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UiB
- E-postBengt-Erik.Haug@uib.no
- Telefon+47 55 58 34 68
- BesøksadresseAllégaten 41Realfagbygget5007 BergenRom3008
- PostadressePostboks 78035020 Bergen
Vi er interessert i forskningsspørsmål som ligger på grensesnittet mellom kjemi og biologi. Forskningsprosjektene vi er involvert i er forankret i legemiddelkjemi og biologisk kjemi, og vi bruker syntetisk organisk kjemi som metode for å addressere våre forskningsspørsmål. Flere av prosjektene vi jobber med krever også tilgang til syntetiske peptider, og gruppen har etablert og driver Laboratorium for peptidsyntese ved Kjemisk institutt. Besøk våre gruppesider for mer informasjon.
Vitenskapelig artikkel
- (2022). Identification of a phage display-derived peptide interacting with the N-terminal region of factor VII activating protease (FSAP) enables characterization of zymogen activation. ACS Chemical Biology. 2631-2642.
- (2021). Repurposing 18F-FMISO as a PET tracer for translational imaging of nitroreductase-based gene directed enzyme prodrug therapy. Theranostics. 6044-6057.
- (2021). CytoCy5S™, a compound of many structures. in vitro and in vivo evaluation of four near-infrared fluorescent substrates of nitroreductase (NTR). Dyes and pigments. 1-11.
- (2021). Comparison of Five Near-Infrared Fluorescent Folate Conjugates in an Ovarian Cancer Model. Molecular Imaging and Biology. 1-12.
- (2021). An Experimental Toolbox for Structure-Based Hit Discovery for P. aeruginosa FabF, a Promising Target for Antibiotics . ChemMedChem. 2715.
- (2020). Unequivocal structure confirmation of a breitfussin analog by anisotropic NMR measurements. Chemical Science. 12081-12088.
- (2020). Total synthesis of phorbazole B. Molecules. 1-10.
- (2019). Kinase chemodiversity from the Arctic: the breitfussins. Journal of Medicinal Chemistry. 10167-10181.
- (2018). Structural determinants and cellular environment define processed actin as the sole substrate of the N-terminal acetyltransferase NAA80. Proceedings of the National Academy of Sciences of the United States of America. 4405-4410.
- (2018). Aldol condensations on a 3-alkylidene-2,5-diketopiperazine - synthesis of two marine natural products. Synlett : Accounts and Rapid Communications in Synthetic Organic Chemistry. 1303-1306.
- (2017). Synthesis of a novel tripeptidomimetic scaffold and biological evaluation for CXC chemokine receptor 4 (CXCR4) antagonism. Tetrahedron. 3866-3877.
- (2017). Oncolytic peptide LTX-315 induces an immune-mediated abscopal effect in a rat sarcoma model. Oncoimmunology. 1-13.
- (2017). LTX-315: a first-in-class oncolytic peptide that reprograms the tumor microenvironment. Future Medicinal Chemistry. 1339-1344.
- (2017). Influence of chain length on the activity of tripeptidomimetic antagonists for CXC chemokine receptor 4 (CXCR4). Bioorganic & Medicinal Chemistry. 646-657.
- (2016). Discovery of a 9-mer cationic peptide (LTX-315) as a potential first in class oncolytic peptide. Journal of Medicinal Chemistry. 2918-2927.
- (2016). Crystal structure of the Golgi-associated human N-alpha acetyltransferase 60 (Naa60/NatF) reveals the molecular determinants for substrate-specific acetylation. Structure. 1044-1056.
- (2015). Pseudoaeruginosins, nonribosomal peptides in nodularia spumigena. ACS Chemical Biology. 725-733.
- (2015). Probing the molecular interactions between CXC chemokine receptor 4 (CXCR4) and an arginine-based tripeptidomimetic antagonist (KRH-1636). Journal of Medicinal Chemistry. 8141-8153.
- (2015). Discovery of a Specific Inhibitor of Pyomelanin Synthesis in Legionella pneumophila. Journal of Medicinal Chemistry. 8402-8412.
- (2015). A concise total synthesis of breitfussin A and B. Organic Letters. 122-125.
- (2014). Reversible ketomethylene-based inhibitors of human neutrophil proteinase 3. Journal of Medicinal Chemistry. 9396-9408.
- (2014). In silico design, synthesis, and assays of specific substrates for proteinase 3: Influence of fluorogenic and charged groups. Journal of Medicinal Chemistry. 1111-1115.
- (2014). Design, synthesis, and biological evaluation of scaffold-based tripeptidomimetic antagonists for CXC chemokine receptor 4 (CXCR4). Bioorganic & Medicinal Chemistry. 4759-4769.
- (2013). Synthesis and docking of novel piperidine renin inhibitors. Monatshefte für Chemie. 479-494.
- (2013). Nitroreductase, a near-infrared reporter platform for in vivo time-domain optical imaging of metastatic cancer. Cancer Research. 1276-1286.
- (2012). The relative spatial positions of tryptophan and cationic residues in helical membrane-active peptides determines their cytotoxicity. Journal of Biological Chemistry. 233-244.
- (2012). Interaction of local anaesthetic articaine enantiomers with brain lipids: A Langmuir monolayer study. European Journal of Pharmaceutical Sciences. 394-401.
- (2012). Debenzylation of Functionalized 4-and 5-substituted 1,2,3-fTriazoles. Synthesis (Stuttgart). 2070-2078.
- (2012). 1,3-Dipolar cycloaddition of benzyl azide to two highly functionalized alkynes. Monatshefte für Chemie. 505-512.
- (2011). Synthesis of trans-4-Triazolyl-Substituted 3-Hydroxypiperidines. Synthesis (Stuttgart). 749-754.
- (2011). Intramolecular hydrogen bonding in articaine can be related to superior bone tissue penetration: A molecular dynamics study. Biophysical Chemistry. 18-25.
- (2008). Synthetic antimicrobial peptidomimetics with therapeutic potential. Journal of Medicinal Chemistry. 4306-4314.
- (2008). Antimicrobial Peptides with Stability toward Tryptic Degradation. Biochemistry. 3777-3788.
- (2007). Application of the Suzuki-Miyaura cross-coupling to increase antimicrobial potency generates promising novel antibacterials. Bioorganic & Medicinal Chemistry Letters.
- (2005). Facile degradative lactonization of Gln-Arg and Gln-Phe hydroxyethylene dipeptide derivatives. Journal of Peptide Research.
- (2004). Synthesis of a Gln-Phe hydroxyethylene dipeptide isostere. Organic Letters. 4783-4786.
- (2004). Bulky nonproteinogenic amino acids permit the design of very small and effective cationic antibacterial peptides. Journal of Medicinal Chemistry. 4159-4162.
- (2003). The Pharmacophore of Short Cationic Antibacterial Peptides. Journal of Medicinal Chemistry. 1567-1570.
- (2003). Enhanced antitumor activity of 15-residue bovine lactoferricin derivatives containing bulky aromatic amino acids and lipophilic N-terminal modifications. Journal of Peptide Science. 510-517.
- (2002). Synthesis of a 2-arylsulphonylated tryptophan: the antibacterial activity of bovine lactoferricin peptides containing Trp(2-Pmc). Journal of Peptide Science. 307-313.
- (2002). Simple parameterization of non-proteinogenic amino acids for QSAR of antibacterial peptides. Journal of Peptide Science. 302-306.
- (2001). The effects of charge and lipophilicity on the antibacterial activity of undecapeptides derived from bovine lactoferricin. Journal of Peptide Science. 425-432.
- (2001). The Role of Tryptophan in the Antibacterial Activity of a 15-Residue Bovine Lactoferricin Peptide. Journal of Peptide Science. 190-196.
- (2001). Important structural features of 15-residue lactoferricin derivatives and methods for improvement of antimicrobial activity. International Journal of Biochemistry and Cell Biology.
- (2001). Bulky Aromatic Amino Acids Increase the Antibacterial Activity of Bovine Lactoferricin Peptides. Journal of Peptide Science. 425-432.
- (2000). Fargestoffer i Sopp. Kjemi.
Faglig foredrag
- (2014). Havet - vårt nye medisinskap?
Populærvitenskapelig foredrag
- (2016). Peptider, peptidomimetika og legemiddelutvikling.
- (2013). Hvordan lager man legemiddelmolekyler?
- (2012). The Nobel Prize in Chemistry 2012.
- (2012). Peptider og legemiddelutvikling.
- (2012). Hvordan lager man et legemiddel?
- (2007). Antimikrobielle peptider - En kilde til utvikling av fremtidenslegemidler mot mikrober og kreft?
Vitenskapelig foredrag
- (2023). Phospholipid membrane interactions of model peptides and depth of insertion investigated via solid-state NMR.
- (2023). A fragment to bind them all: Characterising phorbazole fragments as pan-kinase inhibitor.
- (2022). TARGETING A PSEUDOMONAS AERUGINOSA β-KETOACYL-(ACYL-CARRIER-PROTEIN) SYNTHASE WITH COVALENT INHIBITORS INSPIRED BY CERULENIN.
- (2022). Innovative molecular imaging technique for Granzyme-B characterization as an emerging biomarker for radio-immunotherapy combinations.
- (2022). Biogas Residues as Feedstock for Hydrothermal Conversion: Bio-Oil Yield Optimisation and Fate of Drugs.
- (2021). Targeting Bacterial Fatty Acid Synthesis using Fragment-Based Drug Design.
- (2020). Synthesis and Biological Activity of the Breitfussins.
- (2016). Discovery of LTX-315 - A potential first-in-class oncolytic peptide.
- (2016). BIOSNet - From marine natural products to commercial leads.
- (2015). Total synthesis of breitfussin A and B.
- (2014). Design and synthesis of substrates and inhibitors for Proteinase 3.
- (2014). Design and synthesis of ketomethylene-based inhibitors of human neutrophil Proteinase 3.
- (2012). Synthesis of piperidine derivatives.
- (2012). Novel Renin Inhibitors.
- (2012). Hvordan lager man et legemiddel?
- (2010). [3+2] Cycloaddition of benzyl azide to two highly functionalized alkynes.
- (2009). Synthesis of biologically active peptides and peptidomimetics.
- (2006). Synthesis of a Gln-Phe hydroxyethylene dipeptide isostere.
- (2001). Antibacterial Activity of 15-Residues Bovine Lactoferricin Derivatives Employing non-coded Aromatic Amino Acids, Peptides 2000.
- (2000). Increased Antibacterial activity of 15-residues Bovine Lactoferricin Derivatives employing non-coded Aromatic Amino Acids,.
Annet produkt
- (2001). Antimicrobial compounds and formulations.
Kompendium
- (2010). IUPAC ICOS-18 Proceedings.
Populærvitenskapelig artikkel
- (2001). FARGESTOFFER I SOPP. Blekksoppen. 16-19.
Doktorgradsavhandling
- (2016). Synthesis of Bicyclic CXCR4 Antagonists .
- (2014). Synthesis of serine protease inhibitors.
- (2012). Synthesis of novel renin inhibitors.
- (2012). Synthesis of Some Nitrogen Heterocycles of Medicinal Relevance.
Sammendrag/abstract
- (2012). Synthesis and docking of 4-triazolyl substituted piperidine derivatives as novel renin inhibitors. Journal of Peptide Science. S125-S125.
- (2011). SAR and Binding Mode for CXCR4 Antagonists Based on an Arg-Arg-Nal Tripeptide Motif. Biopolymers. 492-492.
Poster
- (2022). Structure-based hit discovery for riboswitch ligands.
- (2022). A P. AERUGINOSA FATTY ACID SYNTHESIS PROTEIN CRYSTALLOGRAPHIC FRAGMENT SCREEN AND ATTEMPTED OPTIMIZATION OF A HIT.
- (2020). Inhibition of the Actin N-terminal acetyltransferase NAA80.
- (2018). naa10 knockdown and NatA inhibition point to role for the NatA complex in zebrafish dorsoventral axis formation .
- (2018). Inhibition of the Actin N-terminal acetyltransferase NAA80.
- (2017). Synthesis of the natural product (3Z,6Z)-3-((1H-imidazol-5-yl)methylene)-6-(2-methylpropylidene)-piperazine-2,5-dione.
- (2017). Halogenation of electron rich heterocycles: Where does it go?
- (2016). Total Synthesis of Breitfussin A and B.
- (2016). Synthesis of a Challenging Amide.
- (2016). Synthesis of Analogues of the Bioactive Compound Barettin.
- (2016). Scaffold-based tripeptidomimetic CXCR4 antagonists.
- (2015). Synthetic studies towards peptidomimetic CXCR4 antagonists.
- (2015). Synthetic studies towards nitroreductase-activated fluorescent probes.
- (2015). Synthetic studies towards CXCR4 antagonists.
- (2014). Synthetic studies towards CXCR4 antagonists.
- (2014). Synthetic studies towards CXCR4 antagonists.
- (2014). Synthesis and biological evaluation of pseudopeptide inhibitors of Proteinase 3.
- (2012). Synthesis of a Ketomethylene Dipeptide Isostere.
- (2012). Synthesis and docking of 4-triazolyl substituted piperidine derivatives as novel renin inhibitors.
- (2012). Local Anesthetic Articaine Enantiomers interaction with Brain Lipids.
- (2011). Synthesis of 3,4-disubstituted piperidines.
- (2011). Synthesis of 3,4-disubstituted piperidines.
- (2009). Cycloaddition with highly functionalized terminal alkynes.
- (2006). Novel Antibacterial Tripeptides.
- (2001). Preparation of (2S)-3-amino-(2,2,5,7,8-pentamethyl-chroman-6-sulfonyl)-1H-indol-3-yl)-propionic acid and its incorporation into antibacterial lactoferricin peptides.
Vitenskapelig oversiktsartikkel/review
- (2015). Progress toward rationally designed small-molecule peptide and peptidomimetic CXCR4 antagonists. Future Medicinal Chemistry. 1261-1283.
- (2007). The medicinal chemistry of short lactoferricin-based antibacterial peptides. Current Medicinal Chemistry. 1-18.
Informasjon om pågående forskningsprosjekter i gruppen finnes på våre gruppesider.
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