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Reviews

Recent developments in the use of differential scanning fluorometry in protein and small molecule discovery and characterization

Pages 1071-1082 | Published online: 06 Jun 2013

Bibliography

  • Fang Y. Ligand–receptor interaction platforms and their applications for drug discovery. Expert Opin Drug Discov 2012;7(10):969-88
  • Garbett NC, Chaires JB. Thermodynamic studies for drug design and screening. Expert Opin Drug Discov 2012;7(4):299-314
  • Hau JC, Fontana P, Zimmermann C, et al. Leveraging the contribution of thermodynamics in drug discovery with the help of fluorescence-based thermal shift assays. J Biomol Screen 2011;16(5):552-6
  • Senisterra G, Chau I, Vedadi M. Thermal denaturation assays in chemical biology. Assay Drug Dev Technol 2012;10(2):128-36
  • Zhang R, Monsma F. Fluorescence-based thermal shift assays. Curr Opin Drug Discov Devel 2010;13(4):389-402
  • Bergsdorf C, Ottl J. Affinity-based screening techniques: their impact and benefit to increase the number of high quality leads. Expert Opin Drug Discov 2010;5(11):1095-107
  • Niesen FH, Berglund H, Vedadi M. The use of differential scanning fluorimetry to detect ligand interactions that promote protein stability. Nat Protoc 2007;2(9):2212-21
  • Vedadi M, Niesen FH, Allali-Hassani A, et al. Chemical screening methods to identify ligands that promote protein stability, protein crystallization, and structure determination. Proc Natl Acad Sci USA 2006;103(43):15835-40
  • Clemente JC, Nulton E, Nelen M, et al. Screening and Characterization of Human Monoglyceride Lipase Active Site Inhibitors Using Orthogonal Binding and Functional Assays. J Biomol Screen 2012;17(5):629-40
  • Pantoliano MW, Petrella EC, Kwasnoski JD, et al. High-Density Miniaturized Thermal Shift Assays as a General Strategy for Drug Discovery. J Biomol Screen 2001;6(6):429-40
  • Major LL, Denton H, Smith TK. Coupled enzyme activity and thermal shift screening of the Maybridge rule of 3 fragment library against Trypanosoma brucei choline kinase; a genetically validated drug target. In: El-Shemy HA, editor, Drug discovery. ISBN 978-953-51-0906-8, Published: January 23, 2013 DOI: 10.5772/52668
  • Egger S, Chaikuad A, Kavanagh KL, et al. Structure and Mechanism of Human UDP-glucose 6-Dehydrogenase. J Biol Chem 2011;286(27):23877-87
  • Crowther GJ, Napuli AJ, Thomas AP, et al. Buffer optimization of thermal melt assays of Plasmodium proteins for detection of small-molecule ligands. J Biomol Screen 2009;14(6):700-7
  • Winquist J, Abdurakhmanov E, Baraznenok V, et al. Resolution of the interaction mechanisms and characteristics of non-nucleoside inhibitors of hepatitis C virus polymerase. Antiviral Res 2013;97(3):356-68
  • Lo M-C, Aulabaugh A, Jin G, et al. Evaluation of fluorescence-based thermal shift assays for hit identification in drug discovery. Anal Biochem 2004;332(1):153-9
  • Herzog G, Joerger AC, Shmueli MD, et al. Evaluating drosophila p53 as a model system for studying cancer mutations. J Biol Chem 2012;287(53):44330-7
  • Breuer S, Chang MW, Yuan J, Torbett BE. Identification of HIV-1 inhibitors targeting the nucleocapsid protein. J Med Chem 2012;55(11):4968-77
  • Applied Biosystems real-time PCR platforms. Available from: http://www.invitrogen.com/site/us/en/home/Products-and-Services/Applications/PCR/real-time-pcr/real-time-pcr-applications/real-time-pcr-protein-analysis/protein-thermal-shift.html?icid=fr-proteinmelt
  • Photon Technology International Plate Reader. Available from: http://www.pti-nj.com/PlateReader/PlateReader-FluoDia.html
  • Rabeh Wael M, Bossard F, Xu H, et al. Correction of both NBD1 energetics and domain interface is required to restore ΔF508 CFTR folding and function. Cell 2012;148(1–2):150-63
  • ProteoStat®: Ultrasensitive Fluorescent Assays. Available from: http://www.enzolifesciences.com/browse/bioprocess/proteostat-range-overview/
  • Menzen T, Friess W. High-throughput melting-temperature analysis of a monoclonal antibody by differential scanning fluorimetry in the presence of surfactants. J Pharm Sci 2013;102(2):415-28
  • Senisterra GA, Soo Hong B, Park HW, Vedadi M. Application of high-throughput isothermal denaturation to assess protein stability and screen for ligands. J Biomol Screen 2008;13(5):337-42
  • Patel R, Lebrun LA, Wang S, et al. ATLAS–a high-throughput affinity-based screening technology for soluble proteins: technology application using p38 MAP kinase. Assay Drug Dev Technol 2008;6(1):55-68
  • Thompson PA, Wang S, Howett LJ, et al. Identification of ligand binding by protein stabilization: comparison of ATLAS with biophysical and enzymatic methods. Assay Drug Dev Technol 2008;6(1):69-81
  • Biggar KK, Dawson NJ, Storey KB. Real-time protein unfolding: a method for determining the kinetics of native protein denaturation using a quantitative real-time thermocycler. Biotechniques 2012;53(4):231-8
  • Amrane S, De Cian A, Rosu F, et al. Identification of trinucleotide repeat ligands with a FRET melting Assay. ChemBioChem 2008;9(8):1229-34
  • Mergny J-L, Maurizot J-C. Fluorescence resonance energy transfer as a probe for G-quartet formation by a telomeric repeat. ChemBioChem 2001;2(2):124-32
  • Renčiuk D, Zhou J, Beaurepaire L, et al. A FRET-based screening assay for nucleic acid ligands. Methods 2012;57(1):122-8
  • Stefan L, Bertrand B, Richard P, et al. Assessing the differential affinity of small molecules for noncanonical DNA structures. ChemBioChem 2012;13(13):1905-12
  • Waldron TT, Murphy KP. Stabilization of proteins by ligand binding: application to drug screening and determination of unfolding energetics. Biochemistry 2003;42(17):5058-64
  • Matulis D, Kranz JK, Salemme FR, Todd MJ. Thermodynamic stability of carbonic anhydrase: measurements of binding affinity and stoichiometry using thermofluor. Biochemistry 2005;44(13):5258-66
  • Lavinder JJ, Hari SB, Sullivan BJ, Magliery TJ. High-throughput thermal scanning: a general, rapid dye-binding thermal shift screen for protein engineering. J Am Chem Soc 2009;131(11):3794-5
  • Crowther GJ, He P, Rodenbough PP, et al. Use of thermal melt curves to assess the quality of enzyme preparations. Anal Biochem 2010;399(2):268-75
  • Kopec J, Schneider G. Comparison of fluorescence and light scattering based methods to assess formation and stability of protein–protein complexes. J Struct Biol 2011;175(2):216-23
  • Senisterra GA, Finerty JPJ. High throughput methods of assessing protein stability and aggregation. Mol Biosyst 2009;5(3):217-23
  • Bershtein S, Mu W, Serohijos AW, et al. Protein quality control acts on folding intermediates to shape the effects of mutations on organismal fitness. Mol Cell 2013;49(1):133-44
  • Brandts JF, Lin LN. Study of strong to ultratight protein interactions using differential scanning calorimetry. Biochemistry 1990;29(29):6927-40
  • Layton CJ, Hellinga HW. Quantitation of protein-protein interactions by thermal stability shift analysis. Protein Sci 2011;20(8):1439-50
  • Zubriene A, Matuliene J, Baranauskiene L, et al. Measurement of nanomolar dissociation constants by titration calorimetry and thermal shift assay - radicicol binding to Hsp90 and ethoxzolamide binding to CAII. Int J Mol Sci 2009;10(6):2662-80
  • Holdgate GA. Thermodynamics of binding interactions in the rational drug design process. Expert Opin Drug Discov 2007;2(8):1103-14
  • Cooper A, Johnson CM, Lakey JH, Nollmann M. Heat does not come in different colours: entropy-enthalpy compensation, free energy windows, quantum confinement, pressure perturbation calorimetry, solvation and the multiple causes of heat capacity effects in biomolecular interactions. Biophys Chem 2001;93(2-3):215-30
  • Holdgate GA, Ward WH. Measurements of binding thermodynamics in drug discovery. Drug Discov Today 2005;10(22):1543-50
  • Sancho J. The stability of 2-state, 3-state and more-state proteins from simple spectroscopic techniques.. plus the structure of the equilibrium intermediates at the same time. Arch Biochem Biophys 2013;531(1-2):4-13
  • Weber PC, Salemme FR. Applications of calorimetric methods to drug discovery and the study of protein interactions. Curr Opin Struct Biol 2003;13(1):115-21
  • Goldberg DS, Bishop SM, Shah AU, Sathish HA. Formulation development of therapeutic monoclonal antibodies using high-throughput fluorescence and static light scattering techniques: role of conformational and colloidal stability. J Pharm Sci 2011;100(4):1306-15
  • Li Y, Mach H, Blue JT. High throughput formulation screening for global aggregation behaviors of three monoclonal antibodies. J Pharm Sci 2011;100(6):2120-35
  • He F, Hogan S, Latypov RF, et al. High throughput thermostability screening of monoclonal antibody formulations. J Pharm Sci 2010;99(4):1707-20
  • King AC, Woods M, Liu W, et al. High-throughput measurement, correlation analysis, and machine-learning predictions for pH and thermal stabilities of Pfizer-generated antibodies. Protein Sci 2011;20(9):1546-57
  • Rettig W. Charge separation in excited states of decoupled systems: TICT compounds and implications regarding the development of new laser dyes and the primary process of vision and photosynthesis. Angew Chem Int Ed Engl 1986;25(11):971-88
  • Yu W, Smil D, Li F, et al. Bromo-deaza-SAH: a potent and selective DOT1L inhibitor. Bioorg Med Chem 2013;21(7):1787-94
  • Parks DJ, Lafrance LV, Calvo RR, et al. 1,4-Benzodiazepine-2,5-diones as small molecule antagonists of the HDM2-p53 interaction: discovery and SAR. Bioorg Med Chem Lett 2005;15(3):765-70
  • Wassman CD, Baronio R, Demir Ö, et al. Computational identification of a transiently open L1/S3 pocket for reactivation of mutant p53. Nat Commun 2013;4:1407
  • Senisterra G, Wu H, Allali-Hassani A, et al. Small-molecule inhibition of MLL activity by disruption of its interaction with WDR5. Biochem J 2013;449(1):151-9
  • Wahlberg E, Karlberg T, Kouznetsova E, et al. Family-wide chemical profiling and structural analysis of PARP and tankyrase inhibitors. Nat Biotech 2012;30(3):283-8
  • Small Molecule Inhibitors of FGF22-Mediated Excitatory Synaptogenesis & Epilepsy Measured in Biochemical System Using RT-PCR - 7012-01_Inhibitor_SinglePoint_HTS_Activity - BioAssay Summary, AID651658. 2012. Available from: http://pubchem.ncbi.nlm.nih.gov/assay/assay.cgi?aid=651658
  • Molinski S, Eckford PD, Pasyk S, et al. Functional rescue of F508del-CFTR using small molecule correctors. Front Pharmacol 2012;3:160
  • Boyd RE, Lee G, Rybczynski P, et al. Pharmacological chaperones as therapeutics for lysosomal storage diseases. J Med Chem 2013;56(7):2705-25
  • Sampson Heidi M, Robert R, Liao J, et al. Identification of a NBD1-binding pharmacological chaperone that corrects the trafficking defect of F508del-CFTR. Chem Biol 2011;18(2):231-42
  • Maegawa GHB, Tropak MB, Buttner JD, et al. Identification and characterization of ambroxol as an enzyme enhancement agent for Gaucher disease. J Biol Chem 2009;284(35):23502-16
  • Marugan JJ, Zheng W, Motabar O, et al. Evaluation of quinazoline analogues as glucocerebrosidase inhibitors with chaperone activity. J Med Chem 2011;54(4):1033-58
  • Patnaik S, Zheng W, Choi JH, et al. Discovery, structure–activity relationship, and biological evaluation of noninhibitory small molecule chaperones of glucocerebrosidase. J Med Chem 2012;55(12):5734-48
  • McDevitt CA, Ogunniyi AD, Valkov E, et al. A molecular mechanism for bacterial susceptibility to zinc. PLoS Pathog 2011;7(11):e1002357
  • Jakobi AJ, Mashaghi A, Tans SJ, Huizinga EG. Calcium modulates force sensing by the von Willebrand factor A2 domain. Nat Commun 2011;2:385
  • Buysschaert G, Verstraete K, Savvides SN, Vergauwen B. Structural and biochemical characterization of an atypical short-chain dehydrogenase/reductase reveals an unusual cofactor preference. FEBS J 2013;280(5):1358-70
  • Niesen FH, Schultz L, Jadhav A, et al. High-affinity inhibitors of human NAD+-dependent 15-hydroxyprostaglandin dehydrogenase: mechanisms of Inhibition and structure-activity relationships. PLoS ONE 2010;5(11):e13719
  • Park J, Lin Y-S, De Schutter J, et al. Ternary complex structures of human farnesyl pyrophosphate synthase bound with a novel inhibitor and secondary ligands provide insights into the molecular details of the enzyme's active site closure. BMC Struct Biol 2012;12(1):32
  • Auld DS, Lovell S, Thorne N, et al. Molecular basis for the high-affinity binding and stabilization of firefly luciferase by PTC124. Proc Natl Acad Sci USA 2010;107(11):4878-83
  • Auld DS, Thorne N, Maguire WF, Inglese J. Mechanism of PTC124 activity in cell-based luciferase assays of nonsense codon suppression. Proc Natl Acad Sci USA 2009;106(9):3585-90
  • Auld DS, Thorne N, Nguyen DT, Inglese J. A specific mechanism for nonspecific activation in reporter-gene assays. ACS Chem Biol 2008;3(8):463-70
  • Lea WA, Simeonov A. Differential scanning fluorometry signatures as indicators of enzyme inhibitor mode of action: case study of glutathione S-transferase. PLoS One 2012;7(4):e36219
  • Torres FE, Recht MI, Coyle JE, et al. Higher throughput calorimetry: opportunities, approaches and challenges. Curr Opin Struct Biol 2010;20(5):598-605
  • Vedadi M, Arrowsmith CH, Allali-Hassani A, et al. Biophysical characterization of recombinant proteins: a key to higher structural genomics success. J Struct Biol 2010;172(1):107-19

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