[HTML][HTML] Analysis of RAS and drug induced homo-and heterodimerization of RAF and KSR1 proteins in living cells using split Nanoluc luciferase

L Rohrer, C Spohr, C Beha, R Griffin, S Braun… - Cell Communication and …, 2023 - Springer
The dimerization of RAF kinases represents a key event in their activation cycle and in
RAS/ERK pathway activation. Genetic, biochemical and structural approaches provided key …

[HTML][HTML] Physiological cell culture media tune mitochondrial bioenergetics and drug sensitivity in cancer cell models

O Torres-Quesada, C Doerrier, S Strich, E Gnaiger… - Cancers, 2022 - mdpi.com
Simple Summary Cell biologists trust in standard media for analyzing cellular functions and
for the specification of target-oriented drug efficacies in cell culture settings. Here, we …

[HTML][HTML] Resistor: an algorithm for predicting resistance mutations via Pareto optimization over multistate protein design and mutational signatures

N Guerin, A Feichtner, E Stefan, T Kaserer, BR Donald - Cell systems, 2022 - cell.com
Resistance to pharmacological treatments is a major public health challenge. Here, we
introduce Resistor—a structure-and sequence-based algorithm that prospectively predicts …

[HTML][HTML] A comprehensive study of SARS-CoV-2 main protease (Mpro) inhibitor-resistant mutants selected in a VSV-based system

F Costacurta, A Dodaro, D Bante, H Schöppe… - bioRxiv, 2023 - ncbi.nlm.nih.gov
Nirmatrelvir was the first protease inhibitor (PI) specifically developed against the SARS-
CoV-2 main protease (3CL pro/M pro) and licensed for clinical use. As SARS-CoV-2 …

[HTML][HTML] Kinase perturbations redirect mitochondrial function in cancer

O Torres-Quesada, S Strich, E Stefan - Bioenergetics …, 2022 - ncbi.nlm.nih.gov
Protein kinases take the center stage in numerous signaling pathways by phosphorylating
compartmentalized protein substrates for controlling cell proliferation, cell cycle and …

[HTML][HTML] Tracking mutation and drug-driven alterations of oncokinase conformations

A Feichtner, V Kugler, S Schwaighofer… - memo-Magazine of …, 2022 - Springer
Numerous kinases act as central nodes of cellular signaling networks. As such, many of
these enzymes function as molecular switches for coordinating spatiotemporal signal …

Tracking and blocking interdependencies of cellular BRAF-MEK oncokinase activities

J Fleischmann, S Schwaighofer, L De Falco… - PNAS …, 2023 - academic.oup.com
The selective targeting of mutated kinases in cancer therapies has the potential to improve
therapeutic success and thereby the survival of patients. In the case of melanoma, the …

[HTML][HTML] Allosteric kinase inhibitors reshape MEK1 kinase activity conformations in cells and in silico

J Fleischmann, A Feichtner, L DeFalco, V Kugler… - Biomolecules, 2021 - mdpi.com
Mutations at different stages of the mitogen-activated protein kinase (MAPK) signaling
pathway lead to aberrant activation of the involved protein kinase entities. These oncogenic …

Kinases in motion: impact of protein and small molecule interactions on kinase conformations

V Kugler, S Schwaighofer, A Feichtner, F Enzler… - bioRxiv, 2024 - biorxiv.org
Protein kinases act as central molecular switches in the control of cellular functions.
Alterations in the regulation and function of protein kinases may provoke diseases including …

Resistor: an algorithm for predicting resistance mutations using Pareto optimization over multistate protein design and mutational signatures

N Guerin, T Kaserer, BR Donald - International Conference on Research …, 2022 - Springer
Resistance to pharmacological treatments, such as to antibiotics or cancer therapeutics,
ablates the efficacy of drugs and is a major public health challenge [,]. Accurate, prospective …