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DRUG CLASS:

Phosphotransferase inhibitor

7d
CLIP170 inhibits the metastasis and EMT of papillary thyroid cancer through the TGF-β pathway. (PubMed, Med Oncol)
Remarkably, the TGF-β inhibitor LY2157299 effectively countered TGF-β activity and significantly reversed tumor metastasis and EMT induced by CLIP170 knockdown. In summary, these findings collectively propose CLIP170 as a promising therapeutic target to mitigate metastatic tendencies in PTC.
Journal
|
TGFB1 (Transforming Growth Factor Beta 1) • CLIP1 (CAP-Gly Domain Containing Linker Protein 1)
|
galunisertib (LY2157299)
18d
MicroRNA-431-5p inhibits angiogenesis, lymphangiogenesis, and lymph node metastasis by affecting TGF-β1/SMAD2/3 signaling via ZEB1 in gastric cancer. (PubMed, Mol Carcinog)
Additionally, miR-431-5p enhances the efficacy of anti-PD1 treatment, particularly when combined with galunisertib, anti-PD1 treatment showing a synergistic effect in inhibiting GC progression in C57BL/6 mice. Collectively, these findings suggest that miR-431-5p may modulate the TGF-β1/SMAD2/3 pathways by targeting ZEB1 to impede GC progression, angiogenesis, and lymphangiogenesis, making it a promising therapeutic target for GC management.
Journal • PD(L)-1 Biomarker • IO biomarker
|
TGFB1 (Transforming Growth Factor Beta 1) • ZEB1 (Zinc Finger E-box Binding Homeobox 1)
|
galunisertib (LY2157299)
1m
Long Term Extension Study of Tapinarof Cream, 1% for Subjects With Atopic Dermatitis (clinicaltrials.gov)
P3, N=728, Completed, Dermavant Sciences, Inc. | Recruiting --> Completed | Trial completion date: Sep 2024 --> Mar 2024 | Trial primary completion date: Jul 2024 --> Feb 2024
Trial completion • Trial completion date • Trial primary completion date
3ms
Nano-chemical priming strategy to enhance TGF-β resistance and anti-tumor activity of natural killer cells. (PubMed, J Control Release)
Based on these findings, we designed nanogels that have two primary characteristics: (1) they encapsulate galunisertib (Gal), which is used clinically to inhibit TGF-β receptor activity, thereby blocking TGF-β signaling; and (2) they provide cells with a surface coating of 25 K bPEI...These findings suggest that Gal-loaded 25 K bPEI-coated nanogels exert anti-tumor effects via chemical priming, as well suppressing the effects of TGF-β on NK cells. We also expect 25 K bPEI-based nanogels to have great potential to overcome the suppressive effects of the TME through their NK cell-priming activity and delivery of the desired chemicals.
Journal
|
TGFB1 (Transforming Growth Factor Beta 1)
|
galunisertib (LY2157299)
3ms
TGFβR1 inhibition drives hepatocellular carcinoma proliferation through induction of toll-like-receptor signalling. (PubMed, Int J Exp Pathol)
Effects of constant activation of the SMAD pathway by constitutive expression of ALK5 or knockdown of mediators of TLR signalling, IRAK1 and MyD88, on HCC proliferation, were investigated in the HCC cell line (HUH-7) after treatment with TGFβ1 cytokine or TGFβR1 kinase inhibitor (LY2157299) using PCNA and MTS assay...There is a balance between the canonical SMAD-driven tumour-suppressing arm and the non-canonical tumour-promoting arm of TGFβ signalling. Disruption of this balance, by inhibition of the canonical pathway, induces HCC proliferation through TLR signalling.
Journal • IO biomarker
|
MYD88 (MYD88 Innate Immune Signal Transduction Adaptor) • TLR9 (Toll Like Receptor 9) • TGFB1 (Transforming Growth Factor Beta 1) • PCNA (Proliferating cell nuclear antigen) • IRAK1 (Interleukin 1 Receptor Associated Kinase 1) • TGFBR1 (Transforming Growth Factor Beta Receptor 1) • TRAF6 (TNF Receptor Associated Factor 6)
|
galunisertib (LY2157299)
3ms
Lingual Denervation Improves the Efficacy of Anti-PD-1 Immunotherapy in Oral Squamous Cell Carcinomas by Down-regulating TGFβ Signaling. (PubMed, Cancer Res Commun)
Neural involvement enhanced tumor aggressiveness through upregulating TGFβ signaling and PD-L1 expression in OSCC, while denervation of OSCC inhibited tumor growth, down-regulated TGFβ signaling, enhanced activities of CD8+ T cells and improved the efficacy of anti-PD-1 immunotherapy. This study will encourage further research focusing on denervation as a potential adjuvant therapeutic approach in OSCC.
Journal • PD(L)-1 Biomarker • IO biomarker
|
CD8 (cluster of differentiation 8) • IFNG (Interferon, gamma) • TNFA (Tumor Necrosis Factor-Alpha)
|
PD-L1 expression • IFNG expression
|
galunisertib (LY2157299)
4ms
Oral Probiotics Microgel Plus Galunisertib Reduced TGF-β Blockade Resistance and Enhanced Anti-tumor Immune Responses in Colorectal Cancer. (PubMed, Int J Pharm)
In this study, we developed an oral microgel delivery system of EcN@(CS-SA) by electrostatic interaction between chitosan (CS) and sodium alginate (SA), aiming to enhance its bioavailability in the gastrointestinal tract (GIT). Notably, EcN@(CS-SA) microgel showed a synergistic enhancement of the anti-tumor efficacy of Galunisertib (Gal, a TGF-β inhibitor) by inducing apoptosis and immunogenic cell death (ICD) in tumor cells, as well as promoting increased infiltration of CD8 T cells into the tumor microenvironment (TME).
Journal
|
CD8 (cluster of differentiation 8) • TGFB1 (Transforming Growth Factor Beta 1)
|
galunisertib (LY2157299)
4ms
Comparison of Post-Inflammatory Pigment Alteration After Psoriasis Treatment (PIPA - Dermavant) (clinicaltrials.gov)
P=N/A, N=40, Not yet recruiting, Wake Forest University Health Sciences | Initiation date: Dec 2023 --> Apr 2024 | Trial primary completion date: Jan 2024 --> Jun 2024
Trial initiation date • Trial primary completion date
4ms
Trial completion date • Metastases
|
HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor) • PGR (Progesterone receptor)
|
HER-2 negative • HER-2 expression • ER negative • PGR expression • PGR negative
|
Prosigna™ Breast Cancer Prognostic Gene Signature Assay
|
paclitaxel • galunisertib (LY2157299)
5ms
A Study in Recurrent Glioblastoma (GB) (clinicaltrials.gov)
P2, N=180, Active, not recruiting, Eli Lilly and Company | Trial completion date: Dec 2023 --> Sep 2024
Trial completion date
|
lomustine • galunisertib (LY2157299)
6ms
Trial completion • Metastases
|
HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor) • PGR (Progesterone receptor)
|
HER-2 negative • HER-2 expression • ER negative • PGR expression • PGR negative
|
Prosigna™ Breast Cancer Prognostic Gene Signature Assay
|
paclitaxel • galunisertib (LY2157299)
6ms
Efficacy and safety of abemaciclib alone and with PI3K/mTOR inhibitor LY3023414 or galunisertib versus chemotherapy in previously treated metastatic pancreatic adenocarcinoma: A randomized controlled trial. (PubMed, Cancer Med)
In patients with pretreated metastatic PDAC, abemaciclib-based therapy did not improve DCRs or PFS compared with SOC chemotherapy. No treatment arms advanced to Stage 2. Abemaciclib remains investigational in patients with PDAC.
Journal • Metastases
|
CDK4 (Cyclin-dependent kinase 4) • TGFB1 (Transforming Growth Factor Beta 1)
|
gemcitabine • capecitabine • Verzenio (abemaciclib) • samotolisib (LY3023414) • galunisertib (LY2157299)
6ms
Preclinical
|
TGFB1 (Transforming Growth Factor Beta 1) • APOB (Apolipoprotein B) • TGFBR1 (Transforming Growth Factor Beta Receptor 1)
|
galunisertib (LY2157299)
7ms
Cancer stemness kinase inhibitor amcasertib: a promising therapeutic agent in ovarian cancer stem and cancer cell models with different genetic profiles. (PubMed, Med Oncol)
Furthermore, the suppression of Nanog-mediated stem cell-like features by Amcasertib was particularly pronounced in ER-negative ovarian cancer and cancer stem cells, highlighting its high anticancer efficacy in this subgroup. These results suggest that Amcasertib holds promise as a potential standalone or combination therapy agent for the treatment of ER-negative ovarian cancer.
Journal
|
ER (Estrogen receptor) • NANOG (Nanog Homeobox)
|
ER negative
|
amcasertib (BBI-503)
7ms
Gastric cancer-derived LBP promotes liver metastasis by driving intrahepatic fibrotic pre-metastatic niche formation. (PubMed, J Exp Clin Cancer Res)
The results of this study provide compelling evidence that serological LBP can serve as a valuable diagnostic biomarker for the early detection of GC-LM. Mechanistically, GC-derived LBP mediates the crosstalk between primary GC cells and the intrahepatic microenvironment by promoting TGF-β1 secretion in intrahepatic macrophages, which induces intrahepatic fibrotic PMN formation to promote GC-LM. Importantly, selectively targeting the TGF-β/Smad signaling pathway with galunisertib represents a promising preventive and therapeutic strategy for GC-LM.
Journal • Metastases
|
TGFB1 (Transforming Growth Factor Beta 1)
|
galunisertib (LY2157299)
8ms
Autotaxin secretion is a stromal mechanism of adaptive resistance to TGFβ inhibition in pancreatic ductal adenocarcinoma. (PubMed, Cancer Res)
The autotaxin inhibitor IOA-289 suppressed NF-κB activation in PDAC cells and overcame resistance to galunisertib and gemcitabine. Most importantly, treatment with galunisertib significantly increased plasma levels of autotaxin in patients enrolled in the H9H-MC-JBAJ study, and median progression free survival was significantly longer in patients without an increase of autotaxin upon treatment with galunisertib compared to those with increased autotaxin. These results establish that autotaxin secretion by CAFs is increased by TGFβ inhibition and that circulating autotaxin levels predict response to the combination treatment approach of gemcitabine plus galunisertib.
Journal • Stroma
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TGFB1 (Transforming Growth Factor Beta 1)
|
gemcitabine • galunisertib (LY2157299) • cambritaxestat (IOA-289)
8ms
SIK1 suppresses colorectal cancer metastasis and chemoresistance via the TGF-β signaling pathway. (PubMed, J Cancer)
Our results suggest that the inhibitory effect of SIK1 on the TGF-β pathway contributes to the suppression of metastasis and oxaliplatin chemoresistance in CRC. However, this effect was reversed by galunisertib (LY2157299). In conclusion, our findings provide novel insights into the role of SIK1 in the regulation of the TGF-β pathway in CRC, suggesting its potential as a therapeutic target for the treatment of CRC. Further studies are required to fully characterize the mechanism underlying these observations and to validate these findings in animal models.
Journal
|
TGFB1 (Transforming Growth Factor Beta 1) • SMAD7 (SMAD Family Member 7) • SIK1 (Salt Inducible Kinase 1)
|
oxaliplatin • galunisertib (LY2157299)
9ms
A phase Ib/II study of galunisertib in combination with nivolumab in solid tumors and non-small cell lung cancer. (PubMed, BMC Cancer)
The study met its primary endpoint as galunisertib combined with nivolumab was well tolerated. Preliminary efficacy was observed in a subset of patients in the Phase 2 NSCLC cohort.
P1/2 data • Clinical Trial,Phase II • Journal • Combination therapy • PD(L)-1 Biomarker • IO biomarker
|
IFNG (Interferon, gamma)
|
PD-L1 expression • PD-L1 overexpression
|
Opdivo (nivolumab) • galunisertib (LY2157299)
10ms
WFDC3 inhibits tumor metastasis by promoting the ERβ-mediated transcriptional repression of TGFBR1 in colorectal cancer. (PubMed, Cell Death Dis)
Blocking TGFβ signaling with galunisertib, a drug used in clinical trials that targets TGFBR1, impaired the migration of CRC cells induced by WFDC3 depletion. Moreover, there was clinical significance to WFDC3 in CRC, as CRC patients with high WFDC3 expression in tumor cells had favorable prognoses. Therefore, this work suggests that WFDC3 could be an indicator for therapies targeting the estrogen/ERβ pathway in CRC patients.
Journal
|
ER (Estrogen receptor) • TGFBR1 (Transforming Growth Factor Beta Receptor 1)
|
galunisertib (LY2157299)
10ms
Transcriptomic evidence for tumor-specific beneficial or adverse effects of TGFβ pathway inhibition on the prognosis of patients with liver cancer. (PubMed, FEBS Open Bio)
More importantly, integrative transcriptomics using independent cohorts of patients with HCC demonstrates that galunisertib-induced transcriptional reprogramming in SNU-449 is associated with human HCC with a better clinical outcome (i.e. increased overall survival), while galunisertib-induced transcriptional reprogramming in PLC/PRF/5 is associated with human HCC with a worse clinical outcome (i.e. reduced overall survival), demonstrating that galunisertib could indeed be beneficial or detrimental depending on HCC subtypes. Collectively, our study highlights the importance of patient selection to demonstrate a clinical benefit of TGFβ pathway inhibition and identifies Serpin Family F Member 2 (SERPINF2) as a putative companion biomarker for galunisertib in HCC.
Journal • Adverse events
|
TGFB1 (Transforming Growth Factor Beta 1) • SERPINF2 (Serpin Family F Member 2)
|
galunisertib (LY2157299)
11ms
ING5 overexpression upregulates miR-34c-5p/Snail1 to inhibit EMT and invasion of lung cancer cells. (PubMed, Acta Biochim Biophys Sin (Shanghai))
The TGF-β signaling-specific inhibitor LY2157299 reverses the enhanced EMT, proliferation, migration, and invasion abilities induced by the miR-34c-5p inhibitor...Overall, this study concludes that miR-34c-5p, induced by ING5 overexpression, is a tumor suppressor that targets Snail1 and mediates the inhibitory effects of ING5 on the EMT and invasion of NSCLC cells. These results provide a novel mechanism mediating the antitumor effects of ING5.
Journal
|
TGFB1 (Transforming Growth Factor Beta 1) • SNAI1 (Snail Family Transcriptional Repressor 1) • SMAD3 (SMAD Family Member 3)
|
galunisertib (LY2157299)
11ms
A Dose-Escalation Study in Participants With Recurrent Malignant Glioma (clinicaltrials.gov)
P1, N=66, Active, not recruiting, Eli Lilly and Company | Trial completion date: Dec 2023 --> Sep 2024
Trial completion date • Combination therapy
|
lomustine • galunisertib (LY2157299)
11ms
NOX4 is a better candidate than TGF-beta receptor I to target the TGF-beta signalling in the tumour microenvironment and halt cholangiocarcinoma progression (EACR 2023)
A panel of 8 murine and human CCA cell lines and human hepatic stellate cells (HSC) and CAF were cultured in 2D or 3D to analyse response to TGF-β, TGF-beta receptor I inhibitor galunisertib and dual NOX1/NOX4 inhibitor GKT137831. GKT137831 inhibited fibroblast activation and reduced the size of CCA-fibroblast mixed spheroids.ConclusionDue to the strong suppressor effect of TGF-beta on the CCA tumour cell, inhibitors of the TGF-beta pathway as anti-cancer therapies may lead to counterproductive effects. Targeting the tumour microenvironment by inhibiting downstream mediators of the TGF-beta pathway, such as NOX4, may represent a therapeutic opportunity for CCA.This study is funded by Spanish Association for Cancer Research (AECC) #PRYGN211279FABR.
IO biomarker
|
TGFB1 (Transforming Growth Factor Beta 1) • NOX4 (NADPH Oxidase 4) • SMAD7 (SMAD Family Member 7) • SMAD3 (SMAD Family Member 3) • TGFBR1 (Transforming Growth Factor Beta Receptor 1)
|
galunisertib (LY2157299) • setanaxib (GKT831)
11ms
Study of TGF-β Receptor Inhibitor Galunisertib (LY2157299) and Enzalutamide in Metastatic Castration-resistant Prostate Cancer (clinicaltrials.gov)
P2, N=60, Recruiting, Sidney Kimmel Comprehensive Cancer Center at Johns Hopkins | Trial completion date: Dec 2023 --> Dec 2025 | Trial primary completion date: Jun 2023 --> Jun 2024
Trial completion date • Trial primary completion date • Metastases
|
Xtandi (enzalutamide capsule) • galunisertib (LY2157299)
12ms
Multifunctional nanodrug performs sonodynamic therapy and inhibits TGF-β to boost immune response against colorectal cancer and liver metastasis. (PubMed, Acta Biomater)
Herein, we prepared a nanodrug (NCG) encapsulating the transforming growth factor-β receptor inhibitor galunisertib (Gal) and the sonosensitizer chlorin e6 (Ce6), which was aimed to turn this type of cold tumor into a hot one to promote the ICB-based immunotherapy against it...Here, we reported a TGF-β-targeted inhibitory nanodrug that improved SDT in colon cancer and liver metastasis, reversed the immunosuppressive tumor microenvironment and boosted the immune response to anti-PD-L1 therapy in this cancer. It demonstrated the potential to cure this prevalent but incurable malignancy.
Journal
|
HMGB1 (High Mobility Group Box 1) • TGFB1 (Transforming Growth Factor Beta 1) • CALR (Calreticulin)
|
galunisertib (LY2157299)
12ms
Trial completion date • Metastases
|
HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor) • PGR (Progesterone receptor)
|
HER-2 negative • HER-2 expression • ER negative • PGR expression • PGR negative
|
Prosigna™ Breast Cancer Prognostic Gene Signature Assay
|
paclitaxel • galunisertib (LY2157299)
1year
Galunisertib combined with capecitabine in bowel cancer with peritoneal metastases Galunisertib in combinatie met capecitabine bij naar het buikvlies uitgezaaide darmkanker (clinicaltrialsregister.eu)
P1/2, N=35, Ongoing, Department of Medical Oncology and Clinical Pharmacology, The Netherlands Cancer Institute - Antoni van Leeuwenhoek Hosp
New P1/2 trial • Metastases
|
TGFB1 (Transforming Growth Factor Beta 1)
|
capecitabine • galunisertib (LY2157299)
1year
TGF-β blocking combined with photothermal therapy promote tumor targeted migration and long-term antitumor activity of CAR-T cells. (PubMed, Mater Today Bio)
To targeted block TGF-β at tumor site, we take advantages of nano-techniques to deliver TGF-β inhibitors LY2157299 (LY) towards the tumor sites, in order to help achieve a improved and long-term functions of CAR-T towards lymphoma...Combined therapy of LY/ICG@HES-PCL and CAR-T achieved 2.4 times higher antitumor activity and 2.7 times higher relapse inhibiting rates than CAR-T alone within 15 days and 11 days, respectively. The results suggested that LY/ICG@HES-PCL facilitated the enhanced therapeutic index of CAR-T cells towards lymphoma simply and safely, it may be further potentiated applied for other solid tumors.
Journal • CAR T-Cell Therapy
|
CXCL9 (Chemokine (C-X-C motif) ligand 9) • TGFB1 (Transforming Growth Factor Beta 1) • CXCR3 (C-X-C Motif Chemokine Receptor 3)
|
galunisertib (LY2157299)
over1year
ExIST Study of LY2157299 (Galunisertib) in Rectal Cancer (clinicaltrials.gov)
P2, N=50, Active, not recruiting, Providence Health & Services | Trial completion date: Dec 2022 --> Dec 2025 | Trial primary completion date: Sep 2022 --> Dec 2025
Trial completion date • Trial primary completion date • Metastases
|
CRP (C-reactive protein)
|
capecitabine • galunisertib (LY2157299) • fluorouracil topical
over1year
Therapeutic Effect of Polymeric Nanomicelles Formulation of LY2157299-Galunisertib on CCl-Induced Liver Fibrosis in Rats. (PubMed, J Pers Med)
Indeed, the encapsulated drug reduces collagen deposition, hepatic stellate cells (HSCs) activation, prevents fatty degeneration and restores the correct lobular architecture of the liver as well as normalizes the serum parameters and expression of the genes involved in the onset of HF. In summary, GLY-NM improved the pharmacological activity of the free TGF- β1 inhibitor in the in vivo HF treatment and thus is a candidate as a novel therapeutic strategy.
Preclinical • Journal
|
TGFB1 (Transforming Growth Factor Beta 1)
|
galunisertib (LY2157299)
over1year
Enhancement of the antitumor effect of 5-fluorouracil with modulation in drug transporters expression using PI3K inhibitors in colorectal cancer cells. (PubMed, Life Sci)
Our data provide evidence that survival signaling pathways represent distinctive targets for the enhancement of chemotherapeutic sensitivity. The antitumor efficacy of 5-FU is enhanced when combined with a PI3K inhibitor, and this effect was mediated by alterations in the expression of specific drug transporters.
Journal
|
ABCG2 (ATP Binding Cassette Subfamily G Member 2) • ABCC5 (ATP Binding Cassette Subfamily C Member 5)
|
ABCG2 expression
|
5-fluorouracil • LY294002 • PI-103
over1year
Galunisertib synergistically potentiates the doxorubicin-mediated antitumor effect and kickstarts the immune system against aggressive lymphoma. (PubMed, Int Immunopharmacol)
Based on the tumor-draining lymph node analysis, combination therapy results in better prognosis, including disappearance of disease-exacerbating regulatory T cells and prevention of CD8 T-cell exhaustion by downregulating MDSCs. Galunisertib synergistically potentiates the doxorubicin-mediated antitumor effect without aggravating the toxic effects and the ability to kickstart the immune system, supporting the clinical relevance of targeting TGF-βRI in combination with doxorubicin against lymphoma.
Journal
|
CD8 (cluster of differentiation 8) • TGFB1 (Transforming Growth Factor Beta 1)
|
doxorubicin hydrochloride • galunisertib (LY2157299)
over1year
An autophagy-related gene prognostic index predicting biochemical recurrence, metastasis, and drug resistance for prostate cancer. (PubMed, Asian J Androl)
Drug analysis showed that PI-103 was the common sensitive drug and cell line analysis indicated that PC3 was the common cell line of PI-103 and the definitive gene. In conclusion, we found that ARGPI could predict BCR, metastasis, and chemoresistance in PCa patients who underwent radical radiotherapy or prostatectomy.
Journal
|
SPP1 (Secreted Phosphoprotein 1) • ALDH2 (Aldehyde Dehydrogenase 2 Family Member) • ACSL3 (Acyl-CoA Synthetase Long Chain Family Member 3)
|
PI-103
over1year
A pyridinesulfonamide derivative FD268 suppresses cell proliferation and induces apoptosis via inhibiting PI3K pathway in acute myeloid leukemia. (PubMed, PLoS One)
In this study, we demonstrated that FD268 dose-dependently inhibits survival of AML cells with the efficacy superior to that of PI-103 (pan-PI3K inhibitor) and CAL-101 (selective PI3Kδ inhibitor) in the tested HL-60, MOLM-16, Mv-4-11, EOL-1 and KG-1 cell lines. The bioinformatics analysis of the transcriptome sequencing data also indicated a potential involvement of the PI3K/Akt/mTOR pathway. These studies indicated that FD268 possesses high potent activity toward AML cells via inhibition of PI3K/Akt/mTOR signaling pathway, which sheds some light on the pyridinesulfonamide scaffold for further optimization and investigation.
Journal
|
MCL1 (Myeloid cell leukemia 1) • PIK3CD (Phosphatidylinositol-4 5-Bisphosphate 3-Kinase Catalytic Subunit Delta) • CASP3 (Caspase 3)
|
MCL1 expression
|
Zydelig (idelalisib) • PI-103
over1year
Gold Nanoparticles Disrupt the IGFBP2/mTOR/PTEN Axis to Inhibit Ovarian Cancer Growth. (PubMed, Adv Sci (Weinh))
This mechanism is validated by treating a cell line-based human xenograft tumor with GNPs and an mTOR dual-kinase inhibitor (PI-103), either individually or in combination with GNPs; GNP and PI-103 combination therapy inhibit ovarian tumor growth similarly to GNPs alone. This report illustrates how the self-therapeutic properties of GNPs can be exploited as a discovery tool to identify a critical signaling axis responsible for poor prognosis in ovarian cancer and provides an opportunity to interrogate the axis to improve patient outcomes.
Journal
|
IGFBP2 (Insulin-like growth factor binding protein 2)
|
PI-103
over1year
Cyclin-dependent kinase subunit2 (CKS2) promotes malignant phenotypes and epithelial-mesenchymal transition-like process in glioma by activating TGFβ/SMAD signaling. (PubMed, Cancer Med)
We identified CKS2 as a critical contributor to the gliomagenesis, which might provide a novel therapeutic target for inhibiting the spread and infiltration of glioma.
Journal
|
SMAD4 (SMAD family member 4) • CKS2 (CDC28 Protein Kinase Regulatory Subunit 2) • SMAD2 (SMAD Family Member 2)
|
galunisertib (LY2157299)
over1year
Mitochondrial Aldehyde Dehydrogenase 2 Represents a Potential Biomarker of Biochemical Recurrence in Prostate Cancer Patients. (PubMed, Molecules)
We found that ALDH2 might serve as a potential biomarker predicting biochemical recurrence for PCa patients.
Journal
|
CD8 (cluster of differentiation 8) • ALDH2 (Aldehyde Dehydrogenase 2 Family Member) • NRP1 (Neuropilin 1) • CD96 (CD96 Molecule)
|
PI-103 • PHA 793887
over1year
Novel targets to overcome antiangiogenesis therapy resistance in glioblastoma multiforme: Systems biology approach and suggestion of therapy by galunisertib. (PubMed, Cell Biol Int)
In silico analysis indicated that NRAS, AKT1, and HSPB1 genes can be the main oncogenes in the VEGF signaling pathway and galunisertib strongly interacts with these genes. Consequently, the use of galunisertib to overcome AAT in GBM in combination therapy can be assessed.
Journal
|
NRAS (Neuroblastoma RAS viral oncogene homolog) • AKT1 (V-akt murine thymoma viral oncogene homolog 1) • HSPB1 (Heat shock 27kDa protein 1)
|
VEGFA expression • HSPB1 expression
|
galunisertib (LY2157299)