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GENE:

PIM1 (Pim-1 Proto-Oncogene)

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Other names: PIM1, Pim-1 Proto-Oncogene, Serine/Threonine Kinase, Serine/Threonine-Protein Kinase Pim-1, Proto-Oncogene Serine/Threonine-Protein Kinase Pim-1, Pim-1 Oncogene (Proviral Integration Site 1), Pim-1 Kinase 44 KDa Isoform, Pim-1 Oncogene, Oncogene PIM1, PIM
12d
Structure-guided design and evaluation of oxazolone-based PIM-1 kinase inhibitors with promising anticancer activity. (PubMed, J Biomol Struct Dyn)
Collectively, these results indicate that O29 is the most promising candidate among the tested derivatives, offering high-affinity binding and efficient kinase inhibition. These findings suggest the therapeutic potential of oxazolone-based scaffolds as lead compounds for the development of potent PIM-1 inhibitors in prostate cancer treatment.
Journal
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PIM1 (Pim-1 Proto-Oncogene)
21d
JAK2V617F reprograms Hypoxia Inducible Factor-1 to induce a non-canonical hypoxia regulon in myeloproliferative neoplasms. (PubMed, Leukemia)
Our findings demonstrate that HIF-1 activation by the JAK2V617F-PIM1 axis significantly alters HIF-1 transcription function, desensitising HIF-1 activity to cellular oxygen levels, and restricting the HIF-1 regulon to a set of disease-associated target genes within JAK2V617F-MPNs. These findings restore the potential for specific therapeutic targeting of HIF-1 by delineating malignant activation from the physiological hypoxic response.
Journal • JAK2V617F
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HIF1A (Hypoxia inducible factor 1, alpha subunit) • PIM1 (Pim-1 Proto-Oncogene)
1m
Reconnecting new tetrahydrobenzothieno-4-pyrimidine amides as potent PIM-1 kinase inhibitors via an integrated ligand, machine learning model and structure based scaffold hopping: In vitro anti-tumor investigations. (PubMed, Bioorg Chem)
Compound 7 k portrayed an excellent in silico ADME and drug likeness attributes with predictive absorption percentile of 91.15. Aforesaid outcomes revealed that 7 k recognized as promising lead candidate for development of novel PIM kinases inhibitors as anticancer agents.
Preclinical • Journal
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PIM1 (Pim-1 Proto-Oncogene)
1m
In Silico Identification of Lepiotaprocerin C as a Promising PIM-1 Kinase Inhibitor: An Integrated Docking, Molecular Dynamics, MM/PBSA, QSAR, and ADMET Study. (PubMed, Bioinform Biol Insights)
Molecular docking of 12 Lepiotaprocerins revealed Lepiotaprocerin C as the most potent compound, exhibiting superior binding affinity (-11.4 kcal/mol) compared with the reference inhibitor AZD1208...Prediction of Activity Spectra for Substances and toxicity predictions further revealed high antineoplastic potential (Pa = 0.881) and a nontoxic safety profile. These results highlight Lepiotaprocerin C as a promising, stable, and safe inhibitor of PIM-1 kinase, warranting further in vitro and in vivo validation for potential anticancer drug development.
Journal
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PIM1 (Pim-1 Proto-Oncogene)
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AZD1208
2ms
PIM kinase inhibition attenuates pro-tumoral and immunosuppressive functions of macrophages in classic Hodgkin lymphoma. (PubMed, Cell Death Dis)
PIM blockade attenuated TAM-dependent eosinophil chemoattraction, extracellular matrix remodeling, angiogenesis and regulatory T-cell development. Taken together, our study highlights the role of PIMs in the regulation of pathogenic TAM functions in cHL, further supporting the rationale of PIM targeting in this disease.
Journal • PD(L)-1 Biomarker • IO biomarker
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PD-L1 (Programmed death ligand 1) • CXCL8 (Chemokine (C-X-C motif) ligand 8) • IDO1 (Indoleamine 2,3-dioxygenase 1) • CHI3L1 (Chitinase 3-like 1) • PIM1 (Pim-1 Proto-Oncogene) • TGFB1 (Transforming Growth Factor Beta 1) • MMP9 (Matrix metallopeptidase 9) • MRC1 (Mannose Receptor C-Type 1) • IL4I1 (Interleukin 4 Induced 1)
2ms
High penetrance rare variants underlying familial lung cancer risk: Insights from genetic epidemiology of lung cancer consortium. (PubMed, J Thorac Oncol)
Our findings underscore the significant role of rare, high-penetrance genetic variants in FLC susceptibility, particularly in mucin glycosylation and DNA repair genes. These findings offer promising targets for early detection and personalized therapies.
Journal • BRCA Biomarker
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BRCA2 (Breast cancer 2, early onset) • ROS1 (Proto-Oncogene Tyrosine-Protein Kinase ROS) • ERBB3 (V-erb-b2 avian erythroblastic leukemia viral oncogene homolog 3) • MLH1 (MutL homolog 1) • JAK1 (Janus Kinase 1) • PIM1 (Pim-1 Proto-Oncogene) • MUC4 (Mucin 4, Cell Surface Associated) • EBF1 (EBF Transcription Factor 1) • COL6A3 (Collagen Type VI Alpha 3 Chain) • SYNE1 (Spectrin Repeat Containing Nuclear Envelope Protein 1)
2ms
Cytotoxic and apoptotic activity of Satureja sahendica Bornm essential oil in MDA-MB-231 breast cancer and A549 lung cancer cells: in vitro evidence. (PubMed, 3 Biotech)
Collectively, these findings demonstrate that SSEO exerts cytotoxic effects primarily through the induction of apoptosis in both breast and lung cancer cells, highlighting its potential as a complementary anticancer agent. The online version contains supplementary material available at 10.1007/s13205-025-04656-0.
Preclinical • Journal
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TOP2A (DNA topoisomerase 2-alpha) • NFKB1 (Nuclear factor of kappa light polypeptide gene enhancer in B-cells 1) • PIM1 (Pim-1 Proto-Oncogene) • CTSD (Cathepsin D) • KIFC1 (Kinesin Family Member C1) • ANXA5 (Annexin A5) • MAPK14 (Mitogen-Activated Protein Kinase 14)
3ms
Ensemble Guided Fine-Tuning Pre-Trained Models for Kinase Inhibitor Design. (PubMed, Annu Int Conf IEEE Eng Med Biol Soc)
The iterative feedback mechanism further ensures chemical novelty and biological significance, showcasing the potential of EGFit to optimize compound generation for kinase-specific applications. This framework offers a scalable and effective solution to the challenges of kinase drug discovery, accelerating the development of novel therapeutics and paving the way for broader applications in future studies.
Journal
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EGFR (Epidermal growth factor receptor) • PIM1 (Pim-1 Proto-Oncogene)
3ms
Mechanism of triptolide in the treatment of gastric cancer with diabetes through JAK2/STAT3 pathway. (PubMed, Eur J Pharmacol)
Diabetes is an independent prognostic risk factor for patients with gastric cancer. Triptolide reverses the malignant phenotype of gastric cancer cells induced by high glucose by targeting the PIM1-JAK2/STAT3 signalling axis, providing an experimental basis for the precise treatment of patients with gastric cancer with diabetes.
Journal
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PIM1 (Pim-1 Proto-Oncogene)
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.
Journal
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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)
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TP53 mutation
3ms
Identification and Validation of an inhibitor of the protein kinases PIM and DYRK. (PubMed, bioRxiv)
Functionally, CSH-4044 suppressed PIM3-driven BAD phosphorylation in pancreatic cancer cells and reduced DYRK1A-mediated Tau phosphorylation in neuronal cells. Our findings position CSH-4044 as a promising lead for targeting PIM and DYRK families of kinases and highlight FWGE as a source of potential therapeutic compounds.
Journal
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PIM1 (Pim-1 Proto-Oncogene)
3ms
CBX7 regulates chemotherapy-induced senescence-like growth arrest in multiple myeloma via the ERK/STAT3/PIM1 axis. (PubMed, J Transl Med)
CBX7 is a pivotal target for regulating cellular senescence in myeloma cells, operating through a novel CBX7/ERK/PIM1 regulatory axis. Targeting CBX7 and its downstream pathways may augment the efficacy of standard chemotherapy.
Journal
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B2M (Beta-2-microglobulin) • STAT3 (Signal Transducer And Activator Of Transcription 3) • PIM1 (Pim-1 Proto-Oncogene)
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bortezomib