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    DRUG CLASS:

    Activin receptor inhibitor

    2ms
    Pancreatic Damage in Ovarian Cancer-Associated Cachexia Is Driven by Activin A Signalling. (PubMed, J Cachexia Sarcopenia Muscle)
    These findings demonstrate pancreatic damage occurs during CAC development and highlight the critical role of activin A in this process. Targeting activin A signalling may represent a promising therapeutic strategy to mitigate cachexia in cancer patients and preserve pancreatic function.
    Journal
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    PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha) • SMAD3 (SMAD Family Member 3) • ACVR2B (Activin A Receptor Type 2B)
    2ms
    Activin A protects against lipopolysaccharide/TNF-α induced damage of dopaminergic neurons both in vivo and in vitro by regulating mitochondrial fusion. (PubMed, Neuroscience)
    Additionally, mitochondrial fusion inhibitor (MFI8) increased the intracellular ROS levels, while Act A attenuated MFI8-mediated ROS elevation. In conclusion, our results suggest that Act A is involved in the onset and development of PD and may exert neuronal protective effects by regulating mitochondrial fusion.
    Preclinical • Journal
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    TNFA (Tumor Necrosis Factor-Alpha) • TGFB1 (Transforming Growth Factor Beta 1)
    6ms
    Activation of the MyD88-JNK pathway promotes pathogenetic Th17 differentiation by induction of activin-A secretion and enhances experimental autoimmune encephalomyelitis. (PubMed, Neuroreport)
    MyD88 signaling in T cells may be an attractive clinical target for anti-inflammatory therapies for diseases of the central nervous system.
    Journal
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    MYD88 (MYD88 Innate Immune Signal Transduction Adaptor) • IL17A (Interleukin 17A) • IL23A (Interleukin 23 Subunit Alpha) • IL1B (Interleukin 1, beta) • MAPK8 (Mitogen-activated protein kinase 8)
    7ms
    Sex-chromosome complement and Activin-A shape the therapeutic potential of TNFR2 activation in a model of MS and CNP. (PubMed, Proc Natl Acad Sci U S A)
    This suggests a shared mechanism through which gonadal-derived factors impact TNFR2-mediated pain relief, independent of sex hormones. These findings highlight the importance of considering sex chromosomes and sex-independent gonadal hormones in evaluating potential sex-specific differences in drug efficacy during therapeutic development.
    Journal
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    TNFA (Tumor Necrosis Factor-Alpha)
    8ms
    Activin A Antagonism with Follistatin Reduces Kidney Fibrosis, Injury, and Cellular Senescence-Associated Inflammation in Murine Diabetic Kidney Disease. (PubMed, Kidney360)
    Activin A is a mediator of kidney injury through macrophage-associated inflammation in murine DKD. Follistatin acts through senomorphic activities which inhibit profibrotic, proinflammatory, and pro-senescence signaling by activin A. Hence, anti-activin targeting may aid in development of a promising, novel therapeutic for DKD.
    Preclinical • Journal • IO biomarker
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    WT1 (WT1 Transcription Factor) • TLR4 (Toll Like Receptor 4)
    9ms
    Enhancing human NK cell antitumor function by knocking out SMAD4 to counteract TGFβ and activin A suppression. (PubMed, Nat Immunol)
    SMAD4KO conferred TGFβ resistance across diverse NK cell platforms, including CD19-CAR NK cells, stem cell-derived NK cells and ADAPT-NK cells. These findings position SMAD4 knockout as a versatile and compelling strategy to enhance NK cell antitumor activity, providing a new avenue for improving NK cell-based cancer immunotherapies.
    Journal
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    SMAD4 (SMAD family member 4) • IL2 (Interleukin 2) • TGFB1 (Transforming Growth Factor Beta 1) • IL15 (Interleukin 15)
    11ms
    Activin A receptor type 1C single nucleotide polymorphisms associated with esophageal squamous cell carcinoma risk in Chinese population. (PubMed, World J Gastrointest Oncol)
    ACVR1C rs4556933 and rs77886248 SNPs were associated with the susceptibility to ESCC, which could provide a potential target for early diagnosis and treatment of ESCC in Chinese Han population.
    Journal
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    ACVR1 (Activin A Receptor Type 1) • TGFB1 (Transforming Growth Factor Beta 1)
    11ms
    An Activin Receptor-Like Kinase 1-governed monocytic lineage shapes an immunosuppressive landscape in breast cancer metastases. (PubMed, J Clin Invest)
    Accordingly, breast cancer patients with a prominent ACVRL1hi TAM signature exhibited a significantly shorter survival. In conclusion, we shed light on an unexpected multimodal regulation of tumorigenic phenotypes by ALK1 and demonstrate its utility as a target for anti-angiogenic immunotherapy.
    Journal • IO biomarker
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    ALK1 (Activin A Receptor Like Type 1) • CD14 (CD14 Molecule) • TGFB1 (Transforming Growth Factor Beta 1) • ACVRL1 (Activin A Receptor Like Type 1)
    11ms
    Recent advances in the dual effects of activin A on tumors. (PubMed, Biochem Biophys Res Commun)
    This review explores the biological functions of activin A in tumor progression and treatment, focusing on its influence on tumor cell proliferation, apoptosis, and metastasis. The aim is to offer insights and potential directions for future clinical cancer treatments.
    Review • Journal
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    TGFB1 (Transforming Growth Factor Beta 1)
    11ms
    Activin A promoted the anti-tumor effect of ActRIIA high CD8+ T cells in mouse hepatoma. (PubMed, Cancer Med)
    This study demonstrated that low-dose activin A enhanced the anti-tumor effect of CD8+ T cells, and ActRIIA high CD8+ T cells actively contribute to tumor immunity.
    Preclinical • Journal
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    CD8 (cluster of differentiation 8) • HAVCR2 (Hepatitis A Virus Cellular Receptor 2) • CD69 (CD69 Molecule) • ICOS (Inducible T Cell Costimulator) • GZMB (Granzyme B) • TGFB1 (Transforming Growth Factor Beta 1) • ITGAX (Integrin Subunit Alpha X) • KLRG1 (Killer Cell Lectin Like Receptor G1) • PRF1 (Perforin 1) • ACVR2A (Activin A Receptor Type 2A) • ITGA2 (Integrin Subunit Alpha 2) • METTL3 (Methyltransferase Like 3) • PPM1A (Protein Phosphatase Mg2+/Mn2+ Dependent 1A) • SMAD2 (SMAD Family Member 2)
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    CD8 expression • CD8-H
    1year
    IGFBP7 is a key component of the senescence-associated secretory phenotype (SASP) that induces senescence in healthy cells by modulating the insulin, IGF, and activin A pathways. (PubMed, Cell Commun Signal)
    Notably, our preliminary data indicate that IGFBP7, in addition to blocking Activin A, may interact with its receptors and induce senescence via SMAD pathways.Our findings highlight that IGFBP7, along with other members of the IGFBP family, plays a pivotal role in senescence-related signaling pathways. Therefore, IGFBP7 may serve as a potential target for anti-aging strategies aimed at reducing the burden of senescence on tissues and organs.
    Journal
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    IGF2 (Insulin-like growth factor 2) • IGFBP7 (Insulin Like Growth Factor Binding Protein 7)
    1year
    Stepwise release of Activin-A from its inhibitory prodomain is modulated by cysteines and requires furin coexpression to promote melanoma growth. (PubMed, Commun Biol)
    Disruption of these disulfide linkages with the prodomain enabled Activin-A binding to cognate type II receptors independently of proteolytic maturation. Stepwise proteolytic maturation is a novel mechanism to control Activin-A protein interactions and signaling.
    Journal
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    FURIN (Furin, Paired Basic Amino Acid Cleaving Enzyme)