Publications

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Displaying 101 - 150 of 2418

2023

March 2023

Discovery of a Potent and Selective Targeted NSD2 Degrader for the Reduction of H3K36me2.
Hanley RP, Nie DY, Tabor JR, Li F, Sobh A, Xu C, Barker NK, Dilworth D, Hajian T, Gibson E, Szewczyk MM, Brown PJ, Barsyte-Lovejoy D, Herring LE, Wang GG, Licht JD, Vedadi M, Arrowsmith CH, James LI
J Am Chem Soc . doi: 10.1021/jacs.3c01421
Publication date: March 28, 2023
PMID: 36976643
Development of Cell Permeable NanoBRET Probes for the Measurement of PLK1 Target Engagement in Live Cells.
Yang X, Smith JL, Beck MT, Wilkinson JM, Michaud A, Vasta JD, Robers MB, Willson TM
Molecules 28(7): . doi: 10.3390/molecules28072950
Publication date: March 25, 2023
PMID: 37049713
Discovery of Nanomolar DCAF1 Small Molecule Ligands.
Li ASM, Kimani S, Wilson B, Noureldin M, González-Álvarez H, Mamai A, Hoffer L, Guilinger JP, Zhang Y, von Rechenberg M, Disch JS, Mulhern CJ, Slakman BL, Cuozzo JW, Dong A, Poda G, Mohammed M, Saraon P, Mittal M, Modh P, Rathod V, Patel B, Ackloo S, Santhakumar V, Szewczyk MM, Barsyte-Lovejoy D, Arrowsmith CH, Marcellus R, Guié MA, Keefe AD, Brown PJ, Halabelian L, Al-Awar R, Vedadi M
J Med Chem . doi: 10.1021/acs.jmedchem.2c02132
Publication date: March 22, 2023
PMID: 36948210
Deep Annotation of Donated Chemical Probes (DCP) in Organotypic Human Liver Cultures and Patient-Derived Organoids from Tumor and Normal Colorectum.
Tredup C, Ndreshkjana B, Schneider NS, Tjaden A, Kemas AM, Youhanna S, Lauschke VM, Berger BT, Krämer A, Berger LM, Röhm S, Knapp S, Farin HF, Müller S
ACS Chem Biol . doi: 10.1021/acschembio.2c00877
Publication date: March 21, 2023
PMID: 36944371
Reference compounds for characterizing cellular injury in high-content cellular morphology assays.
Dahlin JL, Hua BK, Zucconi BE, Nelson SD, Singh S, Carpenter AE, Shrimp JH, Lima-Fernandes E, Wawer MJ, Chung LPW, Agrawal A, O'Reilly M, Barsyte-Lovejoy D, Szewczyk M, Li F, Lak P, Cuellar M, Cole PA, Meier JL, Thomas T, Baell JB, Brown PJ, Walters MA, Clemons PA, Schreiber SL, Wagner BK
Nat Commun 14(1):1364 . doi: 10.1038/s41467-023-36829-x
Publication date: March 13, 2023
PMID: 36914634
Chemistry-led investigations into the mode of action of NAMPT activators, resulting in the discovery of non-pyridyl class NAMPT activators.
Tang S, Garzon Sanz M, Smith O, Krämer A, Egbase D, Caton PW, Knapp S, Butterworth S
Acta Pharm Sin B 13(2):709-721 . doi: 10.1016/j.apsb.2022.07.016
Publication date: March 7, 2023
PMID: 36873168
Oxazolo[5,4-f]quinoxaline-type selective inhibitors of glycogen synthase kinase-3α (GSK-3α): Development and impact on temozolomide treatment of glioblastoma cells.
Hasyeoui M, Lassagne F, Erb W, Nael M, Elokely KM, Chaikuad A, Knapp S, Jorda A, Vallés SL, Quissac E, Verreault M, Robert T, Bach S, Samarat A, Mongin F
Bioorg Chem 134:106456 . doi: 10.1016/j.bioorg.2023.106456
Publication date: March 4, 2023
PMID: 36913879
RAS and PP2A activities converge on epigenetic gene regulation.
Aakula A, Sharma M, Tabaro F, Nätkin R, Kamila J, Honkanen H, Schapira M, Arrowsmith C, Nykter M, Westermarck J
Life Sci Alliance 6(5): . doi: 10.26508/lsa.202301928
Publication date: March 2, 2023
PMID: 36858798

February 2023

Design, synthesis and characterisation of a novel type II B-RAF paradox breaker inhibitor.
Arora R, Linders JTM, Aci-Sèche S, Verheyen T, Van Heerde E, Brehmer D, Chaikuad A, Knapp S, Bonnet P
Eur J Med Chem 250:115231 . doi: 10.1016/j.ejmech.2023.115231
Publication date: February 25, 2023
PMID: 36878151
Histone H4K20 monomethylation enables recombinant nucleosome methylation by PRMT1 in vitro.
Li ASM, Homsi C, Bonneil E, Thibault P, Verreault A, Vedadi M
Biochim Biophys Acta Gene Regul Mech 194922 . doi: 10.1016/j.bbagrm.2023.194922
Publication date: February 21, 2023
PMID: 36822575
Discovery and Characterization of BAY-805, a Potent and Selective Inhibitor of Ubiquitin-Specific Protease USP21.
Göricke F, Vu V, Smith L, Scheib U, Böhm R, Akkilic N, Wohlfahrt G, Weiske J, Bömer U, Brzezinka K, Lindner N, Lienau P, Gradl S, Beck H, Brown PJ, Santhakumar V, Vedadi M, Barsyte-Lovejoy D, Arrowsmith CH, Schmees N, Petersen K
J Med Chem . doi: 10.1021/acs.jmedchem.2c01933
Publication date: February 20, 2023
PMID: 36802665
Discovery and Development Strategies for SARS-CoV-2 NSP3 Macrodomain Inhibitors.
Schuller M, Zarganes-Tzitzikas T, Bennett J, De Cesco S, Fearon D, von Delft F, Fedorov O, Brennan PE, Ahel I
Pathogens 12(2): . doi: 10.3390/pathogens12020324
Publication date: February 15, 2023
PMID: 36839595
Toward effective Atg8-based ATTECs: Approaches and perspectives.
Schwalm MP, Knapp S, Rogov VV
J Cell Biochem . doi: 10.1002/jcb.30380
Publication date: February 13, 2023
PMID: 36780422
SS148 and WZ16 inhibit the activities of nsp10-nsp16 complexes from all seven human pathogenic coronaviruses.
Li F, Ghiabi P, Hajian T, Klima M, Li ASM, Yazdi AK, Chau I, Loppnau P, Kutera M, Seitova A, Bolotokova A, Hutchinson A, Perveen S, Boura E, Vedadi M
Biochim Biophys Acta Gen Subj 130319 . doi: 10.1016/j.bbagen.2023.130319
Publication date: February 8, 2023
PMID: 36764586
Antecedent chromatin organization determines cGAS recruitment to ruptured micronuclei.
MacDonald KM, Nicholson-Puthenveedu S, Tageldein MM, Khasnis S, Arrowsmith CH, Harding SM
Nat Commun 14(1):556 . doi: 10.1038/s41467-023-36195-8
Publication date: February 2, 2023
PMID: 36732527

January 2023

Studying Protein Arginine Methylation: Approaches and Methods.
Barsyte-Lovejoy D
J Vis Exp . doi: 10.3791/64821
Publication date: January 20, 2023
PMID: 37602846
Iterative computational design and crystallographic screening identifies potent inhibitors targeting the Nsp3 macrodomain of SARS-CoV-2.
Gahbauer S, Correy GJ, Schuller M, Ferla MP, Doruk YU, Rachman M, Wu T, Diolaiti M, Wang S, Neitz RJ, Fearon D, Radchenko DS, Moroz YS, Irwin JJ, Renslo AR, Taylor JC, Gestwicki JE, von Delft F, Ashworth A, Ahel I, Shoichet BK, Fraser JS
Proc Natl Acad Sci U S A 120(2):e2212931120 . doi: 10.1073/pnas.2212931120
Publication date: January 10, 2023
PMID: 36598939
2022

December 2022

Discovery of potent Plasmodium falciparum protein kinase 6 (PfPK6) inhibitors with a type II inhibitor pharmacophore.
Ong HW, Truong A, Kwarcinski F, de Silva C, Avalani K, Havener TM, Chirgwin M, Galal KA, Willis C, Krämer A, Liu S, Knapp S, Derbyshire ER, Zutshi R, Drewry DH
Eur J Med Chem 249:115043 . doi: 10.1016/j.ejmech.2022.115043
Publication date: December 30, 2022
PMID: 36736152
Systematic Design of Adenosine Analogs as Inhibitors of a Clostridioides difficile-Specific DNA Adenine Methyltransferase Required for Normal Sporulation and Persistence.
Zhou J, Horton JR, Menna M, Fiorentino F, Ren R, Yu D, Hajian T, Vedadi M, Mazzoccanti G, Ciogli A, Weinhold E, Hüben M, Blumenthal RM, Zhang X, Mai A, Rotili D, Cheng X
J Med Chem . doi: 10.1021/acs.jmedchem.2c01789
Publication date: December 29, 2022
PMID: 36581322
Development of a Potent Cyclic Peptide Inhibitor of the nNOS/PSD-95 Interaction.
Balboa JR, Essig DJ, Ma S, Karer N, Clemmensen LS, Pedersen SW, Joerger AC, Knapp S, Østergaard S, Strømgaard K
J Med Chem . doi: 10.1021/acs.jmedchem.2c01803
Publication date: December 29, 2022
PMID: 36580549
Skeletal muscle metabolism and contraction performance regulation by teneurin C-terminal-associated peptide-1.
Hogg DW, Reid AL, Dodsworth TL, Chen Y, Reid RM, Xu M, Husic M, Biga PR, Slee A, Buck LT, Barsyte-Lovejoy D, Locke M, Lovejoy DA
Front Physiol 13:1031264 . doi: 10.3389/fphys.2022.1031264
Publication date: December 17, 2022
PMID: 36523555
High-content live-cell multiplex screen for chemogenomic compound annotation based on nuclear morphology.
Tjaden A, Giessmann RT, Knapp S, Schröder M, Müller S
STAR Protoc 3(4):101791 . doi: 10.1016/j.xpro.2022.101791
Publication date: December 16, 2022
PMID: 36317177
MSC-1186, a Highly Selective Pan-SRPK Inhibitor Based on an Exceptionally Decorated Benzimidazole-Pyrimidine Core.
Schröder M, Leiendecker M, Grädler U, Braun J, Blum A, Wanior M, Berger BT, Krämer A, Müller S, Esdar C, Knapp S, Heinrich T
J Med Chem . doi: 10.1021/acs.jmedchem.2c01705
Publication date: December 14, 2022
PMID: 36516476
The future of chemical probes is diversity.
Müller S, Frye S, Baell J
RSC Med Chem 13(12):1438 . doi: 10.1039/d2md90036j
Publication date: December 14, 2022
PMID: 36561071
Identification of highly specific antibodies for Serine/threonine-protein kinase TBK1 for use in immunoblot, immunoprecipitation and immunofluorescence.
Alshafie W, Fotouhi M, Shlaifer I, Ayoubi R, Edwards AM, Durcan TM, McPherson PS, Laflamme C
F1000Res 11:977 . doi: 10.12688/f1000research.124632.2
Publication date: December 7, 2022
PMID: 36415206
Autoantigenic properties of the aminoacyl tRNA synthetase family in idiopathic inflammatory myopathies.
Preger C, Notarnicola A, Hellström C, Wigren E, Fernandes-Cerqueira C, Kvarnström M, Wahren-Herlenius M, Idborg H, Lundberg IE, Persson H, Gräslund S, Jakobsson PJ
J Autoimmun 134:102951 . doi: 10.1016/j.jaut.2022.102951
Publication date: December 2, 2022
PMID: 36470210
An open source plant kinase chemogenomics set.
Ercoli MF, Ramos PZ, Jain R, Pilotte J, Dong OX, Thompson T, Wells CI, Elkins JM, Edwards AM, Couñago RM, Drewry DH, Ronald PC
Plant Direct 6(11):e460 . doi: 10.1002/pld3.460
Publication date: December 1, 2022
PMID: 36447653

November 2022

Discovery of 3-Amino-1H-pyrazole-Based Kinase Inhibitors to Illuminate the Understudied PCTAIRE Family.
Amrhein JA, Berger LM, Tjaden A, Krämer A, Elson L, Tolvanen T, Martinez-Molina D, Kaiser A, Schubert-Zsilavecz M, Müller S, Knapp S, Hanke T
Int J Mol Sci 23(23): . doi: 10.3390/ijms232314834
Publication date: November 27, 2022
PMID: 36499165
ProxyBind: A compendium of binding sites for proximity-induced pharmacology.
Rovers E, Liu L, Schapira M
Comput Struct Biotechnol J 20:6163-6171 . doi: 10.1016/j.csbj.2022.11.010
Publication date: November 25, 2022
PMID: 36420167
Macrocyclization of Quinazoline-Based EGFR Inhibitors Leads to Exclusive Mutant Selectivity for EGFR L858R and Del19.
Amrhein JA, Beyett TS, Feng WW, Krämer A, Weckesser J, Schaeffner IK, Rana JK, Jänne PA, Eck MJ, Knapp S, Hanke T
J Med Chem . doi: 10.1021/acs.jmedchem.2c01041
Publication date: November 16, 2022
PMID: 36384036
Discovery of Nanomolar-Affinity Pharmacological Chaperones Stabilizing the Oncogenic p53 Mutant Y220C.
Stephenson Clarke JR, Douglas LR, Duriez PJ, Balourdas DI, Joerger AC, Khadiullina R, Bulatov E, Baud MGJ
ACS Pharmacol Transl Sci 5(11):1169-1180 . doi: 10.1021/acsptsci.2c00164
Publication date: November 11, 2022
PMID: 36407959
Comparative structural analyses of the NHL domains from the human E3 ligase TRIM-NHL family.
Chaikuad A, Zhubi R, Tredup C, Knapp S
IUCrJ 9(Pt 6):720-727 . doi: 10.1107/S2052252522008582
Publication date: November 1, 2022
PMID: 36381143

October 2022

Phosphorylation of the DNA repair scaffold SLX4 drives folding of the SAP domain and activation of the MUS81-EME1 endonuclease.
Payliss BJ, Tse YWE, Reichheld SE, Lemak A, Yun HY, Houliston S, Patel A, Arrowsmith CH, Sharpe S, Wyatt HDM
Cell Rep 41(4):111537 . doi: 10.1016/j.celrep.2022.111537
Publication date: October 25, 2022
PMID: 36288699
The Chemical Probes Portal: an expert review-based public resource to empower chemical probe assessment, selection and use.
Antolin AA, Sanfelice D, Crisp A, Villasclaras Fernandez E, Mica IL, Chen Y, Collins I, Edwards A, Müller S, Al-Lazikani B, Workman P
Nucleic Acids Res . doi: 10.1093/nar/gkac909
Publication date: October 21, 2022
PMID: 36268860
Discovery of Hit Compounds for Methyl-lysine Reader Proteins from a Target Class DNA-Encoded Library.
Shell DJ, Rectenwald JM, Buttery PH, Johnson RL, Foley CA, Guduru SKR, Uguen M, Rubiano JS, Zhang X, Li F, Norris-Drouin JL, Axtman M, Brian Hardy P, Vedadi M, Frye SV, James LI, Pearce KH
SLAS Discov . doi: 10.1016/j.slasd.2022.10.003
Publication date: October 19, 2022
PMID: 36272689
PBRM1, SETD2 and BAP1 - the trinity of 3p in clear cell renal cell carcinoma.
Walton J, Lawson K, Prinos P, Finelli A, Arrowsmith C, Ailles L
Nat Rev Urol . doi: 10.1038/s41585-022-00659-1
Publication date: October 17, 2022
PMID: 36253570
Dissecting the stability determinants of a challenging de novo protein fold using massively parallel design and experimentation.
Kim TE, Tsuboyama K, Houliston S, Martell CM, Phoumyvong CM, Lemak A, Haddox HK, Arrowsmith CH, Rocklin GJ
Proc Natl Acad Sci U S A 119(41):e2122676119 . doi: 10.1073/pnas.2122676119
Publication date: October 11, 2022
PMID: 36191185
A Screening of Epigenetic Therapeutic Targets for Non-Small Cell Lung Cancer Reveals PADI4 and KDM6B as Promising Candidates.
Lesbon JCC, Garnica TK, Xavier PLP, Rochetti AL, Reis RM, Müller S, Fukumasu H
Int J Mol Sci 23(19): . doi: 10.3390/ijms231911911
Publication date: October 7, 2022
PMID: 36233212
De novo design of immunoglobulin-like domains.
Chidyausiku TM, Mendes SR, Klima JC, Nadal M, Eckhard U, Roel-Touris J, Houliston S, Guevara T, Haddox HK, Moyer A, Arrowsmith CH, Gomis-Rüth FX, Baker D, Marcos E
Nat Commun 13(1):5661 . doi: 10.1038/s41467-022-33004-6
Publication date: October 3, 2022
PMID: 36192397

September 2022

Covalent Modification of Bromodomain Proteins by Peptides Containing a DNA Damage-Induced, Histone Post-Translational Modification.
Jacinto MP, Heidenreich D, Müller S, Greenberg MM
Chembiochem e202200373 . doi: 10.1002/cbic.202200373
Publication date: September 29, 2022
PMID: 36173930
ChemBioPort: an online portal to navigate the structure, function and chemical inhibition of the human proteome.
Liu L, Rovers E, Schapira M
Database (Oxford) 2022: . doi: 10.1093/database/baac088
Publication date: September 27, 2022
PMID: 36164975
Identification of Novel 2,4,5-Trisubstituted Pyrimidines as Potent Dual Inhibitors of Plasmodial PfGSK3/PfPK6 with Activity against Blood Stage Parasites In Vitro.
Galal KA, Truong A, Kwarcinski F, de Silva C, Avalani K, Havener TM, Chirgwin ME, Merten E, Ong HW, Willis C, Abdelwaly A, Helal MA, Derbyshire ER, Zutshi R, Drewry DH
J Med Chem . doi: 10.1021/acs.jmedchem.2c00996
Publication date: September 27, 2022
PMID: 36166733
Development and Characterization of Type I, Type II, and Type III LIM-Kinase Chemical Probes.
Hanke T, Mathea S, Woortman J, Salah E, Berger BT, Tumber A, Kashima R, Hata A, Kuster B, Müller S, Knapp S
J Med Chem . doi: 10.1021/acs.jmedchem.2c01106
Publication date: September 22, 2022
PMID: 36136092
Fragment-based discovery of orphan nuclear receptor Nur77/NGFI-B ligands.
Arifi S, Zaienne D, Heering J, Wein T, Zhubi R, Chaikuad A, Knapp S, Marschner JA, Merk D
Bioorg Chem 129:106164 . doi: 10.1016/j.bioorg.2022.106164
Publication date: September 17, 2022
PMID: 36162288
A small molecule antagonist of SMN disrupts the interaction between SMN and RNAP II.
Liu Y, Iqbal A, Li W, Ni Z, Wang Y, Ramprasad J, Abraham KJ, Zhang M, Zhao DY, Qin S, Loppnau P, Jiang H, Guo X, Brown PJ, Zhen X, Xu G, Mekhail K, Ji X, Bedford MT, Greenblatt JF, Min J
Nat Commun 13(1):5453 . doi: 10.1038/s41467-022-33229-5
Publication date: September 16, 2022
PMID: 36114190
Identification and Utilization of a Chemical Probe to Interrogate the Roles of PIKfyve in the Lifecycle of β-Coronaviruses.
Drewry DH, Potjewyd FM, Bayati A, Smith JL, Dickmander RJ, Howell S, Taft-Benz S, Min SM, Hossain MA, Heise M, McPherson PS, Moorman NJ, Axtman AD
J Med Chem . doi: 10.1021/acs.jmedchem.2c00697
Publication date: September 16, 2022
PMID: 36111834
CDK11 regulates pre-mRNA splicing by phosphorylation of SF3B1.
Hluchý M, Gajdušková P, Ruiz de Los Mozos I, Rájecký M, Kluge M, Berger BT, Slabá Z, Potěšil D, Weiß E, Ule J, Zdráhal Z, Knapp S, Paruch K, Friedel CC, Blazek D
Nature . doi: 10.1038/s41586-022-05204-z
Publication date: September 14, 2022
PMID: 36104565
Identification of Histone Peptide Binding Specificity and Small-Molecule Ligands for the TRIM33α and TRIM33β Bromodomains.
Sekirnik AR, Reynolds JK, See L, Bluck JP, Scorah AR, Tallant C, Lee B, Leszczynska KB, Grimley RL, Storer RI, Malattia M, Crespillo S, Caria S, Duclos S, Hammond EM, Knapp S, Morris GM, Duarte F, Biggin PC, Conway SJ
ACS Chem Biol . doi: 10.1021/acschembio.2c00266
Publication date: September 13, 2022
PMID: 36098557
Combinatorial Anticancer Drug Screen Identifies Off-Target Effects of Epigenetic Chemical Probes.
Barghout SH, Mann MK, Aman A, Yu Y, Alteen MG, Schimmer AD, Schapira M, Arrowsmith CH, Barsyte-Lovejoy D
ACS Chem Biol . doi: 10.1021/acschembio.2c00451
Publication date: September 9, 2022
PMID: 36084291

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