Keywords: Biphalin; Opioid receptors; MOR/DOR/KOR agonist; Synergistic analgesic effect; Cyclic peptides; Acm; acetamidomethyl; ACN; acetonitrile; BBB; blood brain barrier; Boc; t-butyloxycarbonyl; BOP; (benzotriazol-1-yloxytris(dimethylamino)phosphonium hexafluoro
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Keywords: ABD3; albumin-binding domain 3; ACN; acetonitrile; AUC; area under the curve; BA; bioavailability; cAMP; cyclic adenosine monophosphate; CHO; Chinese hamster ovary; DIEA; diisopropyl ethylene diamine; Cmax; peak plasma concentration; CLp; plasma clearance
Keywords: AMPs; antimicrobial peptides; TOAC; 2,2,6,6-tetramethyl-piperidine-1-oxyl-4-amino-4-carboxylic acid; HPLC; high performance liquid chromatography; HBTU; O-Benzotriazole-N,N,N',N'-tetramethyl-uronium-hexafluoro-phosphate; TFA; trifluoroacetic acid; TIS; tr
The organic chemistry of poly(1H-pyrazol-1-yl)methanes
Keywords: AIBN; azobisisobutyronitrile; CAN; Ceric ammonium nitrate; DFT; Density functional theory; GIAO; Gauge-including atomic orbital; HBTU; 2-(1H-benzotriazol-1-yl)-1,1,3,3-tetramethyluronium hexafluorophosphate; HSAB; Hard and soft acids and bases; LiHMDS; Li
Keywords: BBB; blood brain barrier; BK; bradykinin; Boc; t-butyloxycarbonyl; BR; bradykinin receptor; CNS; central nervous system; DALKD; [des-Arg10, Leu9]-kallidin; DIPEA; diisopropylethylamine; DMF; N,N-dimethylformamide; Dyn A; dynorphin A; Fmoc; fluorenylmethyl
Keywords: CD; circular dichroism; CPE; cytopathic effect; DMF; dimethylformamide; FBS; fetal bovine serum; Fmoc; 9-fluorenylmethoxycarbonyl; HBTU; O-benzotriazole-N,N,Nâ²,Nâ²-tetramethyl-uronium-hexafluorophosphate; HOBt; N-hydroxybenzotriazole; HPLC; high perfor
Keywords: ACN; Acetonitrile; AFM; Atomic force microscopy; CNPE; Carbon nanotube paste electrode; CNT; Carbon nanotube; CPE; Carbon paste electrode; CS; Chitosan; CV; Cyclic voltammetry; DMF; Dimethylformamide; DNA; Deoxyribonucleic acid; DPV; Differential pulse vo
Keywords: ATX/NPP2; autotaxin; DIPEA; N,N-diisopropylethylamine; DMF; N,N-dimethylformamide; DMSO; dimethylsulfoxide; GPCR; G-protein coupled receptor; GRI; Genomic Research Institute; HBTU; O-(benzotriazol-1-yl)-N,N,Nâ²,Nâ²-tetramethyluronium hexafluorophosphate
Keywords: MeCN; acetonitrile; CL; clearance; Dess-Martin periodinane; 1,1,1-tris(acetyloxy)-1,1-dihydro-1,2-benziodoxol-3-(1H)-one; DIBALH; diisobutylaluminum hydride; DMF; N,N-dimethylformamide; EtOAc; ethyl acetate; HBTU; N,N,Nâ²,Nâ²-tetramethyl-O-(1H-benzotr
Keywords: Cyclic peptides; Microwave assisted synthesis; Lactam-bridge cyclic peptides; SHU9119; MTII; MWA-SPPS; microwave-assisted solid phase peptide synthesis; MBHA; methylbenzhydryl; MCR; melanocortin receptors; NDP; [Nle4, DPhe7]-αMSH; MTII; melanotan-II; RP-
Keywords: Ac; acetyl; ACTH; adrenocorticotropic hormone; Alloc; allyloxycarbonyl; Boc; t-butoxycarbonyl; BSA; bovine serum albumin; DIC; N,Nâ²,-diisopropylcarbodiimide; DIEA; diisopropylethylamine; DMEM; Dulbecco's Modified Eagle Medium; DMF; N,N-dimethylformami
Keywords: Influenza; Virus; Neuraminidase; Inhibitor; Pharmacokinetics; Molecular modeling; BQLKEXSYWRBWQK-AFMQGRBTSA-N; AUC; area under the concentration-versus-time curve; CC50; 50% cytotoxicity concentration; CL; clearance; CPE; cytopathic effect; D; distributio
Keywords: AMPs; antimicrobial peptides; ATCC; American type culture collection; CD; circular dichroism; CFU; colony forming units; CLSI; Clinical and Laboratory Standards Institute; DIPEA; N,N-diisopropylethylamine; DMEM; Dulbecco's modified eagle's medium; DMF; N,
Microcystins: Synthesis and structure-activity relationship studies toward PP1 and PP2A
Keywords: Adda; (2S,3S,8S,9S)-3-amino-9-methoxy-2,6,8-trimethyl-10-phenyldeca-4,6-dienoic acid; Amba; (2S,3S)-3-amino-2-methylbutanoic acid; Boc; tert-butoxycarbonyl; BOP; benzotriazol-1-yloxy-tris-dimethylaminophosphoniumhexafluoro phosphate; Cbz; carboxybenzyl; D
Synthesis and biological evaluation of a library of hybrid derivatives as inhibitors of influenza virus PA-PB1 interaction
Keywords: Anti-Influenza; PA-PB1; RdRp; Amino acid coupling; SPPS; Diphenyl-pyridine; AcOEt; Ethyl acetate; CC50; Half maximal cytotoxic concentration; cRNA; complementar RNA; DCM; dichloromethane; DDQ; 2,3-Dichloro-5,6-dicyano-1,4-benzoquinone; DIPEA; N,N-Diisopro
Acylguanidine derivatives of zanamivir and oseltamivir: Potential orally available prodrugs against influenza viruses
Keywords: Acylguanidine; Zanamivir; Oseltamivir; Neuraminidase inhibitor; Influenza; Arg; arginine; Boc; tert-butoxycarbonyl; (Boc)2O; di(tert-butyl) dicarbonate; CC50; half maximal cytotoxicity concentration; CPE; cytopathic effect; DIEA; diisopropyl ethylamine; D
Enhanced antimalarial activity of plasmepsin V inhibitors by modification of the P2 position of PEXEL peptidomimetics
Keywords: Plasmepsin; Malaria; Protease; Peptidomimetic; PEXEL; Trafficking; Abu; aminobutyric acid; Cav; canavanine; CyHexGly; cyclohexylglycine; CyPenGly; cyclopentylglycine; EtNva; beta-ethyl-norvaline; GFP; green fluorescent protein; HBTU; O-(benzotriazol-1-yl)
Synthesis and biological evaluation of novel thiazole- VX-809 hybrid derivatives as F508del correctors by QSAR-based filtering tools
Keywords: Aminoarylthiazole; Corrector; QSAR; Cystic fibrosis; CFTR; VX809; CF; cystic fibrosis; CFTR; CF transmembrane conductance regulator; AATs; aminoarylthiazoles; HS-YFP; halide-sensitive yellow fluorescent protein; QSAR; quantitative-structure activity relat
Phenylglycine racemization in Fmoc-based solid-phase peptide synthesis: Stereochemical stability is achieved by choice of reaction conditions
Keywords: COMU; (1-cyano-2-ethoxy-2-oxoethylidenaminooxy)dimethylaminomorpholinocarbenium hexafluorophosphate; DBU; 1,8-diazabicyclo[5.4.0]undec-7-ene; DEPBT; 3-diethoxyphosphoryloxy)-1,2,3-benzotriazin-4(3H)-one; DIPEA; N,N-diisopropylethylamine; DMF; N,N-dimethyl
PNA monomers fully compatible with standard Fmoc-based solid-phase synthesis of pseudocomplementary PNA
Keywords: Bhoc; benzhydryloxycarbonyl; HBTU; 1-[bis(dimethylamino)methylene]-1H-benzotriazolium hexafluorophosphate 3-oxide; PyAOP; 7-azabenzotriazol-1-yl-N-oxy-tris(pyrrolidino)-phosphonium hexafluorophosphate; Peptide nucleic acid; Strand invasion; Pseudocompleme
Synthesis and biological evaluation of Santacruzamate-A based analogues
Keywords: AcCN; acetonitrile; BnOH; benzyl alcohol; DMF; N,N-dimethylformamide; DMSO; dimethylsulphoxide; EtOAc; ethyl acetate; EtOH; ethanol; GABA; γ-aminobutyric acid; GADPH; glyceraldehyde 3-phosphate dehydrogenase; HBTU; O-(benzotriazol-1-yl)-N,N,Nâ²,Nâ²-tet
Comparison of extracellular Cys/Trp motif between Schizosaccharomyces pombe Ctr4 and Ctr5
Keywords: Ctr; copper transporter; BCA; bicinchoninic acid; Fmoc; 9-fluorenylmethyloxycarbonyl; NMP; N-methylpyrrolidone; HBTU; 2-(1H-benzotriazol-1-yl)-1,1,3,3-tetramethyluronium hexafluorophosphate; HOBt; 1-hydroxybenzotriazol; DIEA; N,N-diisopropylethylamine; DM
Insights into amyloid-like aggregation of H2 region of the C-terminal domain of nucleophosmin
Keywords: TIS; Triisopropylsilane; TFA; Trifluoroacetic acid; DMF; Dimethylformamide; HBTU; 1-H-Benzotriazolium, 1-[bis(dimethylamino)methylene]-Hexafluorophosphate(1-),3 oxide; HOBt; N-hydroxybenzotriazole; DIEA; Di-isopropylethylamine; Fmoc; Fluorenylmethoxycarbo
Bivalent SIRT1 inhibitors
Keywords: β-NAD+; β-nicotinamide adenine dinucleotide; NAM; nicotinamide; 2â²-O-AADPR; 2â²-O-acyl-ADP-ribose; RP-HPLC; reversed-phase high performance liquid chromatography; HRMS; high-resolution mass spectrometry; EDC-MeI; 1-(3-dimethylaminopropyl)-3-ethylcarb
Ser422 phosphorylation blocks human Tau cleavage by caspase-3: Biochemical implications to Alzheimer's Disease
Keywords: Aa; amino acid; ACN; acetonitrile; AUFS; absorbance units full scale; CHCA; 1-Cyano 4-Hydroxy Cinnamic Acid; Da; Dalton; DHB; 2,5-dihydroxy benzoic acid; DMF; N,Nâ²-dimethyl formamide; EDT; ethane dithiol; h; human; HATU; 1-[Bis(dimethylamino)methylene]-
Design, synthesis and pharmacological evaluation of 4-hydroxyphenylglycine and 4-hydroxyphenylglycinol derivatives as GPR88 agonists
Keywords: 2-PCCA; (1R,2R)-2-(pyridin-2-yl)cyclopropane carboxylic acid ((2S,3S)-2-amino-3-methylpentyl)-(4â²-propylbiphenyl-4-yl)amide; 2-AMPP; (2S)-N-((1R)-2-amino-1-(4-(2-methyl-pentyloxy)phenyl)ethyl)-2-phenylpropanamide; SAR; structure activity relationship; P
Stereoselective synthesis of modified cysteines
Keywords: Alloc; allyloxycarbonyl; Ar; aryl; Bn; benzyl; Cbz; benzyloxycarbonyl; Cbz-OSu; benzyloxycarbonylsuccinimide; NBS; N-bromosuccinimide; Boc; tert-butoxycarbonyl; m-CPBA; m-chloroperbenzoic acid; DABCO; 1,4-diazabicyclo[2.2.2]octane; DBU; 1,8-diazabicyclo[5
Synthesis of novel 15-membered 8a-azahomoerythromycin A acylides: Consequences of structural modification at the C-3 and C-6 position on antibacterial activity
Keywords: Macrolide antibiotics; Macrolide resistance; Acylides; Structure-activity relationships; Antibacterial activity; Heck reaction; MLSB; macrolide-lincosamide-streptogramin B; Mef; macrolide efflux; SAR; structure-activity relationships; DABCO; 1,4-diazabicy
Inhibition of amyloid fibril formation and cytotoxicity by caffeic acid-conjugated amyloid-β C-terminal peptides
Keywords: Aβ; amyloid-β; AD; Alzheimer's disease; CA; caffeic acid; DCFH-DA; 2â²,7â²-dichlorodihydrofluorescein diacetate; DHCA; dihydrocaffeic acid; DIPEA; N,N-diisopropylethylamine; DMF; N,N-dimethylformamide; DMSO; dimethyl sulfoxide; Gly; glycine; HBTU; O
Cyclic peptide-based potent and selective SIRT1/2 dual inhibitors harboring Nε-thioacetyl-lysine
Keywords: β-NAD+; β-nicotinamide adenine dinucleotide; MBHA; 4-methylbenzhydrylamine; SPPS; solid phase peptide synthesis; DMF; N,N-dimethylformamide; TFA; trifluoroacetic acid; DCM; dichloromethane; HBTU; 2-(1H-benzotriazole-1-yl)-1,1,3,3-tetramethylaminium hexa
Isolation and characterization of a structurally unique β-hairpin venom peptide from the predatory ant Anochetus emarginatus
Keywords: RP-HPLC; reversed phase-high performance liquid chromatography; LC; liquid chromatography; MS; mass spectrometry; ACN; acetonitrile; TFA; trifluoroacetic acid; MALDI; matrix-assisted laser desorption/ionization; TOF; time-of-flight; FA; ferulic acid; DTT;
High stability and biological activity of the copper(II) complexes of alloferon 1 analogues containing tryptophan
Keywords: CD; Circular Dichroism Spectroscopy; DAPI; 4â²,6-diamidino-2-phenyloindole; DMF; N,N-dimethylformamide; DOPA; 3,4-dihydroxyphenylalanine; EPR; Electron Paramagnetic Resonance Spectroscopy; ESI-MS; Electrospray Ionization Mass Spectrometry; Fmoc; 9-fluo
Molecular interaction of δ-conopeptide EVIA with voltage-gated Na+ channels
Keywords: COSY; correlation spectroscopy; DG; distance geometry; DIEA; N,N-diisopropylethylamine; Fmoc; 9-fluorenylmethoxycarbonyl; GSH; glutathione reduced; GSSG; glutathione oxidized; HBTU; O-(benzotriazol-1-yl)-N,N,Nâ²,Nâ²-tetramethyl-uronium-hexafluorophospha
Modification of amphipathic non-opioid dynorphin A analogues for rat brain bradykinin receptors
Keywords: BK; bradykinin; BR; bradykinin receptor; CNS; central nervous system; DALKD; [des-Arg10,Leu9]-kallidin; DIPEA; diisopropylethylamine; DMF; N,N-dimethylformamide; Dyn A; dynorphin A; HR MS; high resolution mass spectroscopy; Fmoc; 9-fluorenylmethoxycarbony
Design and synthesis of novel bivalent ligands (MOR and DOR) by conjugation of enkephalin analogues with 4-anilidopiperidine derivatives
Keywords: ACN; Acetonitrile; Boc; tert-butyloxycarbonyl; CHO; Chinese hamster ovary; DCM; Dichloromethane; DIPEA; N,N-Diisopropylethylamine; DALEA; [D-Ala2, Leu5] enkephalin amide; DAMGO; [D-Ala2,NMePhe4,Gly5-ol]enkephalin; Dmt; 2,6-dimethyltyrosine; DPDPE; c[D-Pen
Structure-activity relationship study using peptide arrays to optimize Api137 for an increased antimicrobial activity against Pseudomonas aeruginosa
Keywords: Apidaecin; Gram-negative bacterium; Proline-rich antimicrobial peptide (PrAMP); Pseudomonas aeruginosa; SPOT synthesis; AMP; antimicrobial peptide; DIC; N,Nâ²-diisopropylcarbodiimide; DIPEA; N-ethyldiisopropylamine; DMAP; 4-dimethylaminopyridine; gu; N,N
Carbonic anhydrase inhibitors: Design, synthesis and structural characterization of new heteroaryl-N-carbonylbenzenesulfonamides targeting druggable human carbonic anhydrase isoforms
Keywords: Human carbonic anhydrase; Isoquinoline; Quinoline; X-ray; Molecular docking; AAZ; acetazolamide; CAs; carbonic anhydrases; HBTU; N,N,Nâ²,Nâ²-tetramethyl-O-(1H-benzotriazol-1-yl)uranium hexafluorophosphate; TMP; topiramate;
A novel synthetic luteinizing hormone-releasing hormone (LHRH) analogue coupled with modified β-cyclodextrin: Insight into its intramolecular interactions
Keywords: BOP; benzotriazole-1-yl-oxy-tris-(dimethylamino)-phosphonium hexafluorophosphate; CLTR-Cl; 2-chlorotrityl chloride; DCC; N,Nâ²-dicyclohexylcarbodiimide; DMA; dimethylacetamide; DIC; N,Nâ²-diisopropylcarbodiimide; DIEA; diisopropylethylamine; DMF; N,N-di
Specificity studies on Kallikrein-related peptidase 7 (KLK7) and effects of osmolytes and glycosaminoglycans on its peptidase activity
Keywords: KLK; kallikrein-related peptidase; FRET; fluorescence resonance energy transfer; MCA; 4-methyl coumarin-7-amide; Q-EDDnp; glutaminyl-[N-(2,4-dinitrophenyl)-ethylenediamine]; Abz; ortho-amino-benzoic acid; GAGs; glycosaminoglycans; HBTU; N,N,Nâ²,Nâ²-Tetr
Blood-brain transfer and antinociception of linear and cyclic N-methyl-guanidine and thiourea-enkephalins
Keywords: Blood-brain barrier (BBB) transport (influx/efflux); Antinociceptive activity; Linear/cyclic enkephalin analogs; In vivo mouse models; AUC; area under the curve; Alloc; allyloxycarbonyl; BBB; blood-brain barrier; Boc; tertButyloxycarbonyl; BSA; bovine
N-methylthioacetylation of RYYRIK-NH2 with enhanced specific binding affinity and high antagonist activity for nociceptin ORL1 receptor
Keywords: DTT; dithiothreitol; Fmoc; 9-fluorenylmethoxycarbonyl; GPCR; G protein-coupled receptor; HBTU; 2-(1H-benzotriazole-1-yl)-1,1,3,3-tetramethyluronium hexafluorophosphate; HOBt; 1-hydroxybenzotriazole; MALDI-TOF; matrix-assisted laser desorption ionization t
Tritium-labelled isovaleryl-RYYRIK-NH2 as potential antagonist probe for ORL1 nociceptin receptor
Keywords: Boc; butoxycarbonyl; Bmax; receptor density; DMEM; Dulbecco's Modified Eagle's Medium; DMF; N,N-dimethylformamide; FBS; fetal bovine serum; GPCR; G protein-coupled receptor; HBTU; 2-(1H-benzotriazole-1-yl)-1,1,3,3-tetramethyluronium hexafluorophosphat
A total synthesis of a highly N-methylated cyclodepsipeptide [2S,3S-Hmp]-aureobasidin L using solid-phase methods
Keywords: Aureobasidin; N-Methylated cyclodepsipeptide; Depsidipeptide; Fmoc-based solid-phase peptide synthesis; Boc; tert-butyloxycarbonyl; BTC; bis-(trichloromethyl)-carbonate; 13C NMR; carbon-13 nuclear magnetic resonance; COSY; correlation spectroscopy; DBU; 1
G-quadruplex DNA recognition by nucleophosmin: New insights from protein dissection
Keywords: TIS; Triisopropylsilane; TFA; Trifluoroacetic acid; DMF; Dimethylformamide; DCM; Dichloromethane; HBTU; 1-H-Benzotriazolium, 1-[bis(dimethylamino)methylene]-hexafluorophosphate(1-), 3 oxide; HOBt; N-hydroxybenzotriazole; DIEA; Di-isopropylethylamine; Fmoc
Gadolinium-based contrast agents targeted to amyloid aggregates for the early diagnosis of Alzheimer's disease by MRI
Keywords: Alzheimer's disease; Amyloid; Gadolinium; DOTA; Pyridine containing TriAza (PCTA); Magnetic resonance imaging (MRI); BAT; bis-amine-bis-thiol; BTA; 2-(4-N-methylaminophenyl)benzothiazole; CA; contrast agent; CMC; critic micelle concentration; CV; cone vol
N-terminal guanidinylation of TIPP (Tyr-Tic-Phe-Phe) peptides results in major changes of the opioid activity profile
Keywords: BBB; blood-brain barrier; Boc; tert-butyloxycarbonyl; Cl-HOBt; 6-chloro-1-hydroxybenzotriazole; DAMGO; H-Tyr-D-Ala-Gly-Phe(NMe)-Gly-ol; DIC; 1,3-diisopropylcarbodiimide; DIPP; H-Dmt-Tic-Phe-Phe-OH; DIPP-NH2; H-Dmt-Tic-Phe-Phe-NH2; DIPP-NH2[Ψ]; H-Dmt-Ti
Affinity-based screening of MDM2/MDMX-p53 interaction inhibitors by chemical array: Identification of novel peptidic inhibitors
Keywords: FAM; carboxyfluorescein; FP; fluorescence polarization; HBTU; O-(1H-benzotriazol-1-yl)-N,N,Nâ²,Nâ²-tetramethyluronium hexafluorophosphate; HOBt; 1-hydroxy-1H-benzotriazole; MDM2; mouse double minute 2 homolog; MDMX; mouse double minute X homolog; TAMRA;
Development of peptide inhibitor as a therapeutic agent against head and neck squamous cell carcinoma (HNSCC) targeting p38α MAP kinase
Keywords: MAPK; mitogen activated protein kinase; HNSCC; head and neck squamous cell carcinoma; MKK; MAPK kinase; MKKK; MKK kinase; LB; Luria-Bertani; IPTG; isopropyl-Ã-d-galactosidase; DLS; dynamic light scattering; ATF; activated transcription factor; NPP; 4-nit
Plasmodium falciparum synthetic LbL microparticle vaccine elicits protective neutralizing antibody and parasite-specific cellular immune responses
Keywords: CFA; complete Freund's adjuvant; CFSE; carboxyfluorescein succinimide ester; CS; circumsporozoite; DP; designed peptide; EDC; 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide; HBTU; 2-(1H-benzotriazol-1-yl)-1,1,3,3-tetramethyluronium hexafluorophosphate; IFA
The pro-apoptotic action of new analogs of the insect gonadoinhibiting peptide Neb-colloostatin: Synthesis and structure-activity studies
Keywords: Ach; 1-aminocyclohexane-1-carboxylic acid; Acp; 1-aminocyclopentane-1-carboxylic acid; CD; circular dichroism; DMF; dimethylformamide; EDT; 1,2-ethanedithiol; Fmoc; 9-fluorenylmethoxycarbonyl; HBTU; O-benzotriazole-N,N,Nâ²,Nâ²-tetramethyl-uronium-hexafl