Mechanisms of acquired BRAF inhibitor resistance in melanoma: a systematic review

I Proietti, N Skroza, N Bernardini, E Tolino, V Balduzzi… - Cancers, 2020 - mdpi.com
Simple Summary Patients with advanced melanoma are often treated with v-raf murine
sarcoma viral oncogene homolog B1 (BRAF) inhibitors. Although these agents prolong life …

Transposon insertion mutagenesis in mice for modeling human cancers: Critical insights gained and new opportunities

PJ Beckmann, DA Largaespada - International journal of molecular …, 2020 - mdpi.com
Transposon mutagenesis has been used to model many types of human cancer in mice,
leading to the discovery of novel cancer genes and insights into the mechanism of …

The AhR‐SRC axis as a therapeutic vulnerability in BRAFi‐resistant melanoma

A Paris, N Tardif, FM Baietti, C Berra… - EMBO Molecular …, 2022 - embopress.org
The nongenetic mechanisms required to control tumor phenotypic plasticity and shape drug‐
resistance remain unclear. We show here that the Aryl hydrocarbon Receptor (AhR) …

Identification of novel Src inhibitors: Pharmacophore-based virtual screening, molecular docking and molecular dynamics simulations

Y Zhang, T Zhang, S Tu, Z Zhang, F Meng - Molecules, 2020 - mdpi.com
Src plays a crucial role in many signaling pathways and contributes to a variety of cancers.
Therefore, Src has long been considered an attractive drug target in oncology. However, the …

Functional genomic screening independently identifies CUL3 as a mediator of vemurafenib resistance via Src-Rac1 signaling axis

M Vanneste, CR Feddersen, A Varzavand… - Frontiers in …, 2020 - frontiersin.org
Patients with malignant melanoma have a 5-year survival rate of only 15–20% once the
tumor has metastasized to distant tissues. While MAP kinase pathway inhibitors (MAPKi) are …

SRC-RAC1 signaling drives drug resistance to BRAF inhibition in de-differentiated cutaneous melanomas

EY Zhu, JD Riordan, M Vanneste, MD Henry… - NPJ precision …, 2022 - nature.com
Rare gain-of-function mutations in RAC1 drive drug resistance to targeted BRAF inhibition in
cutaneous melanoma. Here, we show that wildtype RAC1 is a critical driver of growth and …

Machine learning approach informs biology of cancer drug response

EY Zhu, AJ Dupuy - BMC bioinformatics, 2022 - Springer
Background The mechanism of action for most cancer drugs is not clear. Large-scale
pharmacogenomic cancer cell line datasets offer a rich resource to obtain this knowledge …

p21-Activated kinases in thyroid cancer

L Bautista, CM Knippler, MD Ringel - Endocrinology, 2020 - academic.oup.com
The family of p21-activated kinases (PAKs) are oncogenic proteins that regulate critical
cellular functions. PAKs play central signaling roles in the integrin/CDC42/Rho, ERK/MAPK …

[HTML][HTML] BH3 mimetics potentiate pro-apoptotic activity of encorafenib in BRAFV600E melanoma cells

ML Hartman, A Gajos-Michniewicz, JA Talaj… - Cancer Letters, 2021 - Elsevier
Abstract BRAF V600-and MEK1/2-targeting therapies rarely produce durable response in
melanoma patients. We investigated five BRAF V600E melanoma cell lines derived from …

Single-cell genomics analysis reveals complex genetic interactions in an in vivo model of acquired BRAF inhibitor resistance

JL Schillo, CR Feddersen, RM Peplinski… - NAR …, 2024 - academic.oup.com
The evolution of therapeutic resistance is a major obstacle to the success of targeted
oncology drugs. While both inter-and intratumoral heterogeneity limit our ability to detect …