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Displaying 101 - 150 of 2329


March 2022

Kinase domain autophosphorylation rewires the activity and substrate specificity of CK1 enzymes.
Cullati SN, Chaikuad A, Chen JS, Gebel J, Tesmer L, Zhubi R, Navarrete-Perea J, Guillen RX, Gygi SP, Hummer G, Dötsch V, Knapp S, Gould KL
Mol Cell . doi: 10.1016/j.molcel.2022.03.005
Publication date: March 21, 2022
PMID: 35353987
PRMT5 regulates ATF4 transcript splicing and oxidative stress response.
Szewczyk MM, Luciani GM, Vu V, Murison A, Dilworth D, Barghout SH, Lupien M, Arrowsmith CH, Minden MD, Barsyte-Lovejoy D
Redox Biol 51:102282 . doi: 10.1016/j.redox.2022.102282
Publication date: March 11, 2022
PMID: 35305370
Stopping pandemics before they start: Lessons learned from SARS-CoV-2.
Edwards AM, Baric RS, Saphire EO, Ulmer JB
Science 375(6585):1133-1139 . doi: 10.1126/science.abn1900
Publication date: March 11, 2022
PMID: 35271333
Development of novel urea-based ATM kinase inhibitors with subnanomolar cellular potency and high kinome selectivity.
Dimitrov T, Anli C, Moschopoulou AA, Kronenberger T, Kudolo M, Geibel C, Schwalm MP, Knapp S, Zender L, Forster M, Laufer S
Eur J Med Chem 235:114234 . doi: 10.1016/j.ejmech.2022.114234
Publication date: March 8, 2022
PMID: 35325634
Resistance to kinase inhibition through shortened target engagement.
Rangwala AM, Berger BT, Robers MB, Knapp S, Seeliger MA
Mol Cell Oncol 9(1):2029999 . doi: 10.1080/23723556.2022.2029999
Publication date: March 8, 2022
PMID: 35252553
Evolutionary history of the p53 family DNA-binding domain: insights from an Alvinella pompejana homolog.
Zhang Q, Balourdas DI, Baron B, Senitzki A, Haran TE, Wiman KG, Soussi T, Joerger AC
Cell Death Dis 13(3):214 . doi: 10.1038/s41419-022-04653-8
Publication date: March 7, 2022
PMID: 35256607
The MYC oncoprotein directly interacts with its chromatin cofactor PNUTS to recruit PP1 phosphatase.
Wei Y, Redel C, Ahlner A, Lemak A, Johansson-Åkhe I, Houliston S, Kenney TMG, Tamachi A, Morad V, Duan S, Andrews DW, Wallner B, Sunnerhagen M, Arrowsmith CH, Penn LZ
Nucleic Acids Res . doi: 10.1093/nar/gkac138
Publication date: March 4, 2022
PMID: 35244724
Longitudinal assessment of reactivity and affinity profile of anti-Jo1 autoantibodies to distinct HisRS domains and a splice variant in a cohort of patients with myositis and anti-synthetase syndrome.
Notarnicola A, Preger C, Lundström SL, Renard N, Wigren E, Van Gompel E, Galindo-Feria AS, Persson H, Fathi M, Grunewald J, Jakobsson PJ, Gräslund S, Lundberg IE, Fernandes-Cerqueira C
Arthritis Res Ther 24(1):62 . doi: 10.1186/s13075-022-02745-6
Publication date: March 2, 2022
PMID: 35236390
Nanobodies as allosteric modulators of Parkinson's disease-associated LRRK2.
Singh RK, Soliman A, Guaitoli G, Störmer E, von Zweydorf F, Dal Maso T, Oun A, Van Rillaer L, Schmidt SH, Chatterjee D, David JA, Pardon E, Schwartz TU, Knapp S, Kennedy EJ, Steyaert J, Herberg FW, Kortholt A, Gloeckner CJ, Versées W
Proc Natl Acad Sci U S A 119(9): . doi: 10.1073/pnas.2112712119
Publication date: March 1, 2022
PMID: 35217606

February 2022

LRRK2 dynamics analysis identifies allosteric control of the crosstalk between its catalytic domains.
Weng JH, Aoto PC, Lorenz R, Wu J, Schmidt SH, Manschwetus JT, Kaila-Sharma P, Silletti S, Mathea S, Chatterjee D, Knapp S, Herberg FW, Taylor SS
PLoS Biol 20(2):e3001427 . doi: 10.1371/journal.pbio.3001427
Publication date: February 23, 2022
PMID: 35192607
Image-Based Annotation of Chemogenomic Libraries for Phenotypic Screening.
Tjaden A, Chaikuad A, Kowarz E, Marschalek R, Knapp S, Schröder M, Müller S
Molecules 27(4): . doi: 10.3390/molecules27041439
Publication date: February 21, 2022
PMID: 35209227
Cascade Synthesis of Kinase-Privileged 3-Aminoindazoles via Intramolecular N-N Bond Formation.
Zhu WF, Krämer A, Knapp S, Proschak E, Hernandez-Olmos V
J Org Chem . doi: 10.1021/acs.joc.1c03057
Publication date: February 18, 2022
PMID: 35179025
Development of the First Covalent Monopolar Spindle Kinase 1 (MPS1/TTK) Inhibitor.
M Serafim RA, da Silva Santiago A, Schwalm MP, Hu Z, Dos Reis CV, Takarada JE, Mezzomo P, Massirer KB, Kudolo M, Gerstenecker S, Chaikuad A, Zender L, Knapp S, Laufer S, Couñago RM, Gehringer M
J Med Chem . doi: 10.1021/acs.jmedchem.1c01165
Publication date: February 15, 2022
PMID: 35167750
Cdyl Deficiency Brakes Neuronal Excitability and Nociception through Promoting Kcnb1 Transcription in Peripheral Sensory Neurons.
Sun ZW, Waybright JM, Beldar S, Chen L, Foley CA, Norris-Drouin JL, Lyu TJ, Dong A, Min J, Wang YP, James LI, Wang Y
Adv Sci (Weinh) e2104317 . doi: 10.1002/advs.202104317
Publication date: February 4, 2022
PMID: 35119221

January 2022

Development of dihydropyrrolopyridinone-based PKN2/PRK2 chemical tools to enable drug discovery.
Scott F, Fala AM, Takarada JE, Ficu MP, Pennicott LE, Reuillon TD, Couñago RM, Massirer KB, Elkins JM, Ward SE
Bioorg Med Chem Lett 60:128588 . doi: 10.1016/j.bmcl.2022.128588
Publication date: January 29, 2022
PMID: 35104640
Target 2035 - update on the quest for a probe for every protein.
Müller S, Ackloo S, Al Chawaf A, Al-Lazikani B, Antolin A, Baell JB, Beck H, Beedie S, Betz UAK, Bezerra GA, Brennan PE, Brown D, Brown PJ, Bullock AN, Carter AJ, Chaikuad A, Chaineau M, Ciulli A, Collins I, Dreher J, Drewry D, Edfeldt K, Edwards AM, Egner U, Frye SV, Fuchs SM, Hall MD, Hartung IV, Hillisch A, Hitchcock SH, Homan E, Kannan N, Kiefer JR, Knapp S, Kostic M, Kubicek S, Leach AR, Lindemann S, Marsden BD, Matsui H, Meier JL, Merk D, Michel M, Morgan MR, Mueller-Fahrnow A, Owen DR, Perry BG, Rosenberg SH, Saikatendu KS, Schapira M, Scholten C, Sharma S, Simeonov A, Sundström M, Superti-Furga G, Todd MH, Tredup C, Vedadi M, von Delft F, Willson TM, Winter GE, Workman P, Arrowsmith CH
RSC Med Chem 13(1):13-21 . doi: 10.1039/d1md00228g
Publication date: January 27, 2022
PMID: 35211674
Autoantibodies against Four-and-a-Half-LIM Domain 1 (FHL1) in Inflammatory Myopathies: Results from an Australian Single-Center Cohort.
Galindo-Feria AS, Horuluoglu B, Day J, Fernandes-Cerqueira C, Wigren E, Gräslund S, Proudman S, Lundberg IE, Limaye V
Rheumatology (Oxford) . doi: 10.1093/rheumatology/keac003
Publication date: January 12, 2022
PMID: 35022656
Aurora Kinase A Is Involved in Controlling the Localization of Aquaporin-2 in Renal Principal Cells.
Baltzer S, Bulatov T, Schmied C, Krämer A, Berger BT, Oder A, Walker-Gray R, Kuschke C, Zühlke K, Eichhorst J, Lehmann M, Knapp S, Weston J, von Kries JP, Süssmuth RD, Klussmann E
Int J Mol Sci 23(2): . doi: 10.3390/ijms23020763
Publication date: January 11, 2022
PMID: 35054947
Design of a Potent TLX Agonist by Rational Fragment Fusion.
Faudone G, Zhubi R, Celik F, Knapp S, Chaikuad A, Heering J, Merk D
J Med Chem . doi: 10.1021/acs.jmedchem.1c01757
Publication date: January 6, 2022
PMID: 34989568
TDP-43 Modulation by Tau-Tubulin Kinase 1 Inhibitors: A New Avenue for Future Amyotrophic Lateral Sclerosis Therapy.
Nozal V, Martínez-González L, Gomez-Almeria M, Gonzalo-Consuegra C, Santana P, Chaikuad A, Pérez-Cuevas E, Knapp S, Lietha D, Ramírez D, Petralla S, Monti B, Gil C, Martín-Requero A, Palomo V, de Lago E, Martinez A
J Med Chem . doi: 10.1021/acs.jmedchem.1c01942
Publication date: January 3, 2022
PMID: 34978799
Structural Aspects of LIMK Regulation and Pharmacology.
Chatterjee D, Preuss F, Dederer V, Knapp S, Mathea S
Cells 11(1): . doi: 10.3390/cells11010142
Publication date: January 2, 2022
PMID: 35011704

December 2021

Histone lysine methacrylation is a dynamic post-translational modification regulated by HAT1 and SIRT2.
Delaney K, Tan M, Zhu Z, Gao J, Dai L, Kim S, Ding J, He M, Halabelian L, Yang L, Nagarajan P, Parthun MR, Lee S, Khochbin S, Zheng YG, Zhao Y
Cell Discov 7(1):122 . doi: 10.1038/s41421-021-00344-4
Publication date: December 28, 2021
PMID: 34961760
Selective BH3 mimetics synergize with BET inhibition to induce mitochondrial apoptosis in rhabdomyosarcoma cells.
Erdogdu U, Dolgikh N, Laszig S, Särchen V, Meister MT, Wanior M, Knapp S, Boedicker C
Neoplasia 24(2):109-119 . doi: 10.1016/j.neo.2021.11.012
Publication date: December 23, 2021
PMID: 34959030
Prediction and Validation of a Protein's Free Energy Surface Using Hydrogen Exchange and (Importantly) Its Denaturant Dependence.
Peng X, Baxa M, Faruk N, Sachleben JR, Pintscher S, Gagnon IA, Houliston S, Arrowsmith CH, Freed KF, Rocklin GJ, Sosnick TR
J Chem Theory Comput . doi: 10.1021/acs.jctc.1c00960
Publication date: December 22, 2021
PMID: 34936354
Single tracer-based protocol for broad-spectrum kinase profiling in live cells with NanoBRET.
Robers MB, Wilkinson JM, Vasta JD, Berger LM, Berger BT, Knapp S
STAR Protoc 2(4):100822 . doi: 10.1016/j.xpro.2021.100822
Publication date: December 17, 2021
PMID: 34568844
Discovery of Novel BRD4 Ligand Scaffolds by Automated Navigation of the Fragment Chemical Space.
Piticchio SG, Martínez-Cartró M, Scaffidi S, Rachman M, Rodriguez-Arevalo S, Sanchez-Arfelis A, Escolano C, Picaud S, Krojer T, Filippakopoulos P, von Delft F, Galdeano C, Barril X
J Med Chem . doi: 10.1021/acs.jmedchem.1c01108
Publication date: December 13, 2021
PMID: 34898210
Structural basis for the recognition of the S2, S5-phosphorylated RNA polymerase II CTD by the mRNA anti-terminator protein hSCAF4.
Zhou M, Ehsan F, Gan L, Dong A, Li Y, Liu K, Min J
FEBS Lett . doi: 10.1002/1873-3468.14256
Publication date: December 13, 2021
PMID: 34897689
The Transcriptional Repressor Orphan Nuclear Receptor TLX Is Responsive to Xanthines.
Faudone G, Kilu W, Ni X, Chaikuad A, Sreeramulu S, Heitel P, Schwalbe H, Knapp S, Schubert-Zsilavecz M, Heering J, Merk D
ACS Pharmacol Transl Sci 4(6):1794-1807 . doi: 10.1021/acsptsci.1c00195
Publication date: December 10, 2021
PMID: 34927011
Huntingtin structure is orchestrated by HAP40 and shows a polyglutamine expansion-specific interaction with exon 1.
Harding RJ, Deme JC, Hevler JF, Tamara S, Lemak A, Cantle JP, Szewczyk MM, Begeja N, Goss S, Zuo X, Loppnau P, Seitova A, Hutchinson A, Fan L, Truant R, Schapira M, Carroll JB, Heck AJR, Lea SM, Arrowsmith CH
Commun Biol 4(1):1374 . doi: 10.1038/s42003-021-02895-4
Publication date: December 8, 2021
PMID: 34880419
FOXN1 forms higher-order nuclear condensates displaced by mutations causing immunodeficiency.
Rota IA, Handel AE, Maio S, Klein F, Dhalla F, Deadman ME, Cheuk S, Newman JA, Michaels YS, Zuklys S, Prevot N, Hublitz P, Charles PD, Gkazi AS, Adamopoulou E, Qasim W, Davies EG, Hanson I, Pagnamenta AT, Camps C, Dreau HM, White A, James K, Fischer R, Gileadi O, Taylor JC, Fulga T, Lagerholm BC, Anderson G, Sezgin E, Holländer GA
Sci Adv 7(49):eabj9247 . doi: 10.1126/sciadv.abj9247
Publication date: December 3, 2021
PMID: 34860543

November 2021

Structure-Based Design of Dual Partial Peroxisome Proliferator-Activated Receptor γ Agonists/Soluble Epoxide Hydrolase Inhibitors.
Lillich FF, Willems S, Ni X, Kilu W, Borkowsky C, Brodsky M, Kramer JS, Brunst S, Hernandez-Olmos V, Heering J, Schierle S, Kestner RI, Mayser FM, Helmstädter M, Göbel T, Weizel L, Namgaladze D, Kaiser A, Steinhilber D, Pfeilschifter W, Kahnt AS, Proschak A, Chaikuad A, Knapp S, Merk D, Proschak E
J Med Chem . doi: 10.1021/acs.jmedchem.1c01331
Publication date: November 24, 2021
PMID: 34818007
NUAK family kinase 2 is a novel therapeutic target for prostate cancer.
Fu W, Zhao MT, Driver LM, Schirmer AU, Yin Q, You S, Freedland SJ, DiGiovanni J, Drewry DH, Macias E
Mol Carcinog . doi: 10.1002/mc.23374
Publication date: November 24, 2021
PMID: 34818445
Inhibitors of the Hippo Pathway Kinases STK3/MST2 and STK4/MST1 Have Utility for the Treatment of Acute Myeloid Leukemia.
Bata N, Chaikuad A, Bakas NA, Limpert AS, Lambert LJ, Sheffler DJ, Berger LM, Liu G, Yuan C, Wang L, Peng Y, Dong J, Celeridad M, Layng F, Knapp S, Cosford NDP
J Med Chem . doi: 10.1021/acs.jmedchem.1c00804
Publication date: November 22, 2021
PMID: 34807584
Mutation in Abl kinase with altered drug-binding kinetics indicates a novel mechanism of imatinib resistance.
Lyczek A, Berger BT, Rangwala AM, Paung Y, Tom J, Philipose H, Guo J, Albanese SK, Robers MB, Knapp S, Chodera JD, Seeliger MA
Proc Natl Acad Sci U S A 118(46): . doi: 10.1073/pnas.2111451118
Publication date: November 16, 2021
PMID: 34750265
A chemical probe targeting the PWWP domain alters NSD2 nucleolar localization.
Dilworth D, Hanley RP, Ferreira de Freitas R, Allali-Hassani A, Zhou M, Mehta N, Marunde MR, Ackloo S, Carvalho Machado RA, Khalili Yazdi A, Owens DDG, Vu V, Nie DY, Alqazzaz M, Marcon E, Li F, Chau I, Bolotokova A, Qin S, Lei M, Liu Y, Szewczyk MM, Dong A, Kazemzadeh S, Abramyan T, Popova IK, Hall NW, Meiners MJ, Cheek MA, Gibson E, Kireev D, Greenblatt JF, Keogh MC, Min J, Brown PJ, Vedadi M, Arrowsmith CH, Barsyte-Lovejoy D, James LI, Schapira M
Nat Chem Biol . doi: 10.1038/s41589-021-00898-0
Publication date: November 15, 2021
PMID: 34782742

October 2021

Selectivity aspects of activity-based (chemical) probes.
Heinzlmeir S, Müller S
Drug Discov Today . doi: 10.1016/j.drudis.2021.10.021
Publication date: October 30, 2021
PMID: 34728376
The human pseudouridine synthase PUS7 recognizes RNA with an extended multi-domain binding surface.
Guegueniat J, Halabelian L, Zeng H, Dong A, Li Y, Wu H, Arrowsmith CH, Kothe U
Nucleic Acids Res . doi: 10.1093/nar/gkab934
Publication date: October 28, 2021
PMID: 34718722
Structural basis of the TAM domain of BAZ2A in binding to DNA or RNA independent of methylation status.
Chen S, Zhou M, Dong A, Loppnau P, Wang M, Min J, Liu K
J Biol Chem 101351 . doi: 10.1016/j.jbc.2021.101351
Publication date: October 26, 2021
PMID: 34715126
Design of a Two-in-One Mutant-Selective Epidermal Growth Factor Receptor Inhibitor That Spans the Orthosteric and Allosteric Sites.
Wittlinger F, Heppner DE, To C, Günther M, Shin BH, Rana JK, Schmoker AM, Beyett TS, Berger LM, Berger BT, Bauer N, Vasta JD, Corona CR, Robers MB, Knapp S, Jänne PA, Eck MJ, Laufer SA
J Med Chem . doi: 10.1021/acs.jmedchem.1c00848
Publication date: October 20, 2021
PMID: 34668706
Chemical Genetics Screen Identifies COPB2 Tool Compounds That Alters ER Stress Response and Induces RTK Dysregulation in Lung Cancer Cells.
Saraon P, Snider J, Schormann W, Rai A, Radulovich N, Sánchez-Osuna M, Coulombe-Huntington J, Huard C, Mohammed M, Lima-Fernandes E, Thériault B, Halabelian L, Chan M, Joshi D, Drecun L, Yao Z, Pathmanathan S, Wong V, Lyakisheva A, Aboualizadeh F, Niu L, Li F, Kiyota T, Subramanian R, Joseph B, Aman A, Prakesch M, Isaac M, Mamai A, Poda G, Vedadi M, Marcellus R, Uehling D, Leighl N, Sacher A, Samaržija M, Jakopović M, Arrowsmith C, Tyers M, Tsao MS, Andrews D, Al-Awar R, Stagljar I
J Mol Biol 433(23):167294 . doi: 10.1016/j.jmb.2021.167294
Publication date: October 16, 2021
PMID: 34662547
The structure of nontypeable Haemophilus influenzae SapA in a closed conformation reveals a constricted ligand-binding cavity and a novel RNA binding motif.
Lukacik P, Owen CD, Harris G, Bolla JR, Picaud S, Alibay I, Nettleship JE, Bird LE, Owens RJ, Biggin PC, Filippakopoulos P, Robinson CV, Walsh MA
PLoS One 16(10):e0256070 . doi: 10.1371/journal.pone.0256070
Publication date: October 16, 2021
PMID: 34653190
Structure-Activity Relationship of USP5 Inhibitors.
Mann MK, Zepeda-Velázquez CA, González-Álvarez H, Dong A, Kiyota T, Aman AM, Loppnau P, Li Y, Wilson B, Arrowsmith CH, Al-Awar R, Harding RJ, Schapira M
J Med Chem . doi: 10.1021/acs.jmedchem.1c00889
Publication date: October 14, 2021
PMID: 34648286
Discovery of a Potent and Highly Isoform-Selective Inhibitor of the Neglected Ribosomal Protein S6 Kinase Beta 2 (S6K2).
Gerstenecker S, Haarer L, Schröder M, Kudolo M, Schwalm MP, Wydra V, Serafim RAM, Chaikuad A, Knapp S, Laufer S, Gehringer M
Cancers (Basel) 13(20): . doi: 10.3390/cancers13205133
Publication date: October 13, 2021
PMID: 34680283

September 2021

Synthesis and Evaluation of Novel 1,2,6-Thiadiazinone Kinase Inhibitors as Potent Inhibitors of Solid Tumors.
Kalogirou AS, East MP, Laitinen T, Torrice CD, Maffuid KA, Drewry DH, Koutentis PA, Johnson GL, Crona DJ, Asquith CRM
Molecules 26(19): . doi: 10.3390/molecules26195911
Publication date: September 29, 2021
PMID: 34641454
Design and Development of a Chemical Probe for Pseudokinase Ca2+/calmodulin-Dependent Ser/Thr Kinase.
Russ N, Schröder M, Berger BT, Mandel S, Aydogan Y, Mauer S, Pohl C, Drewry DH, Chaikuad A, Müller S, Knapp S
J Med Chem . doi: 10.1021/acs.jmedchem.1c00845
Publication date: September 20, 2021
PMID: 34543009
Characterizing the role of the dark kinome in neurodegenerative disease - A mini review.
Axtman AD
Biochim Biophys Acta Gen Subj 130014 . doi: 10.1016/j.bbagen.2021.130014
Publication date: September 18, 2021
PMID: 34547390
Assessing reversible and irreversible binding effects of kinase covalent inhibitors through ADP-Glo assays.
Schröder M, Chaikuad A
STAR Protoc 2(3):100717 . doi: 10.1016/j.xpro.2021.100717
Publication date: September 17, 2021
PMID: 34401783
Novel quaternary structures of the human prion protein globular domain.
Bortot LO, Rangel VL, Pavlovici FA, El Omari K, Wagner A, Brandao-Neto J, Talon R, von Delft F, Reidenbach AG, Vallabh SM, Minikel EV, Schreiber S, Nonato MC
Biochimie 191:118-125 . doi: 10.1016/j.biochi.2021.09.005
Publication date: September 10, 2021
PMID: 34517052


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