Publications by authors named "Rainer Machauer"

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Discovery of NP3-742: A Structurally Diverse NLRP3 Inhibitor Identified through an Unusual Phenol Replacement.
Juraj Velcicky, Jean-Baptiste Langlois, Michael Wright, Philipp Janser, Daniela Angst, Rainer Machauer

J Med Chem· November 2025

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Discovery and Optimization of Selective Inhibitors of Large Tumor Suppressor Kinases LATS1 and 2 for In Vivo Investigation of the Hippo-YAP Pathway in Tissue Regeneration.
Kenji Namoto, Eric Vangrevelinghe, Rainer Machauer, Dirk Behnke, Nicole Buschmann

J Med Chem· July 2025

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NIBR-LTSi is a selective LATS kinase inhibitor activating YAP signaling and expanding tissue stem cells in vitro and in vivo.
Kenji Namoto, Clara Baader, Vanessa Orsini, Alexandro Landshammer, Eva Breuer, Rainer Machauer

Cell Stem Cell· April 2024

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JDQ443, a Structurally Novel, Pyrazole-Based, Covalent Inhibitor of KRAS for the Treatment of Solid Tumors.
Edwige Lorthiois, Marc Gerspacher, Kim S Beyer, Andrea Vaupel, Catherine Leblanc, Rainer Machauer

J Med Chem· December 2022

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Discovery of Umibecestat (CNP520): A Potent, Selective, and Efficacious β-Secretase (BACE1) Inhibitor for the Prevention of Alzheimer's Disease.
Rainer Machauer, Rainer Lueoend, Konstanze Hurth, Siem J Veenstra, Heinrich Rueeger

J Med Chem· October 2021

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Synthesis of the Potent, Selective, and Efficacious β-Secretase (BACE1) Inhibitor NB-360.
Heinrich Rueeger, Rainer Lueoend, Rainer Machauer, Siem J Veenstra, Philipp Holzer

J Med Chem· April 2021

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The β-secretase (BACE) inhibitor NB-360 in preclinical models: From amyloid-β reduction to downstream disease-relevant effects.
Ulf Neumann, Rainer Machauer, Derya R Shimshek

Br J Pharmacol· September 2019

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Discovery and Structural Characterization of ATP-Site Ligands for the Wild-Type and V617F Mutant JAK2 Pseudokinase Domain.
Randall McNally, Qing Li, Kunhua Li, Carien Dekker, Eric Vangrevelinghe, Rainer Machauer

ACS Chem Biol· April 2019

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The BACE-1 inhibitor CNP520 for prevention trials in Alzheimer's disease.
Ulf Neumann, Mike Ufer, Laura H Jacobson, Marie-Laure Rouzade-Dominguez, Gunilla Huledal, Rainer Machauer

EMBO Mol Med· November 2018

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Discovery of amino-1,4-oxazines as potent BACE-1 inhibitors.
Siem Jakob Veenstra, Heinrich Rueeger, Markus Voegtle, Rainer Lueoend, Philipp Holzer, Rainer Machauer

Bioorg Med Chem Lett· July 2018

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Discovery of Potent, Selective, and Structurally Novel Dot1L Inhibitors by a Fragment Linking Approach.
Henrik Möbitz, Rainer Machauer, Philipp Holzer, Andrea Vaupel, Frédéric Stauffer

ACS Med Chem Lett· March 2017

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Discovery of Novel Dot1L Inhibitors through a Structure-Based Fragmentation Approach.
Chao Chen, Hugh Zhu, Frédéric Stauffer, Giorgio Caravatti, Susanne Vollmer, Rainer Machauer

ACS Med Chem Lett· August 2016

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Pharmacological BACE1 and BACE2 inhibition induces hair depigmentation by inhibiting PMEL17 processing in mice.
Derya R Shimshek, Laura H Jacobson, Carine Kolly, Natasa Zamurovic, Kamal Kumar Balavenkatraman, Rainer Machauer

Sci Rep· February 2016

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A novel BACE inhibitor NB-360 shows a superior pharmacological profile and robust reduction of amyloid-β and neuroinflammation in APP transgenic mice.
Ulf Neumann, Heinrich Rueeger, Rainer Machauer, Siem Jacob Veenstra, Rainer M Lueoend

Mol Neurodegener· September 2015

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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.
Heinrich Rueeger, Rainer Lueoend, Rainer Machauer, Siem Jacob Veenstra, Laura Helen Jacobson

Bioorg Med Chem Lett· October 2013

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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.
Heinrich Rueeger, Rainer Lueoend, Olivier Rogel, Jean-Michel Rondeau, Henrik Möbitz, Rainer Machauer

J Med Chem· April 2012

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Macrocyclic BACE-1 inhibitors acutely reduce Abeta in brain after po application.
Andreas Lerchner, Rainer Machauer, Claudia Betschart, Siem Veenstra, Heinrich Rueeger

Bioorg Med Chem Lett· January 2010

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Structure-based design and synthesis of macrocyclic peptidomimetic beta-secretase (BACE-1) inhibitors.
Rainer Machauer, Siem Veenstra, Jean-Michel Rondeau, Marina Tintelnot-Blomley, Claudia Betschart

Bioorg Med Chem Lett· March 2009

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Macrocyclic peptidomimetic beta-secretase (BACE-1) inhibitors with activity in vivo.
Rainer Machauer, Kurt Laumen, Siem Veenstra, Jean-Michel Rondeau, Marina Tintelnot-Blomley

Bioorg Med Chem Lett· March 2009

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