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- | doxorubicin hydrochloride / Generic mfg.
Journal: CRISPRi/a screens in human iPSC-cardiomyocytes identify glycolytic activation as a druggable target for doxorubicin-induced cardiotoxicity. (Pubmed Central) - Nov 15, 2024
Mechanistically, doxorubicin-induced CA12 potentiated a glycolytic activation in cardiomyocytes, contributing to DIC by interfering with cellular metabolism and functions. Collectively, our study provides a roadmap for future drug discovery efforts, potentially leading to more targeted therapies with minimal off-target toxicity.
- | doxorubicin hydrochloride / Generic mfg.
Journal: Dual Inhibitors of P-gp and Carbonic Anhydrase XII (hCA XII) against Tumor Multidrug Resistance with Piperazine Scaffold. (Pubmed Central) - Jul 31, 2024
In particular, compound 33 displayed the best activity by enhancing the cytotoxicity and intracellular accumulation of doxorubicin in HT29/DOX and A549/DOX cells, thus resulting as promising P-gp-mediated MDR reverser with a synergistic mechanism. Furthermore, compounds 13, 27 and 32 induced collateral sensitivity (CS) in MDR cells, as they were more cytotoxic in resistant cells than in the sensitive ones; their CS mechanisms were extensively investigated.
- | Journal: Network Pharmacology Along with Molecular Docking to Explore the Mechanism of Danshen Injection against Anthracycline-induced Cardiotoxicity and Transcriptome Validation. (Pubmed Central) - Mar 14, 2024
The present study suggested that DSI might exert a cardioprotective effect on AIC via the inhibition of CA12, NOS3, and POLH, as well as the modulation of calcium signaling. Further experiments are warranted to verify the findings.
- | Journal: Estrogen-Induced LncRNA, LINC02568, Promotes Estrogen Receptor-Positive Breast Cancer Development and Drug Resistance Through Both In Trans and In Cis Mechanisms. (Pubmed Central) - Sep 7, 2023
Taken together, the findings reveal the dual mechanisms of LINC02568 in regulating ER? signaling and pH homeostasis in ER-positive breast cancer, and indicated that targeting LINC02568 might represent a potential therapeutic avenue in the clinic.
- | Journal: Trafficking of carbonic anhydrase 12 and bicarbonate transporters by histamine stimulation mediates intracellular acidic scenario in lung cancer cells. (Pubmed Central) - Aug 21, 2023
Inhibition of protein trafficking by bafilomycin restored CA12 and AE2 localisation and diminished cellular acidosis. Thus, we verified that histamine stimulation induced an acidic scenario, which revealed trafficking of CA12 and its associated bicarbonate transporters in lung cancer cells and its dysregulated pH modulation may be involved in the histamine signalling-mediated anti-cancer process.
- | Journal: Tiliroside suppresses triple-negative breast cancer as a multifunctional CAXII inhibitor. (Pubmed Central) - Nov 25, 2022
Further RT-PCR and Caspase-3 activity analyses also revealed the positive regulating effects of TS on E2F1,3/Caspase-3 axis in TNBC cells cultured in 2D or 3D systems. The findings indicate that TS suppresses TNBC progression as a potential novel CAXII inhibitor in preclinical experiments, which warrants further investigation on its therapeutic implications.
- | Journal: Novel benzenesulfonamide-thiouracil conjugates with a flexible N-ethyl acetamide linker as selective CA IX and CA XII inhibitors. (Pubmed Central) - Nov 15, 2022
Molecular docking simulations showed that the synthesized conjugates adopted comparable binding modes in the CA I, CA II, CA IX, and CA XII isoforms, involving the deep fitting of the sulfonamide moiety in the base of the CA active site via chelation of the Zn ion and H-bond interaction with the key amino acids Thr199 and/or Thr200. Moreover, the N-ethyl acetamide flexible linker enables the substituted thiouracils and fused thiouracil tail to achieve multiple interactions with the surrounding hydrophobic and hydrophilic regions.
- | Journal: Role of the Hedgehog Pathway and CAXII in Controlling Melanoma Cell Migration and Invasion in Hypoxia. (Pubmed Central) - Oct 15, 2022
Moreover, the N-ethyl acetamide flexible linker enables the substituted thiouracils and fused thiouracil tail to achieve multiple interactions with the surrounding hydrophobic and hydrophilic regions. Our results suggest that CAXII and the Hh pathway are relevant in melanoma invasion and may be novel and promising therapeutical targets for melanoma clinical management.
- | Journal, PD(L)-1 Biomarker, IO biomarker: The construction of a hypoxia-based signature identified CA12 as a risk gene affecting uveal melanoma cell malignant phenotypes and immune checkpoint expression. (Pubmed Central) - Oct 14, 2022
These results validate the prognostic role of the hypoxia signature in UM and demonstrate that CA12 is a critical factor for UM cell progression as well as a target to improve immunotherapeutic effects. We believe our study contributes to the understanding of hypoxia's roles in UM and provides a novel target that will benefit future therapeutic strategy development.
- | doxorubicin hydrochloride / Generic mfg., docetaxel / Generic mfg.
Journal: Correlation between CA12 and TFF3 and their prediction value of neoadjuvant chemotherapy response in breast cancer. (Pubmed Central) - May 25, 2022
We believe our study contributes to the understanding of hypoxia's roles in UM and provides a novel target that will benefit future therapeutic strategy development. CA12 and TFF3 were correlated with each other, and their high expression might explain the worse efficacy of neoadjuvant chemotherapy in oestrogen receptor-positive breast cancer patients.
- || Review, Journal, Combination therapy: Carbonic anhydrase XII inhibition overcomes P-glycoprotein-mediated drug resistance: a potential new combination therapy in cancer. (Pubmed Central) - May 19, 2022
This review covers the use of CA XII inhibitors, both small molecule and antibody, in combination with chemotherapeutics that are substrates for Pgp. This combination therapy approach restores the efficacy of chemotherapy in resistant cells and offers a potential new therapeutic window to re-examine the targeting of Pgp as a safe, effective, and novel anticancer strategy.
- ||||| Combination therapy: Article Sharing 🌿Carbonic anhydrase XII inhibition overcomes P-glycoprotein-mediated drug resistance: a potential new combination therapy in cancer🫒 https://t.co/6IvR9596il @Thomas_Hayman @lab_gomes @StraussmanR @BivonaLabUCSF @andyjminn (Twitter) - May 10, 2022
- | SLC-0111 / SignalChem Lifesci, Welichem
Preclinical, Journal: Perfusion-Based Bioreactor Culture and Isothermal Microcalorimetry for Preclinical Drug Testing with the Carbonic Anhydrase Inhibitor SLC-0111 in Patient-Derived Neuroblastoma. (Pubmed Central) - Apr 9, 2022
The system was successfully used for consecutive drug response monitoring with isothermal microcalorimetry. The described approach for drug testing, relying on an advanced 3D culture system combined with a rapid and highly sensitive metabolic assessment, can facilitate development of personalized treatment strategies for neuroblastoma.
- | Journal, IO biomarker: Carbonic anhydrase XII mediates the survival and prometastatic functions of macrophages in human hepatocellular carcinoma. (Pubmed Central) - Apr 8, 2022
Selective targeting of tumor-infiltrating macrophages with a CA12 inhibitor reduced tumor growth in mice and was sufficient to synergistically enhance the therapeutic efficacy of immune-checkpoint blockade. We suggest that CA12 activity is a previously unappreciated mechanism regulating the accumulation and functions of macrophages in tumor microenvironments and therefore represents a selective vulnerability that could be exploited in future designs for antitumor immunotherapeutic strategies.
- | Journal, PD(L)-1 Biomarker, IO biomarker: An acid trip activates protumoral macrophages to promote hepatocellular carcinoma malignancy. (Pubmed Central) - Apr 8, 2022
Notably, dual treatment with anti-PD1 and CA12 inhibitors synergistically attenuated tumor growth and metastasis and enhanced survival compared with either treatment alone. These findings suggest that targeting CA12 in combination with immune-checkpoint blockade may provide treatment options for HCC.