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RASGRF1 (Ras Protein Specific Guanine Nucleotide Releasing Factor 1)

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26d

A Decade-Old Atlas of TMEM (Transmembrane) Protein Family in Lung Cancer: Lessons Learnt and Future Directions. (PubMed, Int J Mol Sci)

Yet for most TMEMs, only pre-clinical or early-phase data exist, with many supported by a single study lacking independent validation. This review brings together scattered evidence on TMEM proteins in lung cancer, with the aim of guiding future work on their possible use as biomarkers or therapeutic targets.

26 days ago

Review • Journal • IO biomarker

ROS1 (Proto-Oncogene Tyrosine-Protein Kinase ROS) • STING (stimulator of interferon response cGAMP interactor 1) • ANO1 (Anoctamin 1) • RASGRF1 (Ras Protein Specific Guanine Nucleotide Releasing Factor 1) • TMEM87A (Transmembrane Protein 87A)

Neutrophil-hijacking vesicles suppress NET-mediated metastasis via targeted siRNA delivery after radiotherapy. (PubMed, J Control Release)

Concurrently, activated neutrophils secrete cytotoxic and immunostimulatory factors, enhancing anti-tumor immunity. This strategy synergizes immune modulation with gene silencing to amplify RT efficacy and suppress metastasis, offering a safe and translatable approach to overcome RT-induced tumor progression.

1 month ago

Journal

RASGRF1 (Ras Protein Specific Guanine Nucleotide Releasing Factor 1) • CCDC25 (Coiled-Coil Domain Containing 25)

2ms

First-in-Class Quinoline-Dione-Derived PROTACs: Potent Degraders of Cdc25 Phosphatases for Antitumor Therapy. (PubMed, J Med Chem)

Mechanistically, D3 exerts antitumor effects by degrading the target protein Cdc25, upregulating p-CDK1/2 levels, and subsequently inducing G2/M phase cell cycle arrest and apoptosis. This study validates PROTACs as a breakthrough strategy to target "undruggable" Cdc25, provides a novel quinoline-dione-based scaffold for antitumor drug development, and offers a rational design paradigm for tackling intractable phosphatase targets.

2 months ago

Journal

CDK1 (Cyclin-dependent kinase 1) • RASGRF1 (Ras Protein Specific Guanine Nucleotide Releasing Factor 1) • CDC25A (Cell Division Cycle 25A) • GNRP (Ras-Specific Guanine Nucleotide-Releasing Factor 1)

2ms

Chemical modification of STL427944 toward morpholine-based 1,3,5-triazines as anticancer agents targeting FOXM1: green synthesis, biological evaluation and ADME-Tox profiling in a colorectal cancer model. (PubMed, Eur J Med Chem)

It was more potent than 5-fluorouracil in SW620 cells (IC50 = 21.7 μM)...Overall, compound 14 significantly outperformed the original hit (STL427944), achieving FOXM1 inhibition at <12.5 μM (vs. 25-50 μM for STL). This marks it as a next-generation FOXM1-targeting lead, combining potent and selective anticancer activity with sustainable synthesis, and positioning it as a strong candidate for further preclinical development.

2 months ago

Preclinical • Journal

PIK3CG (Phosphatidylinositol-4,5-Bisphosphate 3-Kinase Catalytic Subunit Gamma) • FOXM1 (Forkhead Box M1) • CYP3A4 (Cytochrome P450, family 3, subfamily A, polypeptide 4) • RASGRF1 (Ras Protein Specific Guanine Nucleotide Releasing Factor 1) • CCNB1 (Cyclin B1) • GNRP (Ras-Specific Guanine Nucleotide-Releasing Factor 1)

5-fluorouracil

2ms

Tumor-derived neutrophil extracellular trap-associated DNA impairs treatment efficacy in breast cancer via CCDC25-dependent epithelial-mesenchymal transition. (PubMed, J Clin Invest)

Clinically, tumoral CCDC25 abundance is closely associated with poor prognosis in patients who underwent chemotherapy. Overall, our data reveal the mechanism of NET formation and elucidate the interaction of NET-CCDC25 in therapy resistance, highlighting CCDC25 as an appealing target for anticancer interventions.

2 months ago

Journal

TLR4 (Toll Like Receptor 4) • CFB (Complement Factor B) • RASGRF1 (Ras Protein Specific Guanine Nucleotide Releasing Factor 1) • CCDC25 (Coiled-Coil Domain Containing 25) • CXCL1 (Chemokine (C-X-C motif) ligand 1)

2ms

Identification of hub genes and signaling pathways as possible therapeutic targets in human glioblastoma: evidenced by bioinformatics analysis. (PubMed, Brain Res)

THBS1 and ENG are significant prognostic biomarkers and potential therapeutic targets in GBM. Their strong correlation with immunosuppressive M2 macrophage infiltration implicates actin cytoskeleton remodeling pathways in GBM-mediated immune evasion. Targeting these hub genes may disrupt critical tumor microenvironment interactions, offering new avenues for therapy.

2 months ago

Journal

CD31 (Platelet and endothelial cell adhesion molecule 1) • PECAM1 (Platelet And Endothelial Cell Adhesion Molecule 1) • RASGRF1 (Ras Protein Specific Guanine Nucleotide Releasing Factor 1) • TGFB2 (Transforming Growth Factor Beta 2)

3ms

A novel dual CDC25-HDAC inhibitor suppresses glioblastoma progression via chromosomal passenger complex disruption. (PubMed, Biomed Pharmacother)

Glioblastoma (GBM) is a highly aggressive and therapeutically challenging brain tumor characterized by poor prognosis, rapid recurrence, and resistance to standard treatments such as temozolomide (TMZ)...Disruption of CPC function led to reduced mitotic activity and increased mitotic defects in treated cultures. Collectively, these findings indicate that dual inhibition of CDC25 and HDAC by MPT1B394 disrupts CPC-mediated mitosis and aberrant cell cycle progression, representing a promising therapeutic avenue for GBM treatment.

3 months ago

Journal

BIRC5 (Baculoviral IAP repeat containing 5) • PLK1 (Polo Like Kinase 1) • CCNA2 (Cyclin A2) • RASGRF1 (Ras Protein Specific Guanine Nucleotide Releasing Factor 1) • CCNB1 (Cyclin B1) • CDCA8 (Cell Division Cycle Associated 8) • CENPA (Centromere protein A) • GNRP (Ras-Specific Guanine Nucleotide-Releasing Factor 1) • MCM5 (Minichromosome Maintenance Complex Component 5)

temozolomide

3ms

Gene Expression Profiling Provides an Improved Characterization of CD79B-Mutated Diffuse Large B-Cell Lymphomas. (PubMed, J Pers Med)

TP53 mutation showed an association with poorer overall survival in a secondary analysis, consistent with prior reports, while survival by CD79B/MYD88 mutation status and the differentially expressed genes showed no significant differences in this cohort. In conclusion, the current study identified novel up-regulated genes in CD79B-mutated DLBCLs beyond NF-κB pathway signaling, which may contribute to a better definition of potential therapeutic targets and further improves the characterization of this distinct and aggressive DLBCL subgroup.

3 months ago

Journal

TP53 (Tumor protein P53) • MYD88 (MYD88 Innate Immune Signal Transduction Adaptor) • RUNX1 (RUNX Family Transcription Factor 1) • CD79B (CD79b Molecule) • RUNX1T1 (RUNX1 Partner Transcriptional Co-Repressor 1) • STAT3 (Signal Transducer And Activator Of Transcription 3) • CARD11 (Caspase Recruitment Domain Family Member 11) • IL10 (Interleukin 10) • CD14 (CD14 Molecule) • PIM1 (Pim-1 Proto-Oncogene) • BCL2A1 (BCL2 Related Protein A1) • GZMB (Granzyme B) • IL7 (Interleukin 7) • RASGRF1 (Ras Protein Specific Guanine Nucleotide Releasing Factor 1) • AFDN (Afadin, Adherens Junction Formation Factor) • HSP90AB1 (Heat Shock Protein 90 Alpha Family Class B Member 1) • WNT11 (Wnt Family Member 11)

TP53 mutation

5ms

Acrylamide-mediated errors in the cell cycle regulation are associated with altered TORC2 signaling in Schizosaccharomyces pombe. (PubMed, Sci Rep)

The stress response involves signaling pathways like MAPKs (Mitogen-activated protein kinases) or the target of rapamycin (TOR) constituting two complexes TORC 1 and 2...To our surprise, AA has not affected the expression of sty1, which encodes the major stress-regulating kinase of the MAPK pathway in S. pombe. In the presented study we demonstrate, for the first time, that exposure to AA disrupts cellular homeostasis by altering TORC2 signaling and cell cycle regulation ultimately leading to carcinogenesis.

5 months ago

Journal

AURKA (Aurora kinase A) • CDK1 (Cyclin-dependent kinase 1) • RASGRF1 (Ras Protein Specific Guanine Nucleotide Releasing Factor 1) • GNRP (Ras-Specific Guanine Nucleotide-Releasing Factor 1)

sirolimus

5ms

Quinoline-5,8-dione CDC25 inhibitors: Potent anti-cancer agents in leukemia and patient-derived colorectal organoids. (PubMed, Eur J Med Chem)

Notably, efficacy was validated in colorectal cancer patient-derived organoids, providing clinically relevant insights into patient-specific responses. Together, these findings define a new class of CDC25 inhibitors with potent and selective anticancer activity, advancing prospects for next-generation therapeutics in leukemia and colorectal cancer.

5 months ago

Journal

CDC25C (Cell Division Cycle 25C) • CDK1 (Cyclin-dependent kinase 1) • RASGRF1 (Ras Protein Specific Guanine Nucleotide Releasing Factor 1) • GNRP (Ras-Specific Guanine Nucleotide-Releasing Factor 1)

5ms

Evaluation of anti-liver cancer activity and anticancer mechanism of one novel small molecule compound (THY-10A62) targeting FAK pathway. (PubMed, Front Oncol)

Efficacy was benchmarked against PF-562271...The observed reductions in FAK phosphorylation and changes in BRAF and RASGRF1 phosphorylation suggest pathway-level modulation underlying efficacy. These findings provide preliminary evidence that THY-10A62 is a potential FAK inhibitor for liver cancer therapy and warrant further studies to refine dosing, characterize pharmacokinetics/toxicity, and validate efficacy across additional HCC models.

5 months ago

Journal

BRAF (B-raf proto-oncogene) • RASGRF1 (Ras Protein Specific Guanine Nucleotide Releasing Factor 1)

benzesulfonate (PF-562271)

6ms

A novel quinoid-based CDC25 phosphatase inhibitor against human lung adenocarcinoma across different models. (PubMed, Biomed Pharmacother)

Combination studies of compound 6 with chemotherapeutic drugs indicated that compound 6 exhibited synergistic effects with those drugs in inhibiting the growth of LUAD cells. In conclusion, compound 6 is a promising lead compound for CDC25 inhibition and warrants further investigation as a potential therapeutic agent for LUAD treatment.

6 months ago

Journal

CDC25C (Cell Division Cycle 25C) • RASGRF1 (Ras Protein Specific Guanine Nucleotide Releasing Factor 1) • CDC25A (Cell Division Cycle 25A) • GNRP (Ras-Specific Guanine Nucleotide-Releasing Factor 1)