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Publications
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Displaying 1 - 50 of 2427
2024
March 2024
Identification of high-performing antibodies for Superoxide dismutase [Cu-Zn] 1 (SOD1) for use in Western blot, immunoprecipitation, and immunofluorescence.
Ayoubi R, Alshafie W, You Z, Southern K, McPherson PS, Laflamme C
F1000Res 12:391 . doi: 10.12688/f1000research.132952.1
Publication date: March 15, 2024
PMID: 37860271
F1000Res 12:391 . doi: 10.12688/f1000research.132952.1
Publication date: March 15, 2024
PMID: 37860271
The identification of high-performing antibodies for Coiled-coil-helix-coiled-coil-helix domain containing protein 10 (CHCHD10) for use in Western Blot, immunoprecipitation and immunofluorescence.
Ayoubi R, Alshafie W, Southern K, McPherson PS, Laflamme C
F1000Res 12:403 . doi: 10.12688/f1000research.133479.2
Publication date: March 15, 2024
PMID: 37767023
F1000Res 12:403 . doi: 10.12688/f1000research.133479.2
Publication date: March 15, 2024
PMID: 37767023
Identification of high-performing antibodies for Vacuolar protein sorting-associated protein 35 (hVPS35) for use in Western Blot, immunoprecipitation and immunofluorescence.
Ayoubi R, Fotouhi M, Southern K, McPherson PS, Laflamme C
F1000Res 12:452 . doi: 10.12688/f1000research.133696.2
Publication date: March 15, 2024
PMID: 38434631
F1000Res 12:452 . doi: 10.12688/f1000research.133696.2
Publication date: March 15, 2024
PMID: 38434631
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: March 15, 2024
PMID: 37635943
F1000Res 12:884 . doi: 10.12688/f1000research.139755.1
Publication date: March 15, 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: March 15, 2024
PMID: 37576538
F1000Res 12:348 . doi: 10.12688/f1000research.132249.1
Publication date: March 15, 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: March 15, 2024
PMID: 37384305
F1000Res 12:376 . doi: 10.12688/f1000research.133220.2
Publication date: March 15, 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: March 15, 2024
PMID: 37359785
F1000Res 12:277 . doi: 10.12688/f1000research.131852.2
Publication date: March 15, 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: March 15, 2024
PMID: 37359784
F1000Res 12:355 . doi: 10.12688/f1000research.131851.1
Publication date: March 15, 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: March 15, 2024
PMID: 38359047
PLoS One 19(2):e0293548 . doi: 10.1371/journal.pone.0293548
Publication date: March 15, 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: March 15, 2024
PMID: 38106655
F1000Res 12:172 . doi: 10.12688/f1000research.130126.3
Publication date: March 15, 2024
PMID: 38106655
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
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
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
Proc Natl Acad Sci U S A 121(10):e2313540121 . doi: 10.1073/pnas.2313540121
Publication date: March 5, 2024
PMID: 38416681
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
J Med Chem . doi: 10.1021/acs.jmedchem.3c02217
Publication date: February 29, 2024
PMID: 38422480
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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 Ã, Dierssen M, Krämer A, Knapp S, Meijer L
J Med Chem . doi: 10.1021/acs.jmedchem.3c01888
Publication date: December 5, 2023
PMID: 38051674
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
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
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
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
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
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
J Med Chem . doi: 10.1021/acs.jmedchem.3c01471
Publication date: November 23, 2023
PMID: 37996079
Scaling of an antibody validation procedure enables quantification of antibody performance in major research applications.
Ayoubi R, Ryan J, Biddle MS, Alshafie W, Fotouhi M, Bolivar SG, Ruiz Moleon V, Eckmann P, Worrall D, McDowell I, Southern K, Reintsch W, Durcan TM, Brown C, Bandrowski A, Virk H, Edwards AM, McPherson P, Laflamme C
Elife 12: . doi: 10.7554/eLife.91645
Publication date: November 23, 2023
PMID: 37995198
Elife 12: . doi: 10.7554/eLife.91645
Publication date: November 23, 2023
PMID: 37995198
An atypical GABARAP binding module drives the pro-autophagic potential of the AML-associated NPM1c variant.
Mende H, Khatri A, Lange C, Poveda-Cuevas SA, Tascher G, Covarrubias-Pinto A, Löhr F, Koschade SE, Dikic I, Münch C, Bremm A, Brunetti L, Brandts CH, Uckelmann H, Dötsch V, Rogov VV, Bhaskara RM, Müller S
Cell Rep 42(12):113484 . doi: 10.1016/j.celrep.2023.113484
Publication date: November 22, 2023
PMID: 37999976
Cell Rep 42(12):113484 . doi: 10.1016/j.celrep.2023.113484
Publication date: November 22, 2023
PMID: 37999976
Open Source Antibiotics: Simple Diarylimidazoles Are Potent against Methicillin-Resistant Staphylococcus aureus.
Klug DM, Tse EG, Silva DG, Cao Y, Charman SA, Chauhan J, Crighton E, Dichiara M, Drake C, Drewry D, da Silva Emery F, Ferrins L, Graves L, Hopkins E, Kresina TAC, Lorente-MacÃas Ã, Perry B, Phipps R, Quiroga B, Quotadamo A, Sabatino GN, Sama A, Schätzlein A, Simpson QJ, Steele J, Shanu-Wilson J, Sjö P, Stapleton P, Swain CJ, Vaideanu A, Xie H, Zuercher W, Todd MH
ACS Infect Dis . doi: 10.1021/acsinfecdis.3c00286
Publication date: November 22, 2023
PMID: 37991879
ACS Infect Dis . doi: 10.1021/acsinfecdis.3c00286
Publication date: November 22, 2023
PMID: 37991879
From cultivation to cancer: formation of N-nitrosamines and other carcinogens in smokeless tobacco and their mutagenic implications.
Stanfill SB, Hecht SS, Joerger AC, González PJ, Maia LB, Rivas MG, Moura JJG, Gupta AK, Le Brun NE, Crack JC, Hainaut P, Sparacino-Watkins C, Tyx RE, Pillai SD, Zaatari GS, Henley SJ, Blount BC, Watson CH, Kaina B, Mehrotra R
Crit Rev Toxicol 1-44 . doi: 10.1080/10408444.2023.2264327
Publication date: November 21, 2023
PMID: 38050998
Crit Rev Toxicol 1-44 . doi: 10.1080/10408444.2023.2264327
Publication date: November 21, 2023
PMID: 38050998
The PB1 and the ZZ domain of the autophagy receptor p62/SQSTM1 regulate the interaction of p62/SQSTM1 with the autophagosome protein LC3B.
Alcober-Boquet L, Zang T, Pietsch L, Suess E, Hartmann M, Proschak E, Gross LZF, Sacerdoti M, Zeuzem S, Rogov VV, Leroux AE, Piiper A, Biondi RM
Protein Sci e4840 . doi: 10.1002/pro.4840
Publication date: November 20, 2023
PMID: 37984441
Protein Sci e4840 . doi: 10.1002/pro.4840
Publication date: November 20, 2023
PMID: 37984441
Open science discovery of potent noncovalent SARS-CoV-2 main protease inhibitors.
Boby ML, Fearon D, Ferla M, Filep M, Koekemoer L, Robinson MC, Chodera JD, Lee AA, London N, von Delft A, von Delft F, Achdout H, Aimon A, Alonzi DS, Arbon R, Aschenbrenner JC, Balcomb BH, Bar-David E, Barr H, Ben-Shmuel A, Bennett J, Bilenko VA, Borden B, Boulet P, Bowman GR, Brewitz L, Brun J, Bvnbs S, Calmiano M, Carbery A, Carney DW, Cattermole E, Chang E, Chernyshenko E, Clyde A, Coffland JE, Cohen G, Cole JC, Contini A, Cox L, Croll TI, Cvitkovic M, De Jonghe S, Dias A, Donckers K, Dotson DL, Douangamath A, Duberstein S, Dudgeon T, Dunnett LE, Eastman P, Erez N, Eyermann CJ, Fairhead M, Fate G, Fedorov O, Fernandes RS, Ferrins L, Foster R, Foster H, Fraisse L, Gabizon R, García-Sastre A, Gawriljuk VO, Gehrtz P, Gileadi C, Giroud C, Glass WG, Glen RC, Glinert I, Godoy AS, Gorichko M, Gorrie-Stone T, Griffen EJ, Haneef A, Hassell Hart S, Heer J, Henry M, Hill M, Horrell S, Huang QYJ, Huliak VD, Hurley MFD, Israely T, Jajack A, Jansen J, Jnoff E, Jochmans D, John T, Kaminow B, Kang L, Kantsadi AL, Kenny PW, Kiappes JL, Kinakh SO, Kovar B, Krojer T, La VNT, Laghnimi-Hahn S, Lefker BA, Levy H, Lithgo RM, Logvinenko IG, Lukacik P, Macdonald HB, MacLean EM, Makower LL, Malla TR, Marples PG, Matviiuk T, McCorkindale W, McGovern BL, Melamed S, Melnykov KP, Michurin O, Miesen P, Mikolajek H, Milne BF, Minh D, Morris A, Morris GM, Morwitzer MJ, Moustakas D, Mowbray CE, Nakamura AM, Neto JB, Neyts J, Nguyen L, Noske GD, Oleinikovas V, Oliva G, Overheul GJ, Owen CD, Pai R, Pan J, Paran N, Payne AM, Perry B, Pingle M, Pinjari J, Politi B, Powell A, Pšenák V, Pulido I, Puni R, Rangel VL, Reddi RN, Rees P, Reid SP, Reid L, Resnick E, Ripka EG, Robinson RP, Rodriguez-Guerra J, Rosales R, Rufa DA, Saar K, Saikatendu KS, Salah E, Schaller D, Scheen J, Schiffer CA, Schofield CJ, Shafeev M, Shaikh A, Shaqra AM, Shi J, Shurrush K, Singh S, Sittner A, Sjö P, Skyner R, Smalley A, Smeets B, Smilova MD, Solmesky LJ, Spencer J, Strain-Damerell C, Swamy V, Tamir H, Taylor JC, Tennant RE, Thompson W, Thompson A, Tomásio S, Tomlinson CWE, Tsurupa IS, Tumber A, Vakonakis I, van Rij RP, Vangeel L, Varghese FS, Vaschetto M, Vitner EB, Voelz V, Volkamer A, Walsh MA, Ward W, Weatherall C, Weiss S, White KM, Wild CF, Witt KD, Wittmann M, Wright N, Yahalom-Ronen Y, Yilmaz NK, Zaidmann D, Zhang I, Zidane H, Zitzmann N, Zvornicanin SN
Science 382(6671):eabo7201 . doi: 10.1126/science.abo7201
Publication date: November 10, 2023
PMID: 37943932
Science 382(6671):eabo7201 . doi: 10.1126/science.abo7201
Publication date: November 10, 2023
PMID: 37943932
October 2023
Chemical proteomics reveals the target landscape of 1,000 kinase inhibitors.
Reinecke M, Brear P, Vornholz L, Berger BT, Seefried F, Wilhelm S, Samaras P, Gyenis L, Litchfield DW, Médard G, Müller S, Ruland J, Hyvönen M, Wilhelm M, Kuster B
Nat Chem Biol . doi: 10.1038/s41589-023-01459-3
Publication date: October 30, 2023
PMID: 37904048
Nat Chem Biol . doi: 10.1038/s41589-023-01459-3
Publication date: October 30, 2023
PMID: 37904048
Optimization of 3-Cyano-7-cyclopropylamino-pyrazolo[1,5-a]pyrimidines toward the Development of an In Vivo Chemical Probe for CSNK2A.
Yang X, Ong HW, Dickmander RJ, Smith JL, Brown JW, Tao W, Chang E, Moorman NJ, Axtman AD, Willson TM
ACS Omega 8(42):39546-39561 . doi: 10.1021/acsomega.3c05377
Publication date: October 24, 2023
PMID: 37901516
ACS Omega 8(42):39546-39561 . doi: 10.1021/acsomega.3c05377
Publication date: October 24, 2023
PMID: 37901516
Fused Tetrahydroquinolines Are Interfering with Your Assay.
Bashore FM, Annor-Gyamfi J, Du Y, Katis V, Nwogbo F, Flax RG, Frye SV, Pearce KH, Fu H, Willson TM, Drewry DH, Axtman AD
J Med Chem . doi: 10.1021/acs.jmedchem.3c01277
Publication date: October 24, 2023
PMID: 37874947
J Med Chem . doi: 10.1021/acs.jmedchem.3c01277
Publication date: October 24, 2023
PMID: 37874947
Wnt/β-catenin and NFκB signaling synergize to trigger growth-factor-free regeneration of adult primary human hepatocytes.
Oliva-Vilarnau N, Beusch CM, Sabatier P, Sakaraki E, Tjaden A, Graetz L, Büttner FA, Dorotea D, Nguyen M, Bergqvist F, Sundström Y, Müller S, Zubarev RA, Schulte G, Tredup C, Gramignoli R, Tietge UJF, Lauschke VM
Hepatology . doi: 10.1097/HEP.0000000000000648
Publication date: October 23, 2023
PMID: 37870288
Hepatology . doi: 10.1097/HEP.0000000000000648
Publication date: October 23, 2023
PMID: 37870288
Dual Inhibition of Mycobacterium tuberculosis and the Host TGFBR1 by an Anilinoquinazoline.
Nandakumar M, Ollodart A, Fleck N, Kapadia NR, Frando A, Boradia V, Smith JL, Chen J, Zuercher WJ, Willson TM, Grundner C
J Med Chem . doi: 10.1021/acs.jmedchem.3c01273
Publication date: October 23, 2023
PMID: 37871287
J Med Chem . doi: 10.1021/acs.jmedchem.3c01273
Publication date: October 23, 2023
PMID: 37871287
Discovery of FERM domain protein-protein interaction inhibitors for MSN and CD44 as a potential therapeutic approach for Alzheimer's disease.
Du Y, Bradshaw WJ, Leisner TM, Annor-Gyamfi JK, Qian K, Bashore FM, Sikdar A, Nwogbo FO, Ivanov AA, Frye SV, Gileadi O, Brennan PE, Levey AI, Axtman AD, Pearce KH, Fu H, Katis VL
J Biol Chem 105382 . doi: 10.1016/j.jbc.2023.105382
Publication date: October 20, 2023
PMID: 37866628
J Biol Chem 105382 . doi: 10.1016/j.jbc.2023.105382
Publication date: October 20, 2023
PMID: 37866628
Methods for computer-assisted PROTAC design.
Rovers E, Schapira M
Methods Enzymol 690:311-340 . doi: 10.1016/bs.mie.2023.06.020
Publication date: October 20, 2023
PMID: 37858533
Methods Enzymol 690:311-340 . doi: 10.1016/bs.mie.2023.06.020
Publication date: October 20, 2023
PMID: 37858533