-
121
A Rational Design of α-Helix-Shaped Peptides Employing the Hydrogen-Bond Surrogate Approach: A Modulation Strategy for Ras-RasGRF1 Interaction in Neuropsychiatric Disorders
Published 2021-10-01“…Previously, we showed that a cell penetrating peptide, RB3, was able to inhibit downstream signalling by preventing RasGRF1 (Ras guanine nucleotide-releasing factor 1), a neuronal specific GDP/GTP exchange factor, to bind Ras proteins, both in brain slices and in vivo, with an IC<sub>50</sub> value in the micromolar range. …”
Get full text
Article -
122
Characterisation of a cyclic peptide that binds to the RAS binding domain of phosphoinositide 3-kinase p110α
Published 2023-02-01“…Abstract P110α is a member of the phosphoinositide 3-kinase (PI3K) enzyme family that functions downstream of RAS. RAS proteins contribute to the activation of p110α by interacting directly with its RAS binding domain (RBD), resulting in the promotion of many cellular functions such as cell growth, proliferation and survival. …”
Get full text
Article -
123
Targeting KRAS in Solid Tumors: Current Challenges and Future Opportunities of Novel KRAS Inhibitors
Published 2021-05-01“…Historically, KRAS has been acknowledged as “undruggable”, largely because the RAS proteins do not appear to present suitable pockets to which small inhibitory molecules can bind. …”
Get full text
Article -
124
A Small Molecule Promoting Neural Differentiation Suppresses Cancer Stem Cells in Colorectal Cancer
Published 2022-04-01“…We previously showed that CPD0857 inactivates Wnt/β-catenin signaling by promoting the ubiquitin-dependent proteasomal degradation of β-catenin and Ras proteins, thereby decreasing proliferation and increasing the apoptosis of CRC lines. …”
Get full text
Article -
125
Mechanistic insights on anticancer drugs with specific biological targets and signalling pathways
Published 2023-09-01“…As a result of mutations or altered signalling, rat sarcoma (RAS) proteins regulate signalling, which is essential for both healthy growth and the development of cancer. …”
Get full text
Article -
126
Autophagy Stimulus-Dependent Role of the Small GTPase Ras2 in Peroxisome Degradation
Published 2020-11-01“…Yeast Ras2 is homologous to the mammalian Ras proteins, whose mutant forms are responsible for 33% of human cancers. …”
Get full text
Article -
127
RAB27B controls palmitoylation-dependent NRAS trafficking and signaling in myeloid leukemia
Published 2023-06-01“…RAS mutations are among the most prevalent oncogenic drivers in cancers. RAS proteins propagate signals only when associated with cellular membranes as a consequence of lipid modifications that impact their trafficking. …”
Get full text
Article -
128
Andrographolide derivatives inhibit guanine nucleotide exchange and abrogate oncogenic Ras function
Published 2013“…Aberrant signaling by oncogenic mutant rat sarcoma (Ras)proteins occurs in ∼15% of all human tumors, yet direct inhibition of Ras by small molecules has remained elusive. …”
Book Section -
129
Pharmacological modulation of oncogenic Ras by natural products and their derivatives: renewed hope in the discovery of novel anti-Ras drugs
Published 2016“…The anti-Ras strategy of these compounds can be categorized into four main types: inhibition of Ras–effector interaction, interference of Ras membrane association, prevention of Ras–guanosine triphosphate (GTP) formation, and downregulation of Ras proteins. Another promising strategy that must be validated experimentally is enhancement of the intrinsic Ras–guanosine triphosphatase (GTPase) activity by small chemical entities. …”
Get full text
Conference or Workshop Item -
130
Liprin‐α1 contributes to oncogenic MAPK signaling by counteracting ERK activity
Published 2024-03-01“…Furthermore, liprin‐α1 depletion led to more pronounced redistribution of RAS proteins to the cell membrane. Our data suggest that liprin‐α1 is an important contributor to oncogenic RAS/MAPK signaling, and the status of liprin‐α1 may assist in predicting drug responses in cancer cells in a context‐dependent manner.…”
Get full text
Article -
131
Detection of Ras nanoclustering-dependent homo-FRET using fluorescence anisotropy measurements
Published 2023-06-01“…Nanoclusters contain only a few Ras proteins and are necessary for the recruitment of downstream effectors, such as Raf. …”
Get full text
Article -
132
Novel Insights into the Role of Kras in Myeloid Differentiation: Engaging with Wnt/β-Catenin Signaling
Published 2023-01-01“…This review focuses on the differentiation of HL-60 cells. Although the Ras proteins, a group of small GTP-binding proteins, are ubiquitously expressed and highly homologous, each has specific molecular functions. …”
Get full text
Article -
133
-
134
Protein-based Degrader Strategies against Oncogenic RAS
Published 2023“…Targeted therapies have emerged as a promising cancer treatment strategy by inhibiting proteins specific to cancer cells while preserving healthy cells. RAS proteins play a crucial role in cancer development and are associated with increased tumor growth and invasion. …”
Get full text
Thesis -
135
Novel Therapeutic Approaches for KRAS-Mutated Lung Cancer Involving LZTR1 Genetic Alteration
Published 2023-03-01“…LZTR1 is an adaptor of CUL3 E3 ligase that controls the localization and expression levels of RAS proteins by regulating their ubiquitination. Recent studies demonstrated that the loss of <i>LZTR1</i> leads to resistance to the tyrosine kinase inhibitor and the multi-kinase inhibitor, suggesting that <i>LZTR1</i> loss might be associated with the drug resistance of KRAS-mutated lung tumors. …”
Get full text
Article -
136
C3G Is Upregulated in Hepatocarcinoma, Contributing to Tumor Growth and Progression and to HGF/MET Pathway Activation
Published 2020-08-01“…C3G, a guanine nucleotide exchange factor for Rap and other Ras proteins, plays a dual role in cancer acting as either a tumor suppressor or promoter depending on tumor type and stage. …”
Get full text
Article -
137
Regulation of cell signalling by iRhoms
Published 2019“…Oncogenic KRas and HRas stimulate TACE activity, which demonstrates the conserved role of Ras proteins in stimulating the release of EGFR ligands by TACE. …”
Thesis -
138
Pathogen-specific structural features of Candida albicans Ras1 activation complex: uncovering new antifungal drug targets
Published 2023-08-01“…An important function in hyphal growth has also been proposed for the long hypervariable region downstream the G-domain, whose unusual content of polyglutamine stretches and Q/N repeats make CaRas1 unique within Ras proteins. Despite its biological importance, both the structure of CaRas1 and the molecular basis of its activation by CaCdc25 remain unexplored. …”
Get full text
Article -
139
RGD-p21Ras-scFv expressed prokaryotically on a pilot scale inhibits ras-driven colorectal cancer growth by blocking p21Ras-GTP
Published 2024-01-01“…ELISA was adopted to test the immunoreactivity of RGD-p21Ras-scFv against p21Ras proteins, and the IC50 of RGD-p21Ras-scFv was analyzed by CCK-8. …”
Get full text
Article -
140
Functional characterization of Rasd1 : a novel interaction between Rasd1 and Ear2 (NR2F6) is involved in the regulation of renin transcription
Published 2012“…The characteristic GTP binding and hydrolysis properties of Ras proteins render Rasd1 extremely important in numerous signaling pathways and physiological processes. …”
Get full text
Thesis