Publications

  • 2017
  • 2016
      • Thorsell A-G, Ekblad T, Karlberg T, Löw M, Pinto A F, Tresaugues L, Moche M, Cohen M S and Shüler H. Structural basis for potency and promiscuity in poly(ADP-ribose) polymerase (PARP) and tankyrase inhibitors. (2016) J. Med. Chem. DOI: 10.1021/acs.jmedchem.6b00990
      • Exell JC, Thompson MJ, Finger LD, Shaw SJ, Debreczeni J, et al. Cellularly active N-hydroxyurea FEN1 inhibitors block substrate entry to the active site. (2016) Nature Chem. Biol. DOI:10.1038/nchembio.2148
      • Xu H, Gopalsamy A, Hett E, Salter S, Aulabaugh A, Kyne R, Pierce B, Jones LH. Cellular Thermal Shift and Clickable Chemical Probe Assays for the Determination of Drug-Target Engagement in Live Cells. (2016) Org. Biomol. Chem. DOI: 10.1039/C6OB01078D
      • Almqvist H, Axelssson H, Rozbeh J, Dan C, Mateus A, Haraldsson M, Larsson A, Martinez Molina D, Artursson P, Lundbäck T, Nordlund P. CETSA screening identifies known and novel thymidylate synthase inhibitors and slow intracellular activation of 5-fluorouracil. (2016) Nature Communications 7:11040
      • Martinez Molina D, Nordlund P. The Cellular Thermal Shift Assay: A Novel Biophysical Assay for In Situ Drug Target Engagement and Mechanistic Biomarker Studies. (2016) Annu. Rev. Pharmacol. Toxicol. 56:141-161
  • 2015
      • Reinhard FBM, Eberhard D, Werner T, Franken H, Childs D, et al. Thermal proteome profiling monitors ligand interactions with cellular membrane proteins. (2015) Nature Methods 12:1129-1131
      • Qin JJ, Wang W, Voruganti S, Wang H, Zhang WD, Zhang R. Identification of a new class of natural product MDM2 inhibitor: in vitro and in vivo anti-breast cancer activities and target validation. (2015) Oncotarget 6:2623–40
      • Tan BX, Brown CJ, Ferrer FJ, Yuen TY, Quah ST, et al. Assessing the efficacy of Mdm2/Mdm4- inhibiting stapled peptides using cellular thermal shift assays. (2015) Sci. Rep. 5:12116
      • Franken H, Mathieson T, Childs D, Sweetman GMA, Werner T, et al. Thermal proteome profiling for unbiased identification of direct and indirect drug targets using multiplexed quantitative mass spectrometry. (2015) Nature Protocols 10:1567-1593
      • Malik R, Khan AP, Asangani IA, Cieślik M, Prensner JR, et al.Targeting the MLL complex in castration-resistant prostate cancer. (2015) Nat. Med. 21:344–52
      • Sidrauski C, Tsai JC, Kampmann M, Hearn BR, Vedantham P, et.al.Pharmacological dimerization and activation of the exchange factor eIF2B antagonizes the integrated stress response. (2015) eLife 4:e07314
      • Chan-Penebre E, Kuplast KG, Majer CR, Boriack-Sjodin PA, Wigle TJ, et al. A selective inhibitor of PRMT5 with in vivo and in vitro potency in MCL models. (2015) Nat. Chem. Biol. 11:432–3
  • 2014
      • Bradley WD, Arora S, Busby J, Balasubramanian S, Gehling VS, et al. EZH2 inhibitor efficacy in non-Hodgkin’s lymphoma does not require suppression of H3K27 monomethylation. (2014) Chem. Biol. 21:1463–75
      • Bai L, Chen J, McEachern D, Liu L, Zhou H, et al. BM-1197: a novel and specific Bcl-2/Bcl-xL inhibitor inducing complete and long-lasting tumor regression in vivo. (2014) PLOS ONE 9:e99404
      • Miettinen TP, Björklund M. NQO2 is a reactive oxygen species generating off-target for ac- etaminophen. (2014) Mol. Pharm. 11:4395–404
      • Sackton KL, Dimova N, Zeng X, Tian W, Zhang M, et al. Synergistic blockade of mitotic exit by two chemical inhibitors of the APC/C. (2014) Nature 514:646–49
      • Khoo KH, Verma CS and Lane DP. Drugging the p53 pathway: understanding the route to clinical efficacy. (2014) Nature Reviews Drug Discovery 13(3):217-236
      • Huber KVM et al. Stereospecific targeting of MTH1 by (S)-crizotinib as an anticancer strategy. (2014) Nature 508(7495):222–227
      • Jafari R, Almqvist H, Axelsson H, Ignatushchenko M, Lundbäck T, Nordlund P, Martinez Molina D. The cellular thermal shift assay for evaluating drug target interactions in cells. (2014) Nature Protocols 9(9):2100-2122
      • Savitski MM, Reinhard FBM, Franken H, Werner T, Savitski MF, Eberhard D, Martinez Molina D, Jafari R, Dovega RB, Klaeger S, Kuster B, Nordlund P, Bantscheff M,
      • Drewes G. Tracking cancer drugs in living cells by thermal profiling of the proteome. (2014) Science 346(6205):55
  • 2013
      • Swinney DC. The contribution of mechanistic understanding to phenotypic screening for first-in- class medicines. (2013) J. Biomol. Screen 18:1186–92
      • Donner A. Engaging drug discovery. (2013) SciBX: Science-Business eXchange 6(30):1-3
      • Huang J. Tracking Drugs. (2013) New England Journal of Medicine 369(12):1168-1169
      • Martinez Molina D, Jafari R, Ignatushchenko M, Seki T, Larsson EA, Dan C, Sreekumar L, Cao Y, Nordlund P. Monitoring drug target engagement in cells and tissues using the cellular thermal shift assay. (2013) Science 341(6141):84-87