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Cys-X scanning for expansion of active-site residues and modulation of catalytic functions in a glutathione transferase

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Size:100 Gram (165 Servings)

ABBREVIATIONS ACHC aminocyclohexanecarboxylic acid ACN acetonitrile ACPC aminocyclopentanecarboxylic acid ADT 2-aryl-4,5-dihydrothiazole AI artificial intelligence Aib α -aminoisobutyric acid AKAP A-kinase-anchoring protein AKB protein kinase A binding domain Akt protein kinase B Ala Alanine AML1-ETO acute myeloid leukemia 1 protein-ETO fusion protein Aoc aminooctanoic acid APP amyloid precursor protein Arg arginine ARNT aryl hydrocarbon receptor nuclear translocator ASF1 antisilencing function 1 protein Asp aspartic acid ATC 4-amino(methyl)-1,3-thiazole-5-carboxylic acids BAD BCL-2 associated agonist of cell death BAK BCL-2 homologous antagonist killer protein BCL-2 B-cell lymphoma 2 BCL9 B-cell CLL/lymphoma 9 protein BCL-X L B-cell lymphoma extra large BCP bicyclic peptide BEAS-2B human bronchial epithelium cell line, non-tumorigenic BH3 BCL-2 homology domain 3 bHLH basic helix–loop–helix BID BH3 interacting-domain death agonist BIM BCL-2 interacting mediator of cell death Boc tert -butyl carbamate B-Raf serine/threonine protein kinase Bts benzothiazole-2-sulfonyl bZIP basic leucine zipper CAL CFTR-associated ligand cAMP adenosine 3,5-cyclic monophosphate CBP CREB binding protein CD circular dichroism CD137 tumor necrosis factor receptor CDR complementarity determining regions CFTR cystic fibrosis transmembrane conductance regulator CHD cross-linked helix dimers ChIP chromatin immunoprecipitation CHIP C-terminus of Hsc70 interacting protein cIAP1 cellular inhibitor of apoptosis protein 1 CPP cell-penetrating peptide CSL CBF1, suppressor of hairless, Lag-1 (transcription factor in the Notch pathway) CTAD C-terminal transactivation domain CtBP C-terminal binding protein transcriptional repressor CuAAC copper catalyzed azide alkyne cycloaddition Cys cysteine Dap (S)-2,3-diaminopropanoic acid DARPins designed ankyrin repeat proteins DBD DNA binding domain DCM dichloromethane Dcp2 mRNA decapping enzyme Ddz α , α -dimethyl-3,5-dimethoxybenzylcarbonyl DEL DNA-encoded library DEP1 receptor-like protein tyrosine phosphatase DIAD diisopropyl azodicarboxylate DIC N,N’ -diisopropylcarbodiimide DIPEA N,N’ -diisopropylethylamine DMF dimethylformamide DMSO dimethyl sulfoxide DNA DNA DTS DNA templated synthesis E-Box enhancer box ECRV E-cadherin region V EED embryonic ectoderm development protein EGFR epidermal growth factor receptor ELISA enzyme linked immunosorbent assay EphA2 Ephrin type-A receptor 2 Eps15 epidermal growth factor receptor pathway substrate 15 ERK extracellular signal regulated kinase ER α estrogen receptor alpha EZH2 enhancer of zeste homologue 2 FIP Rab11-family interacting proteins FIT flexible in vitro translation FITC fluorescein isothiocyanate Fmoc fluorenylmethoxycarbonyl FP fluorescence polarization GABARAP GABA type A receptor associated protein Gag group-specific antigen GAP GTPase activating protein GEM guanine-nucleotide exchange modulator Gln glutamine GLP-1 glucagon like peptide 1 Glu glutamate Gly glycine Gly-mal glycine maleimide gp41 glycoprotein 41 GPCR G protein coupled receptor GTP guanosine-5′-triphosphate HBS hydrogen bond surrogate HBTU hexafluorophosphate benzotriazole tetramethyl uronium HCT116 human epithelial cell line HCTU O-(1H-6-Chlorobenzotriazole-1-yl)-1,1,3,3-tetramethyluronium hexafluorophosphate HDAC histone deacetylase hDM2 human double minute 2 protein (E3 ubiquitin ligase) HER3 human epidermal growth factor receptor 3 hIAPP human islet amyloid polypeptide HIF1 α hypoxia induced factor 1 subunit alpha HIF1 β hypoxia induced factor 1 subunit beta, encoded by ARNT HIV-1 human immunodeficiency virus HOBt hydroxybenzotriazole HPLC-MS high performance liquid chromatography - mass spectrometry HR2 heptad repeat 2 HRE hypoxia-response element hTEAD human transcriptional enhanced associate domain ICAT inhibitor of β -catenin and TCF-4 protein ICN1 intracellular domain of Notch1 IDE insulin degrading enzyme IDOL inducible degrader of low-density lipoprotein receptor (LDLR) IDR intrinsically disordered region IEDDA inverse electron demand Diels–Alder Ipa isophthalic acid IKK- β inhibitor of nuclear factor kappa B subunit beta IL-1 interleukin 1 IN integrase JM juxtamembrane KDM7 lysine demethylase 7 KEAP1 Kelch-like ECH-associated protein 1 KOTMS potassium trimethylsilanolate K-Ras Kirsten rat sarcoma virus LC-MS liquid chromatography-mass spectrometry LEDGF lens epithelium-derived growth factor Leu leucine Lys lysine mAb monoclonal antibody MAML1 mastermind like transcriptional coactivator 1 MAR matrix associated region MAX MYC-associated factor X MCD mast cell degranulation MCL-1 myeloid leukemia cell differentiation protein MCP macrocyclic peptides MDA-MB-231 triple negative breast cancer cell line MDM2 mouse double minute 2 MEG2 protein tyrosine phosphatase Met methionine ML machine learning Mmt monomethoxytrityl MOrPH-PhD macrocyclic organo-peptide hybrid phage display MP microporous mRNA messenger ribonucleic acid MT1-MMP membrane type 1 - matrix metalloproteinase MTA1 metastasis-associated protein 1 MYC bHLH transcription factor, oncogene MyD88 Myeloid differentiation primary response 88 N2B NHR2-binding motif ncAA noncanonical amino acids NCKAP1 NCK associated protein 1 NEMO NF-kappa-B essential modulator NFAT nuclear factor of activated T cells NHR2 Nervy homology two domain NHR-TF nuclear hormone receptor transcription factor NK- κ B nuclear factor kappa B NMR nuclear magnetic resonance iNOS inducible nitric oxide synthetase nNOS neuronal nitric oxide synthetase NOTCH1 neurogenic locus notch homologue protein 1 NOXA-2 phorbol-12-myristate-13-acetate-induced protein 1 (pro-apoptotic BH3 only protein) NRF2 nuclear factor erythroid 2-related factor NRPS nonribosomal peptide synthetase OBOC one bead one compound OBTC one bead two compound OHM oxopiperazine compounds OLIG2 oligodendrocyte transcription factor OSu oxysuccinimide p300 histone acetyltransferase p53 tumor suppressor PA-1 ovarian tetracarcinoma cell line PANC-1 pancreatic carcinoma cell line pAuNP poly-l-lysine coated gold nanoparticle PBS phosphate buffered saline PCSK9 proprotein convertase subtilisin/kexin type 9 PDB protein data bank PDZ structural domain PEPTIC peptide exploration platform with Tag-free intramolecular chemistry Phe phenylalanine PKA protein kinase A PKC protein kinase C PLSR partial least-squares regression PNA peptide nucleic acid POI protein of interest PolyUb polyubiquitin PPI protein–protein interaction PPIA peptidylprolyl cis–trans isomerase PRL2 phosphatase of regenerating liver 2 Pro proline PROTAC proteolysis targeting chimera PS polystyrene PSA polar surface area PSD-95 postsynaptic density protein PTP1B protein tyrosine phosphatase PURE protein synthesis using recombinant elements Rab Ras associated binding protein RaPID random nonstandard peptide integrated discovery RCM ring closing metathesis REU Rosetta energy units RGS4 regulator of G protein signaling 4 RMSD root-mean-square deviation RNA ribonucleic acid RRM RNA-recognition motifs RSV respiratory syncytial virus RT-PCR real time polymerase chain reaction RuAAC ruthenium catalyzed azide alkyne cycloaddition SAH stabilized α helix SAR structure activity relationship SBDD structure-based drug design Seq sequencing Ser serine SH2 Src homology 2 SHA shavenoid SICLOPPS split intein circular ligation of peptides and proteins SIRT2 sirtuin 2 SJSA-1 osteosarcoma fibroblast SMAD7 Mothers against decapentaplegic homologue 7 SOS1 son of sevenless homologue 1 SPAAC strain promoted azide alkyne cycloaddition SPPS solid phase peptide synthesis SPR surface plasmon resonance SPSB2 SPRY domain-containing SOCS box protein 2 SRC2 steroid receptor coactivator 2 STAT3 signal transducer and activator of transcription 3 STING stimulator of interferon genes adaptor protein STR synthetic transcriptional repressors SUPR scanning unnatural protease resistant tACBC trans-2-aminocyclobutanecarboxylic acid TAMM 2-((alkylthio)(aryl)methylene)malononitrile TAR transactivation binding response TATA 1,3,5-triacryloyl-1,3,5-triazinane TBAB N,N ′ ,N” -(benzene-1,3,5-triyl)-tris(2-bromoacetamide) TBMB 1,3,5-tris(bromomethyl)benzene TCEP tris(2-carboxyethyl)phosphine TCF T-cell factor TEAD1 transcriptional enhancer factor 1 TET1 ten-11 translocation methylcytosine dioxygenase1 TF transcription factor TFA trifluoroacetic acid TFAP4 transcription factor AP-4 TGF- β transforming growth factor beta THF tetrahydrofuran Thr threonine TIS triisopropylsilane TLR toll-like receptor TNBC triple negative breast cancer TNKS tankyrase Trp tryptophan TSG101 tumor susceptibility gene ULM U2AF ligand motifs uPA urokinase-type plasminogen activator uPAR uPA receptor UPRE unfolded protein response element UTR untranslated region Val valine VDR vitamin D receptor VEGF vascular endothelial growth factor vFLIP viral FLICE inhibitory proteins VGL4 vestigial-like protein 4 WNT wingless/Int1 signaling pathway XBP1 X-box binding protein 1 XIAP X-linked inhibitor of apoptosis protein YAP1 Yes1 associated transcriptional regulator γ -AA γ -substituted N -acylated- N -aminoethyl amino acids Biographies Colin S