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doi: 10.1046/j.1365-2265.1998.00501.x

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Volume:30 ML

Glossary Abbreviations α cooperativity Å Angstrom AlphaLISA amplified luminescent proximity homogeneous assay-linked immunosorbent assay BET Bromodomain and Extra-Terminal motif BD bromodomain BIRC baculoviral IAP repeat containing protein BLI Biolayer interferometry Brd bromodomain-containing protein BRET bioluminescence resonance energy transfer BRlogD biologically relevant logD BTK Bruton’s tyrosine kinase CAPA chloroalkane penetration assay CDK cyclin-dependent kinase CDO1 cysteine dioxygenase type 1 CETSA cellular thermal shift assay Chamelogk chameleonicity metric CharVol characteristic volume CHI chromatographic hydrophobicity index cIAP cellular inhibitor of apoptosis protein CRBN cereblon CRL2 VHL VHL cullin 2 RING E3 ubiquitin ligase CRL4 CRBN CRBN cullin 4 RING E3 ubiquitin ligase cryo-EM cryo-electron microscopy Cul Cullin protein ΔH enthalpy ΔG free energy ΔS entropy Da Dalton(s) DDA1 DET1 and DDB1 associated protein 1 DDB1 damage specific DNA binding protein 1 DC50 half-maximal degradation constant DCAF DDB1 and Cul4 associated factor DLS dynamic light scattering D max maximum degradation efficacy value DNA DNA DSF differential scanning fluorimetry E1 E1 ubiquitin-activating enzymes E2 E2 ubiquitin-conjugating enzymes E3 E3 ubiquitin ligases eloB elongin B eloC elongin C EMSA electrophoretic mobility shift assay EPSA experimental polar surface area ER estrogen receptor FEM1C FEM-1 homologue C protein FIDA flow-induced dispersion analysis FITC fluorescein fluoPPi fluorescent PPi FP fluorescence polarization FPS fluorescence proximity sensing FRET Förster resonance energy transfer GFP green fluorescent protein GSPT1 G1 to S phase transition protein 1 GST glutathione S-transferase HADDOCK high-ambiguity driven docking HaloTag haloalkane dehalogenase-tagged HBA and hydrogen bond acceptor HBD number of hydrogen bond donor HDX-MS hydrogen–deuterium exchange mass spectrometry HEK human embryonic kidney HIF-1 hypoxia inducible factor 1 HPLC high-performance liquid chromatography IAM immobilized artificial membrane IC50 half-maximal concentration of inhibition ITC isothermal calorimetry Ka association constant K d dissociation constant K i inhibitor constant KLHDC2 Kelch domain-containing protein 2 koff off-rate kon on-rate LC/MS liquid chromatography/mass spectrometry LED light-emitting diode Log D lipophilicity distribution coefficient of ionizable compounds LogP lipophilicity partition coefficient LPE lipophilic permeability efficiency LRRK2 leucine rich repeat kinase 2 MDCK Madin-Darby canine kidney MST microscale thermophoresis MW molecular weight m / z mass-to-charge ratio N stoichiometry coefficient NanoLuc nanoluciferase nDSF nanoDSF NMR nuclear magnetic resonance nMS native mass spectrometry NRotB number of rotatable bonds P polarity PAMPA parallel artificial membrane permeability assay Papp apparent permeability PPi protein–protein interaction PROTAC proteolysis targeting chimera PSSM position-specific scoring matrix PWM positional weighted matrix RBM39 RNA-binding motif protein 39 RBR RING-Between-RING Rbx RING box protein RF random forest RING really interesting new gene RRCK MDCK-clone Ralph-Russ canine kidney S solubility SAR structure–activity relationships SASA solvent-accessible surface area SAXS small-angle X-ray scattering SDS-PAGE sodium dodecyl sulfate-polyacrylamide gel electrophoresis SEC size exclusion chromatography SILAC stable isotope labeling by amino acids in cell culture smFRET single molecule FRET SOCS suppressor of cytokine signaling SPPIER separation of phases-based protein interaction reporter SpS spectral shift assay SPR surface plasmon resonance ssDNA single-stranded DNA STAT signal transducer and activator of transcription t1/2 half-life TAMRA tetramethylrhodamine TDA thermal denaturation assay TEC tyrosine protein kinase TPD targeted protein degradation TPSA total polar surface area TR-FRET time-resolved Förster resonance energy transfer TRIP12 thyroid hormone receptor interactor 12 TSA thermal shift assays TUBE tandem ubiquitin binding entity Ub ubiquitin UbC50 half-maximal concentration of ubiquitination Ubmax maximum conversion to ubiquitinated substrate UPS ubiquitin proteasome system VCB pVHL-eloB-eloC complex VHL von Hippel-Lindau WDR5 WD repeat-containing protein 5 Biographies Charlotte Crowe is a postdoctoral research associate in the Centre for Targeted Protein Degradation at the University of Dundee