Michal Vieth

Supplementary Tables S1-S4 and Supplementary Figures S1-S6 from Molecular Basis for Necitumumab Inhibition of EGFR Variants Associated with Acquired Cetuximab Resistance

Atrish Bagchi, Jaafar N. Sleiman Haidar, Scott W. Eastman, Michal Vieth et autres

Supplementary Table S1 - Therapeutic antibody induced EGFR ECR mutations; Supplementary Table S2 - Mean SPR KD values for binding of wild type (WT) and cetuximab resistance variants of sEGFR to immobilized Fab fragments from cetuximab (FabC225) and necitumumab (Fab11F8) and to …

Data from Molecular Basis for Necitumumab Inhibition of EGFR Variants Associated with Acquired Cetuximab Resistance

Atrish Bagchi, Jaafar N. Sleiman Haidar, Scott W. Eastman, Michal Vieth et autres

Abstract Acquired resistance to cetuximab, an antibody that targets the EGFR, impacts clinical benefit in head and neck, and colorectal cancers. One of the mechanisms of resistance to cetuximab is the acquisition of mutations that map to the cetuximab epitope on EGFR …

Data from Molecular Basis for Necitumumab Inhibition of EGFR Variants Associated with Acquired Cetuximab Resistance

Atrish Bagchi, Jaafar N. Sleiman Haidar, Scott W. Eastman, Michal Vieth et autres

Abstract Acquired resistance to cetuximab, an antibody that targets the EGFR, impacts clinical benefit in head and neck, and colorectal cancers. One of the mechanisms of resistance to cetuximab is the acquisition of mutations that map to the cetuximab epitope on EGFR …

Supplementary Tables S1-S4 and Supplementary Figures S1-S6 from Molecular Basis for Necitumumab Inhibition of EGFR Variants Associated with Acquired Cetuximab Resistance

Atrish Bagchi, Jaafar N. Sleiman Haidar, Scott W. Eastman, Michal Vieth et autres

Supplementary Table S1 - Therapeutic antibody induced EGFR ECR mutations; Supplementary Table S2 - Mean SPR KD values for binding of wild type (WT) and cetuximab resistance variants of sEGFR to immobilized Fab fragments from cetuximab (FabC225) and necitumumab (Fab11F8) and to …

Structural determinants of dual incretin receptor agonism by tirzepatide

Bingfa Sun, Francis S. Willard, Dan Feng, Jorge Alsina‐Fernandez et autres

SignificanceTirzepatide is a dual agonist of the glucose-dependent insulinotropic polypeptide receptor (GIPR) and the glucagon-like peptide-1 receptor (GLP-1R), which are incretin receptors that regulate carbohydrate metabolism. This investigational agent has proven superior to selective GLP-1R agonists in clinical trials in subjects with …

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Identification of β-Lactams Active against Mycobacterium tuberculosis by a Consortium of Pharmaceutical Companies and Academic Institutions

Ben S. Gold, Jun Zhang, Landys Lopez Quezada, Julia Roberts et autres

(Mtb). In the TB Drug Accelerator (TBDA), a consortium organized by the Bill & Melinda Gates Foundation, individual pharmaceutical companies collaborate with academic screening laboratories. We developed a higher order consortium within the TBDA in which four pharmaceutical companies (GlaxoSmithKline, Sanofi, MSD, …

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Identification of tyrosine kinase inhibitors that halt Plasmodium falciparum parasitemia

Kristina R. Kesely, Panae Noomuna, Michal Vieth, Philip A. Hipskind et autres

Although current malaria therapies inhibit pathways encoded in the parasite's genome, we have looked for anti-malaria drugs that can target an erythrocyte component because development of drug resistance might be suppressed if the parasite cannot mutate the drug's target. In search for …

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Structural insights into probe-dependent positive allosterism of the GLP-1 receptor

Ana Belen Bueno, Bingfa Sun, Francis S. Willard, Dan Feng et autres

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Crystal structure of human RIOK2 bound to a specific inhibitor

Jing Wang, Thibault Vincent Varin, Michal Vieth, Jonathan M. Elkins

The RIO kinases (RIOKs) are a universal family of atypical kinases that are essential for assembly of the pre-40S ribosome complex. Here, we present the crystal structure of human RIO kinase 2 (RIOK2) bound to a specific inhibitor. This first crystal structure …

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Supplementary material from "Crystal structure of human RIOK2 bound to a specific inhibitor"

Jing Wang, Thibault Vincent Varin, Michal Vieth, Jonathan M. Elkins

The RIO kinases (RIOKs) are a universal family of atypical kinases that are essential for assembly of the pre-40S ribosome complex. Here, we present the crystal structure of human RIO kinase 2 (RIOK2) bound to a specific inhibitor. This first crystal structure …

Supplementary Figures and methods for MD simulations from Crystal structure of human RIOK2 bound to a specific inhibitor

Jing Wang, Thibault Vincent Varin, Michal Vieth, Jonathan M. Elkins

Supplementary Figures and methods for MD simulations

Predicting the Conformational Variability of Abl Tyrosine Kinase using Molecular Dynamics Simulations and Markov State Models

Yilin Meng, Cen Gao, David K. Clawson, S. Atwell et autres

Understanding protein conformational variability remains a challenge in drug discovery. The issue arises in protein kinases, whose multiple conformational states can affect the binding of small-molecule inhibitors. To overcome this challenge, we propose a comprehensive computational framework based on Markov state models …

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