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Heberle, A.

Publications and source records attributed to Heberle, A..

2 recordsLinked to original sources

Collective parameter estimation of related models with an initial stability constraint

Parameterisation of dynamic biochemical network models is a challenging aspect of systems biology. Especially when the parameter space is large and data is semi quantitive but comparable across different experimental conditions. Here, we present a set of command line tools utilising Pycotools (COPASI) that leverages the power of high-performance computing to facilitate parameter estimation of large models with many unknown parameters. In particular, we expand upon the abilities of Pycotools to address two particular issues. Firstly, the difficulty of constraining a models parameterisation to assume the system begins in a steady state (prior to a perturbative stimulation). And secondly, parameterising against relative quantitative time series data that have no absolute scale. Our software operates on the SLURM workload manager system and can be applied to any parameter estimation against time series data produced by applying a single perturbation at time zero to an equilibrated system. We validate that our technique can produce a parameterised model of the MTOR (mechanistic target of rapamycin) network based on semi-quantitative time-series data from 2 breast cancer cell lines, stimulated with insulin and amino acids. We also show our model can make reasonable predictions on distinct signaling dynamics in one breast cancer cell line based on the other by adjusting the initial protein quantities only. In conclusion, models should fit both the initial steady state and the dynamics following stimulation, given that stabilising systems prior to stimulation is a common experimental protocol in signaling research. By expanding standard tools, commonly used in the field, we have developed a widely applicable method, which can easily be evaluated and is amenable to wide general use.

systems biology↗

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

Nirmatrelvir was the first protease inhibitor (PI) specifically developed against the SARS-CoV-2 main protease (3CLpro/Mpro) and licensed for clinical use. As SARS-CoV-2 continues to spread, variants resistant to nirmatrelvir and other currently available treatments are likely to arise. This study aimed to identify and characterize mutations that confer resistance to nirmatrelvir. To safely generate Mpro resistance mutations, we passaged a previously developed, chimeric vesicular stomatitis virus (VSV-Mpro) with increasing, yet suboptimal concentrations of nirmatrelvir. Using Wuhan-1 and Omicron Mpro variants, we selected a large set of mutants. Some mutations are frequently present in GISAID, suggesting their relevance in SARS-CoV-2. The resistance phenotype of a subset of mutations was characterized against clinically available PIs (nirmatrelvir and ensitrelvir) with cell-based and biochemical assays. Moreover, we showed the putative molecular mechanism of resistance based on in silico molecular modelling. These findings have implications on the development of future generation Mpro inhibitors, will help to understand SARS-CoV-2 protease-inhibitor-resistance mechanisms and show the relevance of specific mutations in the clinic, thereby informing treatment decisions. TeaserUnderstanding how SARS-CoV-2 could counter the antiviral drug nirmatrelvir and what it means for the future of COVID-19 treatment.

microbiology↗