[PDF][PDF] BI 2536, a potent and selective inhibitor of polo-like kinase 1, inhibits tumor growth in vivo

…, M Krššák, U Gürtler, P Garin-Chesa, S Lieb… - Current biology, 2007 - cell.com
Fine-mapping of the cell-division cycle, notably the identification of mitotic kinase signaling
pathways, provides novel opportunities for cancer-drug discovery. As a key regulator of …

BI-3406, a potent and selective SOS1–KRAS interaction inhibitor, is effective in KRAS-driven cancers through combined MEK inhibition

…, N Pototschnig, F Schachinger, K Schipany, S Lieb… - Cancer Discovery, 2021 - AACR
To date, there are no effective targeted pan-KRAS therapies. In-depth characterization of BI-3406
activity and identification of MEK inhibitors as effective combination partners provide …

Triple angiokinase inhibitor nintedanib directly inhibits tumor cell growth and induces tumor shrinkage via blocking oncogenic receptor tyrosine kinases

…, A Baum, AT Le, RC Doebele, S Lieb… - … of Pharmacology and …, 2018 - ASPET
The triple-angiokinase inhibitor nintedanib is an orally available, potent, and selective inhibitor
of tumor angiogenesis by blocking the tyrosine kinase activities of vascular endothelial …

Synthetic lethality between the cohesin subunits STAG1 and STAG2 in diverse cancer contexts

P van der Lelij, S Lieb, J Jude, G Wutz, CP Santos… - Elife, 2017 - elifesciences.org
10.7554/eLife.26980.001 Recent genome analyses have identified recurrent mutations in
the cohesin complex in a wide range of human cancers. Here we demonstrate that the most …

Werner syndrome helicase is a selective vulnerability of microsatellite instability-high tumor cells

S Lieb, S Blaha-Ostermann, E Kamper, J Rippka… - Elife, 2019 - elifesciences.org
10.7554/eLife.43333.001 Targeted cancer therapy is based on exploiting selective dependencies
of tumor cells. By leveraging recent functional screening data of cancer cell lines we …

Discovery of potent and selective HER2 inhibitors with efficacy against HER2 exon 20 insertion-driven tumors, which preserve wild-type EGFR signaling

…, P Knesl, A Hörmann, A Köferle, M Corcokovic, S Lieb… - Nature Cancer, 2022 - nature.com
Oncogenic alterations in human epidermal growth factor receptor 2 (HER2) occur in
approximately 2% of patients with non-small cell lung cancer and predominantly affect the tyrosine …

[HTML][HTML] Combined KRASG12C and SOS1 inhibition enhances and extends the anti-tumor response in KRASG12C-driven cancers by addressing intrinsic and …

…, K Bosch, N Feng, S Gao, D Gerlach, M Gmachl, S Lieb… - bioRxiv, 2023 - ncbi.nlm.nih.gov
Efforts to improve the anti-tumor response to KRAS G12C targeted therapy have benefited
from leveraging combination approaches. Here, we compare the anti-tumor response induced …

STAG1 vulnerabilities for exploiting cohesin synthetic lethality in STAG2-deficient cancers

P van der Lelij, JA Newman, S Lieb… - Life Science …, 2020 - life-science-alliance.org
The cohesin subunit STAG2 has emerged as a recurrently inactivated tumor suppressor in
human cancers. Using candidate approaches, recent studies have revealed a synthetic lethal …

Structure of the helicase core of Werner helicase, a key target in microsatellite instability cancers

JA Newman, AE Gavard, S Lieb… - Life Science …, 2021 - life-science-alliance.org
Loss of WRN, a DNA repair helicase, was identified as a strong vulnerability of microsatellite
instable (MSI) cancers, making WRN a promising drug target. We show that ATP binding …

[PDF][PDF] Probing and overcoming KRASG12C inhibitor resistance by combination with a pan-KRAS SOS1 inhibitor

…, M Gmachl, D Alpar, S Lieb… - Cancer …, 2022 - medinfo.boehringer-ingelheim.com
• The recent accelerated approval of the KRASG12C mutantselective inhibitor Sotorasib (AMG
510) for the treatment of 2nd line KRASG12C mutation-positive NSCLC patients marks …