Publications

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Displaying 1 - 50 of 2440

2024

April 2024

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: April 19, 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: April 19, 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: April 19, 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: April 19, 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: April 19, 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: April 19, 2024
PMID: 38106655
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: April 19, 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: April 19, 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: April 19, 2024
PMID: 37384305
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
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
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
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
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
Discovery of pyrazolo[3,4-d]pyrimidines as novel mitogen-activated protein kinase kinase 3 (MKK3) inhibitors.
Takarada JE, Cunha MR, Almeida VM, Vasconcelos SNS, Santiago AS, Godoi PH, Salmazo A, Ramos PZ, Fala AM, de Souza LR, Da Silva IEP, Bengtson MH, Massirer KB, Couñago RM
Bioorg Med Chem 98:117561 . doi: 10.1016/j.bmc.2023.117561
Publication date: December 20, 2023
PMID: 38157838
The co-crystal structure of Cbl-b and a small-molecule inhibitor reveals the mechanism of Cbl-b inhibition.
Kimani SW, Perveen S, Szewezyk M, Zeng H, Dong A, Li F, Ghiabi P, Li Y, Chau I, Arrowsmith CH, Barsyte-Lovejoy D, Santhakumar V, Vedadi M, Halabelian L
Commun Biol 6(1):1272 . doi: 10.1038/s42003-023-05655-8
Publication date: December 16, 2023
PMID: 38104184
Characterization of 2,4-Dianilinopyrimidines Against Five P. falciparum Kinases PfARK1, PfARK3, PfNEK3, PfPK9, and PfPKB.
Ong HW, de Silva C, Avalani K, Kwarcinski F, Mansfield CR, Chirgwin M, Truong A, Derbyshire ER, Zutshi R, Drewry DH
ACS Med Chem Lett 14(12):1774-1784 . doi: 10.1021/acsmedchemlett.3c00354
Publication date: December 14, 2023
PMID: 38116430
Development of HC-258, a Covalent Acrylamide TEAD Inhibitor That Reduces Gene Expression and Cell Migration.
Fnaiche A, Chan HC, Paquin A, González Suárez N, Vu V, Li F, Allali-Hassani A, Cao MA, Szewczyk MM, Bolotokova A, Allemand F, Gelin M, Barsyte-Lovejoy D, Santhakumar V, Vedadi M, Guichou JF, Annabi B, Gagnon A
ACS Med Chem Lett 14(12):1746-1753 . doi: 10.1021/acsmedchemlett.3c00386
Publication date: December 14, 2023
PMID: 38116405
Epigenetic vulnerabilities of leukemia harboring inactivating EZH2 mutations.
Alqazzaz MA, Luciani GM, Vu V, Machado RAC, Szewczyk MM, Adamson EC, Cheon S, Li F, Arrowsmith CH, Minden MD, Barsyte-Lovejoy D
Exp Hematol 104135 . doi: 10.1016/j.exphem.2023.11.009
Publication date: December 10, 2023
PMID: 38072134
Chemical, Biochemical, Cellular, and Physiological Characterization of Leucettinib-21, a Down Syndrome and Alzheimer's Disease Drug Candidate.
Lindberg MF, Deau E, Miege F, Greverie M, Roche D, George N, George P, Merlet L, Gavard J, Brugman SJT, Aret E, Tinnemans P, de Gelder R, Sadownik J, Verhofstad E, Sleegers D, Santangelo S, Dairou J, Fernandez-Blanco Á, Dierssen M, Krämer A, Knapp S, Meijer L
J Med Chem . doi: 10.1021/acs.jmedchem.3c01888
Publication date: December 5, 2023
PMID: 38051674
Death by a thousand cuts through kinase inhibitor combinations that maximize selectivity and enable rational multitargeting.
Outhwaite IR, Singh S, Berger BT, Knapp S, Chodera JD, Seeliger MA
Elife 12: . doi: 10.7554/eLife.86189
Publication date: December 4, 2023
PMID: 38047771
A unique binding pocket induced by a noncanonical SAH mimic to develop potent and selective PRMT inhibitors.
Deng Y, Song X, Iyamu ID, Dong A, Min J, Huang R
Acta Pharm Sin B 13(12):4893-4905 . doi: 10.1016/j.apsb.2023.07.022
Publication date: December 4, 2023
PMID: 38045046
Synthesis and Biological Evaluation of 2-Substituted Quinazolin-4(3H)-Ones with Antiproliferative Activities.
Karelou M, Kampasis D, Kalampaliki AD, Persoons L, Krämer A, Schols D, Knapp S, De Jonghe S, Kostakis IK
Molecules 28(23): . doi: 10.3390/molecules28237912
Publication date: December 2, 2023
PMID: 38067641
Inhibition of Parkinson's disease-related LRRK2 by type I and type II kinase inhibitors: Activity and structures.
Sanz Murillo M, Villagran Suarez A, Dederer V, Chatterjee D, Alegrio Louro J, Knapp S, Mathea S, Leschziner AE
Sci Adv 9(48):eadk6191 . doi: 10.1126/sciadv.adk6191
Publication date: December 1, 2023
PMID: 38039358

November 2023

SGC-CLK-1: A chemical probe for the Cdc2-like kinases CLK1, CLK2, and CLK4.
Tiek D, Wells CI, Schröder M, Song X, Alamillo-Ferrer C, Goenka A, Iglesia R, Lu M, Hu B, Kwarcinski F, Sintha P, de Silva C, Hossain MA, Picado A, Zuercher W, Zutshi R, Knapp S, Riggins RB, Cheng SY, Drewry DH
Curr Res Chem Biol 3: . doi: 10.1016/j.crchbi.2023.100045
Publication date: November 27, 2023
PMID: 38009092
Discovery of a First-in-Class Small-Molecule Ligand for WDR91 Using DNA-Encoded Chemical Library Selection Followed by Machine Learning.
Ahmad S, Xu J, Feng JA, Hutchinson A, Zeng H, Ghiabi P, Dong A, Centrella PA, Clark MA, Guié MA, Guilinger JP, Keefe AD, Zhang Y, Cerruti T, Cuozzo JW, von Rechenberg M, Bolotokova A, Li Y, Loppnau P, Seitova A, Li YY, Santhakumar V, Brown PJ, Ackloo S, Halabelian L
J Med Chem . doi: 10.1021/acs.jmedchem.3c01471
Publication date: November 23, 2023
PMID: 37996079

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