Florian Colbatzky

Knock‐out of dipeptidase CN2 in human proximal tubular cells disrupts dipeptide and amino acid homeostasis and para‐ and transcellular solute transport

Tilman Pfeffer, Susanne M. Krug, Tamara Kracke, Robin Schürfeld et autres

AIM: Although of potential biomedical relevance, dipeptide metabolism has hardly been studied. We found the dipeptidase carnosinase-2 (CN2) to be abundant in human proximal tubules, which regulate water and solute homeostasis. We therefore hypothesized, that CN2 has a key metabolic role, impacting …

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Molecular basis of GDF15 induction and suppression by drugs in cardiomyocytes and cancer cells toward precision medicine

Lisa-Maria Winter, Diana Reinhardt, Ariane Schatter, Vivien Tissen et autres

GDF15 has recently emerged as a key driver of the development of various disease conditions including cancer cachexia. Not only the tumor itself but also adverse effects of chemotherapy have been reported to contribute to increased GDF15. Although regulation of GDF15 transcription …

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Supplementary Data Content from A Novel RAF Kinase Inhibitor with DFG-Out–Binding Mode: High Efficacy in BRAF-Mutant Tumor Xenograft Models in the Absence of Normal Tissue Hyperproliferation

Irene C. Waizenegger, Anke Baum, Steffen Steurer, Heinz Stadtmüller et autres

Overview about Supplementary Information including brief captions

Supplementary Table S3 from A Novel RAF Kinase Inhibitor with DFG-Out–Binding Mode: High Efficacy in BRAF-Mutant Tumor Xenograft Models in the Absence of Normal Tissue Hyperproliferation

Irene C. Waizenegger, Anke Baum, Steffen Steurer, Heinz Stadtmüller et autres

Overview of in vivo efficacy of BI 882370 and comparator compounds tested as single agents or in combination using melanoma and colorectal cancer xenograft mouse models.

Supplementary Figure Legends from A Novel RAF Kinase Inhibitor with DFG-Out–Binding Mode: High Efficacy in BRAF-Mutant Tumor Xenograft Models in the Absence of Normal Tissue Hyperproliferation

Irene C. Waizenegger, Anke Baum, Steffen Steurer, Heinz Stadtmüller et autres

Legends for Supplementary Figures S1 - S6

Supplementary Materials and Methods from A Novel RAF Kinase Inhibitor with DFG-Out–Binding Mode: High Efficacy in BRAF-Mutant Tumor Xenograft Models in the Absence of Normal Tissue Hyperproliferation

Irene C. Waizenegger, Anke Baum, Steffen Steurer, Heinz Stadtmüller et autres

Protocols for data shown in the Supplement

Supplementary Figures S1 - S6 from A Novel RAF Kinase Inhibitor with DFG-Out–Binding Mode: High Efficacy in BRAF-Mutant Tumor Xenograft Models in the Absence of Normal Tissue Hyperproliferation

Irene C. Waizenegger, Anke Baum, Steffen Steurer, Heinz Stadtmüller et autres

Supplementary Figure S1 - Structure of the BRAF kinase domain with BI 882370 and a bound glucose molecule Supplementary Figure S2 - Drug wash-out experiment prolonged phospho-ERK reduction in A375 melanoma cells treated with BI 882370 vs comparator compound. Supplementary Figure S3 …

Supplementary Table S4 from A Novel RAF Kinase Inhibitor with DFG-Out–Binding Mode: High Efficacy in BRAF-Mutant Tumor Xenograft Models in the Absence of Normal Tissue Hyperproliferation

Irene C. Waizenegger, Anke Baum, Steffen Steurer, Heinz Stadtmüller et autres

Differentially expressed genes in vemurafenib-resistant vs. control A375 tumors, obtained from the in vivo study shown in Fig. 4.

Supplementary Tables S1 and S2 from A Novel RAF Kinase Inhibitor with DFG-Out–Binding Mode: High Efficacy in BRAF-Mutant Tumor Xenograft Models in the Absence of Normal Tissue Hyperproliferation

Irene C. Waizenegger, Anke Baum, Steffen Steurer, Heinz Stadtmüller et autres

Data and statistics from x-ray co-crystallization experiments with BI 882370 or dabrafenib with the BRAF kinase domain.

Supplementary Tables S5 and S6 from A Novel RAF Kinase Inhibitor with DFG-Out–Binding Mode: High Efficacy in BRAF-Mutant Tumor Xenograft Models in the Absence of Normal Tissue Hyperproliferation

Irene C. Waizenegger, Anke Baum, Steffen Steurer, Heinz Stadtmüller et autres

Analysis of mouse tissues and exploratory toxicological assessment in rats revealed a favorable rodent safety profile for BI 882370.

Supplementary Data Content from A Novel RAF Kinase Inhibitor with DFG-Out–Binding Mode: High Efficacy in BRAF-Mutant Tumor Xenograft Models in the Absence of Normal Tissue Hyperproliferation

Irene C. Waizenegger, Anke Baum, Steffen Steurer, Heinz Stadtmüller et autres

Overview about Supplementary Information including brief captions

Supplementary Tables S1 and S2 from A Novel RAF Kinase Inhibitor with DFG-Out–Binding Mode: High Efficacy in BRAF-Mutant Tumor Xenograft Models in the Absence of Normal Tissue Hyperproliferation

Irene C. Waizenegger, Anke Baum, Steffen Steurer, Heinz Stadtmüller et autres

Data and statistics from x-ray co-crystallization experiments with BI 882370 or dabrafenib with the BRAF kinase domain.