W. Haap

发表

A Real-World Perspective on Molecular Design.

W. Guba, J. Hert, B. Kuhn, 2016, Journal of medicinal chemistry.

Cation-pi interactions at the active site of factor Xa: dramatic enhancement upon stepwise N-alkylation of ammonium ions.

F. Diederich, D. Banner, W. Haap, 2009, Angewandte Chemie.

Molecular recognition at the active site of factor Xa: cation-π interactions, stacking on planar peptide surfaces, and replacement of structural water.

F. Diederich, D. Banner, W. Haap, 2012, Chemistry.

Fluorine Scan of Inhibitors of the Cysteine Protease Human Cathepsin L: Dipolar and Quadrupolar Effects in the π‐Stacking of Fluorinated Phenyl Rings on Peptide Amide Bonds

F. Diederich, B. Kuhn, W. Haap, 2016, ChemMedChem.

Discovery of Fluoromethylketone-Based Peptidomimetics as Covalent ATG4B (Autophagin-1) Inhibitors.

B. Kuhn, W. Haap, M. Stahl, 2016, ACS medicinal chemistry letters.

Inhibition of the Cysteine Protease Human Cathepsin L by Triazine Nitriles: Amide⋅⋅⋅Heteroarene π‐Stacking Interactions and Chalcogen Bonding in the S3 Pocket

F. Diederich, B. Kuhn, W. Haap, 2017, ChemMedChem.

Halogen Bonding at the Active Sites of Human Cathepsin L and MEK1 Kinase: Efficient Interactions in Different Environments

Nobuo Shimma, François Diederich, Jörg Benz, 2011, ChemMedChem.

Systematic investigation of halogen bonding in protein-ligand interactions.

François Diederich, Jörg Benz, Bernd Kuhn, 2011, Angewandte Chemie.

What We Learned in 25 Years of Interactive Molecular Design Sessions

B. Kuhn, W. Haap, M. Stahl, 2021, ChemMedChem.

Cathepsin S inhibition suppresses autoimmune‐triggered inflammatory responses in macrophages

Michel Theron, W. Haap, B. Reis, 2017, Biochemical pharmacology.

Selective cathepsin S inhibition attenuates atherosclerosis in apolipoprotein E-deficient mice with chronic renal disease.

P. Libby, W. Haap, Jose-Luiz Figueiredo, 2015, The American journal of pathology.

Cathepsin S inhibition combines control of systemic and peripheral pathomechanisms of autoimmune tissue injury

W. Haap, A. Rufer, H. Anders, 2017, Scientific Reports.

Solid phase synthesis of diverse isoxazolidines via 1,3-dipolar cycloaddition

W. Haap, T. Walk, G. Jung, 1998 .

Cathepsin S Cleavage of Protease-Activated Receptor-2 on Endothelial Cells Promotes Microvascular Diabetes Complications.

Emma J. Reid, W. Haap, C. Cohen, 2016, Journal of the American Society of Nephrology : JASN.

Identification of potent and selective cathepsin S inhibitors containing different central cyclic scaffolds.

D. Banner, W. Haap, A. Kuglstatter, 2013, Journal of medicinal chemistry.

Cathepsin S inhibition suppresses systemic lupus erythematosus and lupus nephritis because cathepsin S is essential for MHC class II-mediated CD4 T cell and B cell priming

W. Haap, H. Anders, O. Kulkarni, 2013, Annals of the rheumatic diseases.

Discovery of a factor Xa inhibitor (3R,4R)-1-(2,2-difluoro-ethyl)-pyrrolidine-3,4-dicarboxylic acid 3-[(5-chloro-pyridin-2-yl)-amide] 4-[[2-fluoro-4-(2-oxo-2H-pyridin-1-yl)-phenyl]-amide] as a clinical candidate.

Martin Stahl, Walter Huber, Jörg Benz, 2010, Bioorganic & medicinal chemistry letters.

Sulfonylureido thiazoles as fructose-1,6-bisphosphatase inhibitors for the treatment of type-2 diabetes.

B. Kuhn, W. Haap, J. Benz, 2010, Bioorganic & medicinal chemistry letters.

Discovery of a Factor Xa Inhibitor (3R,4R)‐1‐(2,2‐difluoro‐ethyl)‐pyrrolidine‐3,4‐dicarboxylic Acid 3‐[(5‐Chloro‐pyridin‐2‐yl)‐amide] 4‐{[2‐Fluoro‐4‐(2‐oxo‐2H‐pyridin‐1‐yl)‐phenyl]‐amide} as a Clinical Candidate.

W. Haap, 2011 .

Increased Cathepsin S in Prdm1−/− dendritic cells alters TFH repertoire and contributes to lupus

P. Gregersen, W. Haap, B. Diamond, 2017, Nature Immunology.

Repurposing a Library of Human Cathepsin L Ligands: Identification of Macrocyclic Lactams as Potent Rhodesain and Trypanosoma brucei Inhibitors.

F. Diederich, B. Kuhn, D. Banner, 2018, Journal of medicinal chemistry.

2 H-1,2,3-Triazole-Based Dipeptidyl Nitriles: Potent, Selective, and Trypanocidal Rhodesain Inhibitors by Structure-Based Design.

Rainer E. Martin, F. Diederich, B. Kuhn, 2018, Journal of medicinal chemistry.

Optimization of Triazine Nitriles as Rhodesain Inhibitors: Structure–Activity Relationships, Bioisosteric Imidazopyridine Nitriles, and X‐ray Crystal Structure Analysis with Human Cathepsin L

F. Diederich, D. Banner, W. Haap, 2013, ChemMedChem.

FT-IR Mapping-A New Tool for Spatially Resolved Characterization of Polymer-Bound Combinatorial Compound Libraries with IR Microscopy.

Günther Jung, W. Haap, T. Walk, 1998, Angewandte Chemie.

Determination of protein-ligand binding constants of a cooperatively regulated tetrameric enzyme using electrospray mass spectrometry.

W. Haap, K. Barylyuk, R. Zenobi, 2014, ACS chemical biology.

Small-Molecule Lead-Finding Trends across the Roche and Genentech Research Organizations.

Melinda M. Mulvihill, W. Haap, A. Stepan, 2022, Journal of medicinal chemistry.

FT‐Infrared Spectroscopy and IR‐Microscopy On‐Bead Analysis of Solid‐Phase Synthesis

W. Haap, G. Jung, H. Bandel, 1999 .

Composition and Purity of Combinatorial Aryl Ether Collections Analyzed by Electrospray Mass Spectrometry

W. Haap, G. Jung, C. Kempter, 2004, Molecular Diversity.

Design of novel aminopyrrolidine factor Xa inhibitors from a screening hit.

Martin Stahl, Jörg Benz, Daniel Schlatter, 2009, European journal of medicinal chemistry.

Effects of Cathepsin S Inhibition in the Age-Related Dry Eye Phenotype

W. Haap, C. Trujillo-Vargas, C. D. de Paiva, 2023, Investigative ophthalmology & visual science.

Cathepsin S inhibition combines control of systemic and peripheral pathomechanisms of autoimmune tissue injury

W. Haap, A. Rufer, S. R. Mulay, 2017, Scientific Reports.

Discovery of Fluoromethylketone-Based Peptidomimetics as Covalent ATG4B (Autophagin-1) Inhibitors.

B. Kuhn, W. Haap, M. Stahl, 2016, ACS medicinal chemistry letters.

Increased Cathepsin S in Prdm1−/− dendritic cells alters TFH repertoire and contributes to lupus

P. Gregersen, W. Haap, B. Diamond, 2017, Nature Immunology.

Inhibition of Cathepsin S in Autoimmune CD25KO Mouse Improves Sjögren Disease–Like Lacrimal Gland Pathology

W. Haap, C. D. de Paiva, J. Galletti, 2024, Investigative ophthalmology & visual science.