
PMID: 38559361
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: June 7, 2024
PMID: 38106655
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

May 2024

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
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
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
Development of Peptide Displacement Assays to Screen for Antagonists of DDB1 Interactions.
Yong D, Ahmad S, Mabanglo MF, Halabelian L, Schapira M, Ackloo S, Perveen S, Ghiabi P, Vedadi M
Biochemistry . doi: 10.1021/acs.biochem.4c00044
Publication date: May 10, 2024
PMID: 38729622

April 2024

Luciferase- and HaloTag-based reporter assays to measure small-molecule-induced degradation pathway in living cells.
Schwalm MP, Saxena K, Müller S, Knapp S
Nat Protoc . doi: 10.1038/s41596-024-00979-z
Publication date: April 18, 2024
PMID: 38637703
Expanding the ligand spaces for E3 ligases for the design of protein degraders.
Shah Zaib Saleem R, Schwalm MP, Knapp S
Bioorg Med Chem 105:117718 . doi: 10.1016/j.bmc.2024.117718
Publication date: April 12, 2024
PMID: 38621319
Development of Highly Potent and Selective Covalent FGFR4 Inhibitors Based on SNAr Electrophiles.
Schwarz M, Kurkunov M, Wittlinger F, Rudalska R, Wang G, Schwalm MP, Rasch A, Wagner B, Laufer SA, Knapp S, Dauch D, Gehringer M
J Med Chem . doi: 10.1021/acs.jmedchem.3c02483
Publication date: April 11, 2024
PMID: 38604131
Emerging structure-based computational methods to screen the exploding accessible chemical space.
Bedart C, Simoben CV, Schapira M
Curr Opin Struct Biol 86:102812 . doi: 10.1016/j.sbi.2024.102812
Publication date: April 10, 2024
PMID: 38603987
MITOCHONDRIAL IMPORT STRESS and PINK1-MEDIATED MITOPHAGY: THE ROLE of the PINK1-TOMM-TIMM23 SUPERCOMPLEX.
Eldeeb MA, Fallahi A, Soumbasis A, Bayne AN, Trempe JF, Fon EA
Autophagy . doi: 10.1080/15548627.2024.2340399
Publication date: April 10, 2024
PMID: 38597070
Tetrahydropyridine LIMK inhibitors: Structure activity studies and biological characterization.
Champiré A, Berabez R, Braka A, Cosson A, Corret J, Girardin C, Serrano A, Aci-Sèche S, Bonnet P, Josselin B, Brindeau P, Ruchaud S, Leguevel R, Chatterjee D, Mathea S, Knapp S, Brion R, Verrecchia F, Vallée B, Plé K, Bénédetti H, Routier S
Eur J Med Chem 271:116391 . doi: 10.1016/j.ejmech.2024.116391
Publication date: April 9, 2024
PMID: 38669909
Discovery and optimization of narrow spectrum inhibitors of Tousled like kinase 2 (TLK2) using quantitative structure activity relationships.
Asquith CRM, East MP, Laitinen T, Alamillo-Ferrer C, Hartikainen E, Wells CI, Axtman AD, Drewry DH, Tizzard GJ, Poso A, Willson TM, Johnson GL
Eur J Med Chem 271:116357 . doi: 10.1016/j.ejmech.2024.116357
Publication date: April 2, 2024
PMID: 38636130
Identification and structural characterization of small molecule inhibitors of PINK1.
Rasool S, Shomali T, Truong L, Croteau N, Veyron S, Bustillos BA, Springer W, Fiesel FC, Trempe JF
Sci Rep 14(1):7739 . doi: 10.1038/s41598-024-58285-3
Publication date: April 2, 2024
PMID: 38565869
Probing the CRL4DCAF12 interactions with MAGEA3 and CCT5 di-Glu C-terminal degrons.
Righetto GL, Yin Y, Duda DM, Vu V, Szewczyk MM, Zeng H, Li Y, Loppnau P, Mei T, Li YY, Seitova A, Patrick AN, Brazeau JF, Chaudhry C, Barsyte-Lovejoy D, Santhakumar V, Halabelian L
PNAS Nexus 3(4):pgae153 . doi: 10.1093/pnasnexus/pgae153
Publication date: April 1, 2024
PMID: 38665159
Loss-of-function mutation in PRMT9 causes abnormal synapse development by dysregulation of RNA alternative splicing.
Shen L, Ma X, Wang Y, Wang Z, Zhang Y, Pham HQH, Tao X, Cui Y, Wei J, Lin D, Abeywanada T, Hardikar S, Halabelian L, Smith N, Chen T, Barsyte-Lovejoy D, Qiu S, Xing Y, Yang Y
Nat Commun 15(1):2809 . doi: 10.1038/s41467-024-47107-9
Publication date: April 1, 2024
PMID: 38561334

March 2024

Discovery of a Potent, Selective, and Cell-Active SPIN1 Inhibitor.
Xiong Y, Greschik H, Johansson C, Seifert L, Gamble V, Park KS, Fagan V, Li F, Chau I, Vedadi M, Arrowsmith CH, Brennan P, Fedorov O, Jung M, Farnie G, Liu J, Oppermann U, Schüle R, Jin J
J Med Chem . doi: 10.1021/acs.jmedchem.4c00121
Publication date: March 27, 2024
PMID: 38533580
Chemical tools for the Gid4 subunit of the human E3 ligase C-terminal to LisH (CTLH) degradation complex.
Yazdi AK, Perveen S, Dong C, Song X, Dong A, Szewczyk MM, Calabrese MF, Casimiro-Garcia A, Chakrapani S, Dowling MS, Ficici E, Lee J, Montgomery JI, O'Connell TN, Skrzypek GJ, Tran TP, Troutman MD, Wang F, Young JA, Min J, Barsyte-Lovejoy D, Brown PJ, Santhakumar V, Arrowsmith CH, Vedadi M, Owen DR
RSC Med Chem 15(3):1066-1071 . doi: 10.1039/d3md00633f
Publication date: March 20, 2024
PMID: 38516600
Discovery of Conformationally Constrained ALK2 Inhibitors.
González-Álvarez H, Ensan D, Xin T, Wong JF, Zepeda-Velázquez CA, Cros J, Hoffer L, Kiyota T, Wilson BJ, Aman A, Roberts O, Isaac MB, Bullock AN, Smil D, Al-Awar R
J Med Chem . doi: 10.1021/acs.jmedchem.3c02308
Publication date: March 18, 2024
PMID: 38498998
Discovery of the sEH Inhibitor Epoxykynin as a Potent Kynurenine Pathway Modulator.
Dötsch L, Davies C, Hennes E, Schönfeld J, Kumar A, Guita CDCL, Ehrler JHM, Hiesinger K, Thavam S, Janning P, Sievers S, Knapp S, Proschak E, Ziegler S, Waldmann H
J Med Chem . doi: 10.1021/acs.jmedchem.3c02245
Publication date: March 12, 2024
PMID: 38470246
Big data and benchmarking initiatives to bridge the gap from AlphaFold to drug design.
Schapira M, Halabelian L, Arrowsmith CH, Harding RJ
Nat Chem Biol . doi: 10.1038/s41589-024-01570-z
Publication date: March 8, 2024
PMID: 38459278
Tom20 gates PINK1 activity and mediates its tethering of the TOM and TIM23 translocases upon mitochondrial stress.
Eldeeb MA, Bayne AN, Fallahi A, Goiran T, MacDougall EJ, Soumbasis A, Zorca CE, Tabah JJ, Thomas RA, Karpilovsky N, Mathur M, Durcan TM, Trempe JF, Fon EA
Proc Natl Acad Sci U S A 121(10):e2313540121 . doi: 10.1073/pnas.2313540121
Publication date: March 5, 2024
PMID: 38416681
Structure-guided drug discovery: back to the future.
Arrowsmith CH
Nat Struct Mol Biol 31(3):395-396 . doi: 10.1038/s41594-024-01244-3
Publication date: March 1, 2024
PMID: 38486110

February 2024

Development of Selective Pyrido[2,3-d]pyrimidin-7(8H)-one-Based Mammalian STE20-Like (MST3/4) Kinase Inhibitors.
Rak M, Menge A, Tesch R, Berger LM, Balourdas DI, Shevchenko E, Krämer A, Elson L, Berger BT, Abdi I, Wahl LM, Poso A, Kaiser A, Hanke T, Kronenberger T, Joerger AC, Müller S, Knapp S
J Med Chem . doi: 10.1021/acs.jmedchem.3c02217
Publication date: February 29, 2024
PMID: 38422480
Synthesis of 5-Benzylamino and 5-Alkylamino-Substituted Pyrimido[4,5-c]quinoline Derivatives as CSNK2A Inhibitors with Antiviral Activity.
Asressu KH, Smith JL, Dickmander RJ, Moorman NJ, Wellnitz J, Popov KI, Axtman AD, Willson TM
Pharmaceuticals (Basel) 17(3): . doi: 10.3390/ph17030306
Publication date: February 27, 2024
PMID: 38543092
Kinetic characterization of human mRNA guanine-N7 methyltransferase.
Perveen S, Yazdi AK, Hajian T, Li F, Vedadi M
Sci Rep 14(1):4509 . doi: 10.1038/s41598-024-55184-5
Publication date: February 24, 2024
PMID: 38402266
Structure-Activity Relationship of a Pyrrole Based Series of PfPKG Inhibitors as Anti-Malarials.
Gilleran JA, Ashraf K, Delvillar M, Eck T, Fondekar R, Miller EB, Hutchinson A, Dong A, Seitova A, De Souza ML, Augeri D, Halabelian L, Siekierka J, Rotella DP, Gordon J, Childers WE, Grier MC, Staker BL, Roberge JY, Bhanot P
J Med Chem . doi: 10.1021/acs.jmedchem.3c01795
Publication date: February 19, 2024
PMID: 38372781
Back-pocket optimization of 2-aminopyrimidine-based macrocycles leads to potent dual EPHA2/GAK kinase inhibitors with antiviral activity.
Gerninghaus J, Zhubi R, Kraemer A, Karim M, Tran DHN, Joerger AC, Schreiber C, Berger LM, Berger BT, Ehret TAL, Elson L, Lenz C, Saxena K, Mueller S, Einav S, Knapp S, Hanke T
bioRxiv . doi: 10.1101/2024.02.18.580805
Publication date: February 18, 2024
PMID: 38405908
Discovery of a Small Molecule Activator of Slack (Kcnt1) Potassium Channels That Significantly Reduces Scratching in Mouse Models of Histamine-Independent and Chronic Itch.
Balzulat A, Zhu WF, Flauaus C, Hernandez-Olmos V, Heering J, Sethumadhavan S, Dubiel M, Frank A, Menge A, Hebchen M, Metzner K, Lu R, Lukowski R, Ruth P, Knapp S, Müller S, Steinhilber D, Hänelt I, Stark H, Proschak E, Schmidtko A
Adv Sci (Weinh) e2307237 . doi: 10.1002/advs.202307237
Publication date: February 13, 2024
PMID: 38350720
Photosensitization enables Pauson-Khand-type reactions with nitrenes.
Li F, Zhu WF, Empel C, Datsenko O, Kumar A, Xu Y, Ehrler JHM, Atodiresei I, Knapp S, Mykhailiuk PK, Proschak E, Koenigs RM
Science 383(6682):498-503 . doi: 10.1126/science.adm8095
Publication date: February 2, 2024
PMID: 38301027

January 2024

Development of Potent Dual BET/HDAC Inhibitors via Pharmacophore Merging and Structure-Guided Optimization.
Bauer N, Balourdas DI, Schneider JR, Zhang X, Berger LM, Berger BT, Schwalm MP, Klopp NA, Siveke JT, Knapp S, Joerger AC
ACS Chem Biol . doi: 10.1021/acschembio.3c00427
Publication date: January 31, 2024
PMID: 38291964
ChemRAP uncovers specific mRNA translation regulation via RNA 5' phospho-methylation.
Ipas H, Gouws EB, Abell NS, Chiou PC, Devanathan SK, Hervé S, Lee S, Mercado M, Reinsborough C, Halabelian L, Arrowsmith CH, Xhemalçe B
EMBO Rep . doi: 10.1038/s44319-024-00059-z
Publication date: January 23, 2024
PMID: 38263329
Small Molecule Screen Identifies Non-catalytic USP3 Chemical Handle.
Mann MK, Wolf E, Silva M, Kwak HA, Wilson B, Bolotokova A, Wilson DJ, Harding RJ, Schapira M
ACS Omega 9(1):917-924 . doi: 10.1021/acsomega.3c07070
Publication date: January 9, 2024
PMID: 38222562
Identification of 4-(6-((2-methoxyphenyl)amino)pyrazin-2-yl)benzoic acids as CSNK2A inhibitors with antiviral activity and improved selectivity over PIM3.
Galal KA, Krämer A, Strickland BG, Smith JL, Dickmander RJ, Moorman NJ, Willson TM
Bioorg Med Chem Lett 99:129617 . doi: 10.1016/j.bmcl.2024.129617
Publication date: January 8, 2024
PMID: 38199328
2023

December 2023

Atg8 family proteins, LIR/AIM motifs and other interaction modes.
Rogov VV, Nezis IP, Tsapras P, Zhang H, Dagdas Y, Noda NN, Nakatogawa H, Wirth M, Mouilleron S, McEwan DG, Behrends C, Deretic V, Elazar Z, Tooze SA, Dikic I, Lamark T, Johansen T
Autophagy Rep 2(1): . doi: 10.1080/27694127.2023.2188523
Publication date: December 31, 2023
PMID: 38214012
Synthesis of Pyrazole-Based Macrocycles Leads to a Highly Selective Inhibitor for MST3.
Amrhein JA, Berger LM, Balourdas DI, Joerger AC, Menge A, Krämer A, Frischkorn JM, Berger BT, Elson L, Kaiser A, Schubert-Zsilavecz M, Müller S, Knapp S, Hanke T
J Med Chem . doi: 10.1021/acs.jmedchem.3c01980
Publication date: December 21, 2023
PMID: 38126712

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