R. Machauer

发表

Discovery of cyclic sulfone hydroxyethylamines as potent and selective β-site APP-cleaving enzyme 1 (BACE1) inhibitors: structure-based design and in vivo reduction of amyloid β-peptides.

Jean-Michel Rondeau, Laura Jacobson, M. Staufenbiel, 2012, Journal of medicinal chemistry.

Enantioselective synthesis of (+)-anatoxin-a via enyne metathesis

S. Martin, R. Machauer, Brenneman Jehrod Burnett, 2004 .

Discovery of cyclic sulfoxide hydroxyethylamines as potent and selective β-site APP-cleaving enzyme 1 (BACE1) inhibitors: structure based design and in vivo reduction of amyloid β-peptides.

M. Staufenbiel, J. Rondeau, S. Desrayaud, 2013, Bioorganic & medicinal chemistry letters.

Synthesis of cis-2,5-disubstituted pyrrolidines via diastereoselective reduction of N-acyl iminium ions

S. Martin, R. Machauer, Alexander C. Rudolph, 2004 .

Macrocyclic peptidomimetic beta-secretase (BACE-1) inhibitors with activity in vivo.

Jean-Michel Rondeau, Marina Tintelnot-Blomley, M. Staufenbiel, 2009, Bioorganic & medicinal chemistry letters.

Pharmacological BACE1 and BACE2 inhibition induces hair depigmentation by inhibiting PMEL17 processing in mice

D. Theil, M. Jucker, R. Kreutzer, 2016, Scientific Reports.

The β‐secretase (BACE) inhibitor NB‐360 in preclinical models: From amyloid‐β reduction to downstream disease‐relevant effects

D. Shimshek, U. Neumann, R. Machauer, 2019, British journal of pharmacology.

The BACE‐1 inhibitor CNP520 for prevention trials in Alzheimer's disease

M. Staufenbiel, S. Vormfelde, N. Beckmann, 2018, EMBO molecular medicine.

A novel BACE inhibitor NB-360 shows a superior pharmacological profile and robust reduction of amyloid-β and neuroinflammation in APP transgenic mice

M. Staufenbiel, G. Laue, D. Shimshek, 2015, Molecular Neurodegeneration.

Structure-based design and synthesis of macrocyclic peptidomimetic beta-secretase (BACE-1) inhibitors.

Jean-Michel Rondeau, Marina Tintelnot-Blomley, P. Paganetti, 2009, Bioorganic & medicinal chemistry letters.

Discovery of Umibecestat (CNP520): A Potent, Selective, and Efficacious β-Secretase (BACE1) Inhibitor for the Prevention of Alzheimer's Disease.

G. Laue, J. Rondeau, L. Jacobson, 2021, Journal of medicinal chemistry.

Discovery and Structural Characterization of ATP-Site Ligands for the Wild-Type and V617F Mutant JAK2 Pseudokinase Domain.

C. Dekker, P. Chène, M. Eck, 2019, ACS Chemical Biology.

Corrigendum to “Structure-based design and synthesis of macrocyclic peptidomimetic β-secretase (BACE-1) inhibitors” [Bioorg. Med. Chem. Lett. 19 (2009) 1361–1365]

Siem J. Veenstra, Jean-Michel Rondeau, Marina Tintelnot-Blomley, 2009 .

A novel BACE inhibitor NB-360 shows a superior pharmacological profile and robust reduction of amyloid-β and neuroinflammation in APP transgenic mice

M. Staufenbiel, G. Laue, D. Shimshek, 2015, Molecular Neurodegeneration.

Macrocyclic BACE-1 inhibitors acutely reduce Abeta in brain after po application.

M. Staufenbiel, P. Paganetti, J. Rondeau, 2010, Bioorganic & medicinal chemistry letters.

Synthesis of the Potent, Selective, and Efficacious β-Secretase (BACE1) Inhibitor NB-360.

Mathias Frederiksen, Philipp Holzer, M. Staufenbiel, 2021, Journal of medicinal chemistry.

Discovery of Potent, Selective, and Structurally Novel Dot1L Inhibitors by a Fragment Linking Approach.

Philipp Holzer, R. Tiedt, G. Caravatti, 2017, ACS medicinal chemistry letters.

THE BACE INHIBITOR NB-360 HAS EXCELLENT BRAIN PENETRATION AND EFFICACY ON AMYLOID-B LOAD IN ANIMAL MODELS

M. Staufenbiel, G. Laue, D. Shimshek, 2014, Alzheimer's & Dementia.

Synthesis of lipidated eNOS peptides by combining enzymatic, noble metal- and acid-mediated protecting group techniques with solid phase peptide synthesis and fragment condensation in solution.

H. Waldmann, R. Machauer, 2001, Chemistry.

JDQ443, a Structurally Novel, Pyrazole-Based, Covalent Inhibitor of KRASG12C for the Treatment of Solid Tumors.

N. Ostermann, R. Wilcken, S. Brachmann, 2022, Journal of medicinal chemistry.

Discovery of amino-1,4-oxazines as potent BACE-1 inhibitors.

Mathias Frederiksen, Philipp Holzer, M. Staufenbiel, 2018, Bioorganic & medicinal chemistry letters.

Discovery of Novel Dot1L Inhibitors through a Structure-Based Fragmentation Approach.

Philipp Holzer, R. Tiedt, G. Caravatti, 2016, ACS medicinal chemistry letters.

NIBR-LTSi is a selective LATS kinase inhibitor activating YAP signaling and expanding tissue stem cells in vitro and in vivo.

H. Ruffner, T. Bouwmeester, P. Liberali, 2024, Cell stem cell.