Tackling Undruggable Targets with Designer Peptidomimetics and Synthetic Biologics

CS Swenson, G Mandava, DM Thomas… - Chemical …, 2024 - ACS Publications
The development of potent, specific, and pharmacologically viable chemical probes and
therapeutics is a central focus of chemical biology and therapeutic development. However, a …

Navigating the ERK1/2 MAPK cascade

A Martin-Vega, MH Cobb - Biomolecules, 2023 - mdpi.com
The RAS-ERK pathway is a fundamental signaling cascade crucial for many biological
processes including proliferation, cell cycle control, growth, and survival; common across all …

Ras suppression potentiates rear actomyosin contractility-driven cell polarization and migration

Y Lin, DS Pal, P Banerjee, T Banerjee, G Qin… - Nature cell …, 2024 - nature.com
Ras has been extensively studied as a promoter of cell proliferation, whereas few studies
have explored its role in migration. To investigate the direct and immediate effects of Ras …

Mechanism-Based Redesign of GAP to Activate Oncogenic Ras

D Berta, S Gehrke, K Nyíri, BG Vértessy… - Journal of the American …, 2023 - ACS Publications
Ras GTPases play a crucial role in cell signaling pathways. Mutations of the Ras gene occur
in about one third of cancerous cell lines and are often associated with detrimental clinical …

D3S-001, a KRAS G12C inhibitor with rapid target engagement kinetics, overcomes nucleotide cycling, and demonstrates robust preclinical and clinical activities

J Zhang, SM Lim, MR Yu, C Chen, J Wang… - Cancer …, 2024 - aacrjournals.org
Abstract First-generation KRAS G12C inhibitors, such as sotorasib and adagrasib, are
limited by the depth and duration of clinical responses. One potential explanation for their …

Functional and structural insights into RAS effector proteins

AM Mozzarelli, DK Simanshu, P Castel - Molecular cell, 2024 - cell.com
RAS proteins are conserved guanosine triphosphate (GTP) hydrolases (GTPases) that act
as molecular binary switches and play vital roles in numerous cellular processes. Upon GTP …

Conditional Cooperativity in RAS Assembly Pathways on Nanodiscs and Altered GTPase Cycling

SY Lee, KY Lee - Angewandte Chemie, 2024 - Wiley Online Library
Abstract Self‐assemblies (ie, nanoclusters) of the RAS GTPase on the membrane act as
scaffolds that activate downstream RAF kinases and drive MAPK signaling for cell …

[HTML][HTML] KRAS Mutation Subtypes and Their Association with other driver mutations in oncogenic pathways

K Mondal, MK Posa, RP Shenoy, S Roychoudhury - Cells, 2024 - mdpi.com
The KRAS mutation stands out as one of the most influential oncogenic mutations, which
directly regulates the hallmark features of cancer and interacts with other cancer-causing …

[HTML][HTML] Single cell spatial biology over developmental time can decipher pediatric brain pathologies

R Nussinov, BR Yavuz, H Jang - Neurobiology of Disease, 2024 - Elsevier
Pediatric low grade brain tumors and neurodevelopmental disorders share proteins,
signaling pathways, and networks. They also share germline mutations and an impaired …

Electric field modulation of ERK dynamics shows dependency on waveform and timing

M Hu, H Li, K Zhu, L Guo, M Zhao, H Zhan… - Scientific reports, 2024 - nature.com
Different exogenous electric fields (EF) can guide cell migration, disrupt proliferation, and
program cell development. Studies have shown that many of these processes were initiated …