[HTML][HTML] The novel dihydroorotate dehydrogenase (DHODH) inhibitor BAY 2402234 triggers differentiation and is effective in the treatment of myeloid malignancies

…, S Ferrara, H Meyer, R Lesche, D Stoeckigt, M Bauser… - Leukemia, 2019 - nature.com
Acute myeloid leukemia (AML) is a devastating disease, with the majority of patients dying
within a year of diagnosis. For patients with relapsed/refractory AML, the prognosis is …

Identification and optimization of the first highly selective GLUT1 inhibitor BAY‐876

…, R Neuhaus, I Heisler, T Müller, M Bauser… - …, 2016 - Wiley Online Library
Despite the long‐known fact that the facilitative glucose transporter GLUT1 is one of the key
players safeguarding the increase in glucose consumption of many tumor entities even …

Pan-mutant-IDH1 inhibitor BAY1436032 is highly effective against human IDH1 mutant acute myeloid leukemia in vivo

…, H Rehwinkel, H Hess-Stumpp, M Bauser… - Leukemia, 2017 - nature.com
Neomorphic mutations in isocitrate dehydrogenase 1 (IDH1) are frequently found in several
human cancer types including acute myeloid leukemia (AML) and lead to the production of …

Preclinical efficacy of the novel monocarboxylate transporter 1 inhibitor BAY-8002 and associated markers of resistance

…, A Kamburov, H Siebeneicher, M Bauser… - Molecular cancer …, 2018 - AACR
The lactate transporter SLC16A1/monocarboxylate transporter 1 (MCT1) plays a central role
in tumor cell energy homeostasis. In a cell-based screen, we identified a novel class of …

Sequential nitration/hydrogenation protocol for the synthesis of triaminophloroglucinol: safe generation and use of an explosive intermediate under continuous-flow …

…, M Damm, D Dallinger, M Bauser… - … Process Research & …, 2014 - ACS Publications
A continuous-flow process for the synthesis of triaminophloroglucinol has been developed.
The synthetic procedure is based on a sequential nitration/reduction protocol which uses …

New class of bacterial phenylalanyl-tRNA synthetase inhibitors with high potency and broad-spectrum activity

…, G Schiffer, S Siegel, M Bauser… - Antimicrobial agents …, 2004 - Am Soc Microbiol
Phenylalanyl (Phe)-tRNA synthetase (Phe-RS) is an essential enzyme which catalyzes the
transfer of phenylalanine to the Phe-specific transfer RNA (tRNA Phe ), a key step in protein …

Donated chemical probes for open science

S Müller, S Ackloo, CH Arrowsmith, M Bauser… - Elife, 2018 - elifesciences.org
Potent, selective and broadly characterized small molecule modulators of protein function (chemical
probes) are powerful research reagents. The pharmaceutical industry has …

[HTML][HTML] Preclinical profile of gadoquatrane: a novel tetrameric, macrocyclic high relaxivity gadolinium-based contrast agent

…, CS Hilger, G Jost, O Panknin, M Bauser… - Investigative …, 2022 - journals.lww.com
Objectives The aim of this report was to characterize the key physicochemical, pharmacokinetic
(PK), and magnetic resonance imaging (MRI) properties of gadoquatrane (BAY 1747846)…

Discovery of an Oral, Beyond-Rule-of-Five Mcl-1 Protein–Protein Interaction Modulator with the Potential of Treating Hematological Malignancies

…, S Joo Koo, W Lento, M Bauser… - Journal of Medicinal …, 2023 - ACS Publications
Avoidance of apoptosis is critical for the development and sustained growth of tumors. The
pro-survival protein myeloid cell leukemia 1 (Mcl-1) is an anti-apoptotic member of the Bcl-2 …

Novel class of potent and cellularly active inhibitors devalidates MTH1 as broad-spectrum cancer target

…, H Irlbacher, H Meyer, N Queisser, M Bauser… - ACS chemical …, 2017 - ACS Publications
MTH1 is a hydrolase responsible for sanitization of oxidized purine nucleoside triphosphates
to prevent their incorporation into replicating DNA. Early tool compounds published in the …