Targeting pak1

G Semenova, J Chernoff - Biochemical Society Transactions, 2017 - portlandpress.com
p21-Activated kinase 1 (PAK1) has attracted much attention as a potential therapeutic target
due to its central role in many oncogenic signaling pathways, its frequent dysregulation in …

[HTML][HTML] Emerging pharmaceutical therapies of Ascidian-derived natural products and derivatives

K Cooreman, B De Spiegeleer, C Van Poucke… - Environmental …, 2023 - Elsevier
In a growing multidrug-resistant environMent, the identification of potential new drug
candidates with an acceptable safety profile is a substantial crux in pharmaceutical …

Genetic effects of DSCAML1 identified in genome-wide association study revealing strong associations with litter size and semen quality in goat (Capra hircus)

K Wang, Z Kang, E Jiang, H Yan, H Zhu, J Liu, L Qu… - Theriogenology, 2020 - Elsevier
The down syndrome cell adhesion molecule like 1 (DSCAML1), is associated with the
development of the nervous system and neurologic diseases. Previous Genome-wide …

HACE1-mediated NRF2 activation causes enhanced malignant phenotypes and decreased radiosensitivity of glioma cells

C Da, J Pu, Z Liu, J Wei, Y Qu, Y Wu, B Shi… - … and Targeted Therapy, 2021 - nature.com
Abstract HACE1, an E3 ubiquitin-protein ligase, is frequently inactivated and has been
evidenced as a putative tumor suppressor in different types of cancer. However, its role in …

Combined inhibition of Aurora A and p21-activated kinase 1 as a new treatment strategy in breast cancer

V Korobeynikov, M Borakove, Y Feng… - Breast cancer research …, 2019 - Springer
Purpose The serine-threonine kinases Aurora A (AURKA) and p21-activated kinase 1
(PAK1) are frequently overexpressed in breast tumors, with overexpression promoting …

Development and utility of a PAK1-selective degrader

HY Chow, S Karchugina, BJ Groendyke… - Journal of medicinal …, 2022 - ACS Publications
Overexpression of PAK1, a druggable kinase, is common in several malignancies, and
inhibition of PAK1 by small molecules has been shown to impede the growth and survival of …

Chemically diverse group I p21-activated kinase (PAK) inhibitors impart acute cardiovascular toxicity with a narrow therapeutic window

J Rudolph, LJ Murray, CO Ndubaku… - Journal of medicinal …, 2016 - ACS Publications
p21-activated kinase 1 (PAK1) has an important role in transducing signals in several
oncogenic pathways. The concept of inhibiting this kinase has garnered significant interest …

Functional proteomics interrogation of the kinome identifies MRCKA as a therapeutic target in high-grade serous ovarian carcinoma

AM Kurimchak, C Herrera-Montávez, J Brown… - Science …, 2020 - science.org
High-grade serous ovarian carcinoma (HGSOC) is the most lethal gynecological cancer with
few effective, targeted therapies. HGSOC tumors exhibit genomic instability with frequent …

RPL22L1 induction in colorectal cancer is associated with poor prognosis and 5-FU resistance

S Rao, S Peri, J Hoffmann, KQ Cai, B Harris… - PLoS …, 2019 - journals.plos.org
We have previously demonstrated that loss of the tumor suppressive activity of ribosomal
protein (RP) RPL22 predisposes to development of leukemia in mouse models and …

Salmonella stimulates pro-inflammatory signalling through p21-activated kinases bypassing innate immune receptors

H Sun, J Kamanova, M Lara-Tejero, JE Galán - Nature microbiology, 2018 - nature.com
Microbial infections are most often countered by inflammatory responses that are initiated
through the recognition of conserved microbial products by innate immune receptors and …