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DRUG:

R-(-)-gossypol (AT 101)

i
Other names: AT 101, AT-101, R-(-)-gossypol acetic acid, (-)-gossypol
Company:
Ascentage Pharma
Drug class:
Bcl2 inhibitor, Bcl-xL inhibitor, MCL1 inhibitor
Related drugs:
19d
Metabolomic Profiling and Network Toxicology: Mechanistic Insights into Effect of Gossypol Acetate Isomers in Uterine Fibroids and Liver Injury. (PubMed, Pharmaceuticals (Basel))
(-)-gossypol acetate and (+)-gossypol acetate play positive roles in the treatment and prevention of uterine fibroids. Gossypol optical isomers cause liver damage through multiple targets and pathways.
Journal • Metabolomic study
|
EGFR (Epidermal growth factor receptor) • BCL2 (B-cell CLL/lymphoma 2) • AKT1 (V-akt murine thymoma viral oncogene homolog 1) • MAPK1 (Mitogen-activated protein kinase 1) • CASP3 (Caspase 3) • HSP90AA1 (Heat Shock Protein 90 Alpha Family Class A Member 1Heat Shock Protein 90 Alpha Family Class A Member 1)
|
R-(-)-gossypol (AT 101)
2ms
Structural basis of lactate dehydrogenase A-gossypol complex. (PubMed, Biochem Biophys Res Commun)
The binding of gossypol affects LDHA activity by a conformational change in the active-site loop. Our research contributes to the structural insight into LDHA with gossypol and approaches gossypol as a novel therapeutic candidate targeting the metabolic pathways for cancer cells.
Journal
|
LDHA (Lactate dehydrogenase A)
|
R-(-)-gossypol (AT 101)
2ms
Highly Efficient Synergistic Chemotherapy and Magnetic Resonance Imaging for Targeted Ovarian Cancer Therapy Using Hyaluronic Acid-Coated Coordination Polymer Nanoparticles. (PubMed, Adv Sci (Weinh))
RNA sequencing analysis reveals that HA@PFG NPs ameliorate OC symptoms mainly through IL-6 signal pathways. This work combines MRI imaging with cisplatin-based chemotherapy, which holds great promise for OC diagnosis and synergistic therapy.
Journal • MRI
|
IL6 (Interleukin 6)
|
cisplatin • R-(-)-gossypol (AT 101)
2ms
Gossypol Inhibits Metastasis of Lung Cell Carcinoma by Reversing Epithelial to Mesenchymal Transition and Suppressing Proteases Activity. (PubMed, Environ Toxicol)
Gossypol reduced vimentin, p-FAK, p-Src and p-paxillin. In vivo studies of gossypol were performed using subcutaneous inoculation and tail vein injection of A549 into immunodeficient BALB/c nude mice and severe combined immunodeficient mice.
Journal
|
MMP2 (Matrix metallopeptidase 2) • VIM (Vimentin) • TGFB1 (Transforming Growth Factor Beta 1)
|
R-(-)-gossypol (AT 101)
4ms
Blockade of CaV3 calcium channels and induction of G0/G1 cell cycle arrest in colon cancer cells by gossypol. (PubMed, Br J Pharmacol)
Gossypol differentially blocked CaV3 channel and its anticancer activity was correlated with high levels of CaV3.1 and CaV3.2 in colorectal cancer cells. The CaV3 regulates cell proliferation and Ca2+ dynamics in colorectal cancer cells. Understanding this blocking mechanism maybe improve cancer therapies.
Journal
|
CAV3 (Caveolin 3)
|
R-(-)-gossypol (AT 101)
5ms
Computational analysis of ligands from natural products on the cellular targets of combined hepatocellular carcinoma and cholangiocarcinoma. (PubMed, Nat Prod Res)
Interestingly, all these phytoconstituents had drug likeliness and ADMET properties similar to the anti-cancer drug, irinotecan...FGFR3, VEGFR3, and PDGFRB, respectively. The order of gossypol, berberine and parthenolide was determined as effective, whereas, the order of berberine, parthenolide and gossypol was found safer for human use.
Journal
|
FGFR2 (Fibroblast growth factor receptor 2) • FGFR3 (Fibroblast growth factor receptor 3) • FGFR1 (Fibroblast growth factor receptor 1) • PDGFRA (Platelet Derived Growth Factor Receptor Alpha) • KDR (Kinase insert domain receptor) • PDGFRB (Platelet Derived Growth Factor Receptor Beta) • FLT1 (Fms-related tyrosine kinase 1) • FLT4 (Fms-related tyrosine kinase 4)
|
irinotecan • R-(-)-gossypol (AT 101)
7ms
Targeting leucine-rich PPR motif-containing protein/LRPPRC by 5,7,4'-trimethoxyflavone suppresses esophageal squamous cell carcinoma progression. (PubMed, Int J Biol Macromol)
Furthermore, 5,7,4'-trimethoxyflavone was verified to bind to LRPPRC, STAT3, and CDK1, dissociating LRPPRC-JAK2-STAT3 and JAK2-STAT3-CDK1 interaction, leading to impaired tumorigenesis in 4-Nitroquinoline N-oxide induced ESCC mouse models and suppressed tumor growth in ESCC patient derived xenograft mouse models. In summary, this study suggests regulation of m6A modification by LRPPRC, and identifies a novel triplex target compound, suggesting that targeting LRPPRC-mediated JAK2/STAT3/MYC axis may overcome JAK2/STAT3/MYC dependent tumor therapeutic dilemma.
Journal
|
JAK2 (Janus kinase 2) • STAT3 (Signal Transducer And Activator Of Transcription 3) • CDK1 (Cyclin-dependent kinase 1) • LRPPRC (Leucine Rich Pentatricopeptide Repeat Containing)
|
Piqray (alpelisib) • Jakafi (ruxolitinib) • Truqap (capivasertib) • R-(-)-gossypol (AT 101)
7ms
Gossypol acetic acid regulates leukemia stem cells by degrading LRPPRC via inhibiting IL-6/JAK1/STAT3 signaling or resulting mitochondrial dysfunction. (PubMed, World J Stem Cells)
Taken together, the results indicate that GAA might overcome the BMM protective effect and be considered as a novel and effective combination therapy for AML.
Journal • IO biomarker
|
BCL2 (B-cell CLL/lymphoma 2) • IL6 (Interleukin 6) • CD38 (CD38 Molecule) • JAK1 (Janus Kinase 1) • CD34 (CD34 molecule) • FOXM1 (Forkhead Box M1) • LRPPRC (Leucine Rich Pentatricopeptide Repeat Containing)
|
cytarabine • R-(-)-gossypol (AT 101)
8ms
Molecular-Scale Investigations Reveal the Effect of Natural Polyphenols on BAX/Bcl-2 Interactions. (PubMed, Int J Mol Sci)
Combined with surface free energy and molecular docking, the results revealed that polyphenols are driven by multiple forces that affect the orientation freedom of PPIs, with hydrogen bonding, hydrophobic interactions, and van der Waals forces being the major contributors. Overall, our work provides valuable insights into how molecules tune PPIs to modulate their function.
Journal
|
BCL2 (B-cell CLL/lymphoma 2) • BAX (BCL2-associated X protein)
|
R-(-)-gossypol (AT 101)
10ms
Clinical trials of R-(-)-gossypol (AT-101) in newly diagnosed and recurrent glioblastoma: NABTT 0602 and NABTT 0702. (PubMed, PLoS One)
AT-101 can be safely administered with radiation therapy and TMZ in patients with newly diagnosed glioblastoma without toxicity unique to patients with CNS tumors. Because of toxicity observed in non-CNS AT-101 clinical trials, further dose-escalation was not attempted. The recommended dose for future studies that utilize continual AT-101 exposure is 20 mg days M-F concurrent with RT/TMZ and 20 mg days 1-21 for each 28-day cycle of TMZ. AT-101 has limited activity as a single agent in unselected patients with recurrent glioblastoma. Future trials should attempt to better understand resistance mechanisms and consider combination therapy.
Journal
|
BCL2 (B-cell CLL/lymphoma 2) • BCL2L1 (BCL2-like 1) • BCL2L2 (BCL2 Like 2)
|
temozolomide • R-(-)-gossypol (AT 101)
10ms
Journal
|
GPX4 (Glutathione Peroxidase 4) • SOX9 (SRY-Box Transcription Factor 9) • IL1B (Interleukin 1, beta) • ACAN (Aggrecan)
|
erastin • R-(-)-gossypol (AT 101)
11ms
NCI-2016-00073: Gossypol Acetic Acid With Lenalidomide and Dexamethasone in Treating Patients With Relapsed Symptomatic Multiple Myeloma (clinicaltrials.gov)
P1, N=10, Completed, Mayo Clinic | Active, not recruiting --> Completed | Phase classification: P1/2 --> P1 | Trial completion date: Dec 2024 --> Dec 2023
Trial completion • Phase classification • Trial completion date • Combination therapy • IO biomarker
|
BCL2 (B-cell CLL/lymphoma 2) • CRBN (Cereblon) • MAPK1 (Mitogen-activated protein kinase 1)
|
BCL2 expression • CRBN expression
|
lenalidomide • R-(-)-gossypol (AT 101)
11ms
The potential roles of gossypol as anticancer agent: advances and future directions. (PubMed, Chin Med)
However, further research is needed to refine gossypol-based therapies, explore combination treatments, and verify their effectiveness across cancer types. The ongoing clinical trials continue to support its potential, suggesting a future where gossypol could play a significant role in cancer treatment protocols.
Review • Journal
|
BCL2 (B-cell CLL/lymphoma 2)
|
R-(-)-gossypol (AT 101)
almost1year
New P2 trial • Metastases
|
CDK6 (Cyclin-dependent kinase 6) • LRPPRC (Leucine Rich Pentatricopeptide Repeat Containing)
|
fulvestrant • AiRuiKang (dalpiciclib) • R-(-)-gossypol (AT 101)
1year
In silico design and cell-based evaluation of two dual anti breast cancer compounds targeting Bcl-2 and GPER. (PubMed, Sci Rep)
Regarding histological classification of BC, the Estrogen (ER) and Progesterone (PR) receptors negative-expression cancer, named Triple-Negative BC (TNBC), represents the most aggressive type of this disease, making it a challenge for drug discovery...Strikingly, 37 assayed on MDA-MB-231 (a TNBC cell model) depicted an outstanding value of 18.66 μM much lower than 65.67 μM yielded by Gossypol Bcl-2 inhibitor whose main disadvantage is to produce multiple toxic effects. Highlighted above, enforce the premise of the computational tools to find new therapeutic options against the most aggressive forms of breast cancer, as the results herein showed.
Journal • IO biomarker
|
ER (Estrogen receptor) • BCL2 (B-cell CLL/lymphoma 2)
|
R-(-)-gossypol (AT 101)
1year
Gossypol enhances the efficacy of sorafenib by trigging autophagy and apoptosis in metastatic lung cancer cells: An upshot of Chou-Talalay combination index process. (PubMed, Toxicol In Vitro)
Additionally, the combination treatment exclusively targeted G/G phase cancer cells. In conclusion combination of gossypol and sorafenib shows synergistic increase in the cytotoxic effect by promoting autophagy and apoptosis.
Journal • Metastases
|
ATG5 (Autophagy Related 5)
|
sorafenib • R-(-)-gossypol (AT 101)
1year
Inhibition of human glutathione transferase by catechin and gossypol: comparative structural analysis by kinetic properties, molecular docking and their efficacy on the viability of human MCF-7 cells. (PubMed, J Biochem)
Combination therapy with tamoxifen resulted in cytotoxicity of 27.3% and 35.2% when combined with catechin and gossypol, respectively. Gossypol showed higher toxicity to MCF-7 cells, but its strong effects on normal cells raised concerns about selectivity and potential side effects.
Journal
|
GSTP1 (Glutathione S-transferase pi 1)
|
tamoxifen • R-(-)-gossypol (AT 101)
over1year
A traditional gynecological medicine inhibits ovarian cancer progression and eliminates cancer stem cells via the LRPPRC-OXPHOS axis. (PubMed, J Transl Med)
Our study identified a therapeutic target and provided a corresponding inhibitor for OXPHOS-based OC therapy. GAA inhibits OC progression by suppressing OXPHOS complex synthesis via targeting LRPPRC protein, supporting its potential utility as a natural therapeutic agent for ovarian cancer.
Journal • Cancer stem
|
LRPPRC (Leucine Rich Pentatricopeptide Repeat Containing)
|
R-(-)-gossypol (AT 101)
over1year
The RNA-binding protein LRPPRC promotes resistance to CDK4/6 inhibition in lung cancer. (PubMed, Nat Commun)
Gossypol acetate (GAA), a gynecological medicine that has been repurposed as a degrader of LRPPRC, enhances the CDK4/6i sensitivity in vitro and in vivo. Our study reveals a mechanism responsible for CDK4/6i resistance and provides an enlightening approach to investigating the combinations of CDK4/6 and LRPPRC inhibitors in cancer therapy.
Journal
|
CDK6 (Cyclin-dependent kinase 6) • E2F1 (E2F transcription factor 1)
|
CDK6 expression
|
R-(-)-gossypol (AT 101)
over1year
NCI-2016-00073: Gossypol Acetic Acid With Lenalidomide and Dexamethasone in Treating Patients With Relapsed Symptomatic Multiple Myeloma (clinicaltrials.gov)
P1/2, N=10, Active, not recruiting, Mayo Clinic | Phase classification: P1 --> P1/2 | Trial completion date: Jun 2023 --> Dec 2024
Phase classification • Trial completion date • Combination therapy
|
BCL2 (B-cell CLL/lymphoma 2)
|
lenalidomide • R-(-)-gossypol (AT 101)
over1year
Selection of qPCR reference gene for human colon cancer cells in cottonseed bioactive research (ACS-Fall 2023)
The qPCR results strongly support the conclusion that the Bcl2 gene is stably expressed at the mRNA level in the human colon cancer cells regardless of the treatment, suggesting that Bcl2 gene expression is not regulated at the mRNA level but at the post-transcriptional level. These results should facilitate studies designated to evaluate bioactivity on gene expression regulation by cottonseed molecules and other natural and synthetic molecules for nutrition and health uses.
IO biomarker
|
BCL2 (B-cell CLL/lymphoma 2) • GAPDH (Glyceraldehyde-3-Phosphate Dehydrogenase)
|
BCL2 expression
|
R-(-)-gossypol (AT 101)
over1year
Involvement of necroptosis in the selective toxicity of the natural compound (±) gossypol on squamous skin cancer cells in vitro. (PubMed, Arch Toxicol)
Gossypol treatment up to 96 h resulted in a selective cytotoxicity of SCL-1 cells (IC: 1.7 µM, 96 h) compared with normal keratinocytes (IC: ≥ 5.4 µM, 96 h) which is mediated by mitochondrial dysfunction and finally leading to necroptotic cell death. Taken together, gossypol shows a high potential as an alternative anticancer drug for the treatment of cutaneous squamous cell carcinoma.
Preclinical • Journal
|
R-(-)-gossypol (AT 101)
over1year
Sequential Treatment with Temozolomide Plus Naturally Derived AT101 as an Alternative Therapeutic Strategy: Insights into Chemoresistance Mechanisms of Surviving Glioblastoma Cells. (PubMed, Int J Mol Sci)
Interestingly, treatment with TMZ+AT101/AT101 concomitantly changed the amount and composition of extracellular vesicles released from surviving GBM cells. Taken together, our analyses revealed that even when chemotherapeutic agents with different effector mechanisms are combined, a variety of chemoresistance mechanisms of surviving GBM cells must be taken into account.
Journal
|
temozolomide • R-(-)-gossypol (AT 101)
over1year
Estrogen-dependent activation of NCOA3 couples with p300 and NF-κB to mediate antiapoptotic genes in ER-positive breast cancer cells. (PubMed, Discov Oncol)
Collectively, our results demonstrate an upstream signaling that activates four antiapoptotic genes in ER-positive breast cancer cells. Importantly, our results also imply that targeting NCOA3 or blocking the assembly of the NCOA3-p300-NF-κB complex may be promising therapeutic strategies for treating ER-positive breast cancer.
Journal • IO biomarker
|
ER (Estrogen receptor) • BCL2 (B-cell CLL/lymphoma 2) • MCL1 (Myeloid cell leukemia 1) • BCL2L1 (BCL2-like 1) • BCL2A1 (BCL2 Related Protein A1) • BCL2L2 (BCL2 Like 2) • NCOA3 (Nuclear Receptor Coactivator 3)
|
ER positive • BCL2L1 overexpression • MCL1 expression
|
R-(-)-gossypol (AT 101)
almost2years
Trial completion date • Combination therapy
|
BCL2 (B-cell CLL/lymphoma 2)
|
lenalidomide • R-(-)-gossypol (AT 101)
almost2years
Identification of Bcl2 as a Stably Expressed qPCR Reference Gene for Human Colon Cancer Cells Treated with Cottonseed-Derived Gossypol and Bioactive Extracts and Bacteria-Derived Lipopolysaccharides. (PubMed, Molecules)
The extensive qPCR results firmly support the conclusion that the Bcl2 gene is stably expressed at the mRNA level in the human colon cancer cells regardless of the treatment, suggesting that Bcl2 gene expression is not regulated at the mRNA level but at the post-transcriptional level. These results should facilitate studies designated to evaluate bioactivity on gene expression regulation by cottonseed molecules and other natural and synthetic molecules for nutrition and health uses.
Journal • IO biomarker
|
BCL2 (B-cell CLL/lymphoma 2) • GAPDH (Glyceraldehyde-3-Phosphate Dehydrogenase)
|
BCL2 expression
|
R-(-)-gossypol (AT 101)
2years
Hypericin, a potential new BH3 mimetic. (PubMed, Front Pharmacol)
In addition, interactions of Hyp, Goss and ABT263, with whole purified proteins Bcl-2 and Mcl-1 by fluorescence spectroscopy show that Hyp interacts stronger with the Bcl-2 and less with Mcl-1 protein than Goss or ABT-263...In combination therapy, low doses of Hyp with Goss effectively decreased U87 MG viability, suggesting a possible synergy effect. Overall, we can conclude that Hyp as BH3 mimetic acts primarily on Bcl-2 protein and can be explored to target cells with Bcl-2 over-expression, or in combination with other BH3 mimetics, that target Mcl-1 or Bcl-XL proteins, in dual therapy.
Journal • IO biomarker
|
BCL2 (B-cell CLL/lymphoma 2) • BCL2L1 (BCL2-like 1)
|
BCL2 overexpression • BCL2 expression • MCL1 expression
|
navitoclax (ABT 263) • R-(-)-gossypol (AT 101)
2years
Comparison of the efficacy of gossypol acetate enantiomers in rats with uterine leiomyoma. (PubMed, J Nat Med)
In contrast, (-)-GA and (+)-GA had certain effects on potassium ion concentration in serum, liver and kidney function, and the effects of (+)-GA on liver function were more obvious than (-)-GA. These findings will be of great significance to the drug development of gossypol optical isomers.
Preclinical • Journal
|
ER (Estrogen receptor) • PGR (Progesterone receptor)
|
ER expression
|
R-(-)-gossypol (AT 101)
2years
(-)-Gossypol enhances the anticancer activity of epirubicin via downregulating survivin in hepatocellular carcinoma. (PubMed, Chem Biol Interact)
HCC xenograft experiments in nude mice also showed that (-)-Gsp treatment acted synergistically with EPI to repress xenograft tumor growth. Overall, our proof-of-concept results may pave the way for novel strategies for the treatment of HCC based on the combination of EPI and (-)-Gsp.
Journal
|
BIRC5 (Baculoviral IAP repeat containing 5) • EIF4EBP1 (Eukaryotic translation initiation factor 4E binding protein 1) • MAPK4 (Mitogen-Activated Protein Kinase 4)
|
BIRC5 expression
|
epirubicin • R-(-)-gossypol (AT 101)
over2years
Apogossypolone Inhibits Cell Proliferation and Epithelial-Mesenchymal Transition in Cervical Cancer via Activating DKK3. (PubMed, Front Oncol)
In addition, ApoG2 treatment inhibited CC xenograft tumor growth and upregulated the protein levels of DKK3, cleaved caspase-3 and E-cadherin. In conclusions, these findings suggested that ApoG2 could effectively inhibit the growth and invasion of CC cells at least partly by activating DKK3.
Journal • IO biomarker
|
BCL2 (B-cell CLL/lymphoma 2) • CDH1 (Cadherin 1) • CASP3 (Caspase 3) • VIM (Vimentin) • CDH2 (Cadherin 2) • DKK3 (Dickkopf WNT Signaling Pathway Inhibitor 3)
|
DKK3 overexpression
|
R-(-)-gossypol (AT 101)
over2years
Trial completion date • Combination therapy
|
BCL2 (B-cell CLL/lymphoma 2)
|
lenalidomide • R-(-)-gossypol (AT 101)
over2years
Gossypol selectively induces necroptosis in squamous cell carcinoma cells (EACR 2022)
This suggests that GP qualitatively attacks mitochondria but is much more potent in tumor cells assuming that the metabolic state of the cells is an important target of GP. Conclusion The selective toxicity as well as the strong mitochondrial impact on SCL-1 at a concentration having no negative impact on NHEK indicate a possible therapeutic window for the treatment of cutaneous squamous cell carcinoma.
IO biomarker
|
BCL2 (B-cell CLL/lymphoma 2)
|
R-(-)-gossypol (AT 101)
over2years
A novel NRF2/ARE inhibitor gossypol induces cytotoxicity and sensitizes chemotherapy responses in chemo-refractory cancer cells. (PubMed, J Food Drug Anal)
In addition, we find that gossypol re-sensitizes topoisomerase II poison treatment in etoposide-resistant cancer cells via suppression of NRF2/ABCC1 axis. Moreover, gossypol suppresses NRF2-mediated G6PD expression thereby leads to induce synthetic lethality with cisplatin not only in parental cancer cells but also in cisplatin-resistant cancer cells. These findings suggest that gossypol is a novel NRF2/ARE inhibitor, and can be a potential adjuvant chemotherapeutic agent for treatment of chemo-refractory tumor.
Journal
|
ABCC1 (ATP Binding Cassette Subfamily C Member 1) • G6PD (Glucose-6-Phosphate Dehydrogenase)
|
cisplatin • etoposide IV • R-(-)-gossypol (AT 101)
over2years
Gossypol induces apoptosis of human pancreatic cancer cells via CHOP/endoplasmic reticulum stress signaling pathway. (PubMed, J Microbiol Biotechnol)
Taken together, our data suggest that gossypol may trigger apoptosis in pancreatic cancer cells via the PERK-CHOP signaling pathway. These findings propose a promising therapeutic approach to pancreatic cancer treatment using gossypol.
Journal
|
BCL2 (B-cell CLL/lymphoma 2) • BAX (BCL2-associated X protein) • CASP3 (Caspase 3) • ANXA5 (Annexin A5)
|
R-(-)-gossypol (AT 101)
over2years
Targeting the miR-34a/LRPPRC/MDR1 axis collapse the chemoresistance in P53 inactive colorectal cancer. (PubMed, Cell Death Differ)
Both in vivo and in vitro experiments revealed that combination chemotherapy with GAA and 5-fluorouracil (5FU) yielded improved treatment outcomes. In this study, we reported a novel mechanism and target related to P53-induced drug resistance and provided corresponding interventional strategies for the precision treatment of CRC.
Journal
|
ABCB1 (ATP Binding Cassette Subfamily B Member 1) • MIR34A (MicroRNA 34a-5p)
|
TP53 mutation • TP53 expression
|
5-fluorouracil • R-(-)-gossypol (AT 101)
over2years
Cottonseed extracts regulate gene expression in human colon cancer cells. (PubMed, Sci Rep)
The inhibitory effects of glandless kernel extract on gene expression may provide a useful opportunity for improving nutrition and healthcare associated with colon cancer. This in turn may provide the potential of increasing cottonseed value by using ethanol extract as a nutrition/health intervention agent.
Journal • IO biomarker
|
BCL2 (B-cell CLL/lymphoma 2)
|
R-(-)-gossypol (AT 101)
almost3years
The ponatinib/gossypol novel combination provides enhanced anticancer activity against murine solid Ehrlich carcinoma via triggering apoptosis and inhibiting proliferation/angiogenesis. (PubMed, Toxicol Appl Pharmacol)
Histopathology revealed a significant decline in neoplastic cells, the majority of which have necrotic changes and numerous apoptotic bodies, as well as a decrease in mitotic figures and tumor giant cells, indicating the capacity to suppress cancer proliferation/persistence. Overall, gossypol could be used as an adjuvant medication for ponatinib in cancer treatment, possibly leading to successful dose reductions and fewer side effects; however, further research is needed before a clinical application could be feasible.
Preclinical • Journal • IO biomarker
|
BCL2 (B-cell CLL/lymphoma 2) • FGFR4 (Fibroblast growth factor receptor 4) • BAX (BCL2-associated X protein) • CASP9 (Caspase 9)
|
Iclusig (ponatinib) • R-(-)-gossypol (AT 101)
almost3years
Chemotherapy AND Bcl-xL Inhibitor (AT-101) For Organ Preservation In Adults With Advanced Laryngeal Cancer (clinicaltrials.gov)
P2, N=55, Completed, University of Michigan Rogel Cancer Center | Active, not recruiting --> Completed
Trial completion
|
BCL2 (B-cell CLL/lymphoma 2)
|
cisplatin • carboplatin • docetaxel • R-(-)-gossypol (AT 101)
3years
Clinical • Trial completion date • Combination therapy
|
BCL2 (B-cell CLL/lymphoma 2)
|
lenalidomide • R-(-)-gossypol (AT 101)
over3years
Bioinformatics Analysis of the Signaling Pathways and Genes of Gossypol Induce Death of Nasopharyngeal Carcinoma Cells. (PubMed, DNA Cell Biol)
In addition, to further investigate the possible molecular mechanisms, we constructed a transcriptional regulatory network of TNFRSF10B containing 109 miRNAs and 47 TFs. Taken together, our results demonstrated that gossypol triggered antitumor effects against NPC cells, indicating its applicability for the management of NPC.
Journal
|
TNFRSF10B (TNF Receptor Superfamily Member 10b) • E2F1 (E2F transcription factor 1)
|
R-(-)-gossypol (AT 101)
over3years
Effects of the Anti-Tumorigenic Agent AT101 on Human Glioblastoma Cells in the Microenvironmental Glioma Stem Cell Niche. (PubMed, Int J Mol Sci)
The present study evaluates the effects of AT101, alone or in combination with temozolomide (TMZ), in a microenvironmental glioma stem cell niche model of two GBM cell lines (U251MG and U87MG). Further, the expression of CXCR7 and the interleukin-6 receptor was significantly regulated upon these stimulatory conditions. Since tumor stem-like cells are known to mediate the development of tumor recurrences and were observed to strongly respond to the AT101 treatment, this might represent a promising approach to prevent the development of GBM recurrences.
Journal
|
IL6R (Interleukin 6 receptor) • ACKR3 (Atypical Chemokine Receptor 3)
|
IL6 expression
|
temozolomide • R-(-)-gossypol (AT 101)
over3years
[VIRTUAL] Gossypol decreased cell viability and down-regulated the expression of a number of genes in human colon cancer cells (ACS-Sp 2021)
In particular, gossypol suppressed the expression of genes coding for mRNAs of CLAUDIN1, ELK1, FAS, GAPDH, IL2, IL8 and ZFAND5 mRNAs, but enhanced the expression of the gene coding for GLUT3 mRNA. The results showed that gossypol inhibited cell survival with decreased expression of a number of genes in the colon cancer cells.
IO biomarker
|
BCL2 (B-cell CLL/lymphoma 2) • CXCL8 (Chemokine (C-X-C motif) ligand 8) • IL2 (Interleukin 2) • GAPDH (Glyceraldehyde-3-Phosphate Dehydrogenase)
|
CXCL8 expression
|
R-(-)-gossypol (AT 101)