Talabostat mesilate is an orally active, specific inhibitor of dipeptidyl peptidases, including tumor-associated fibroblast activation protein. However, by an independent mechanism, talabostat also stimulates the upregulation of cytokines and chemokines to engender a tumor-specific host immune response, thus giving it a unique dual mechanism of action. In clinical trials, talabostat has demonstrated significant activity, including achieving complete responses in patients with non-small-cell lung cancer and malignant melanoma.
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Comparison of Different Keratinocyte Cell Line Models for Analysis of NLRP1 Inflammasome Activation.
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Department of Dermatology and Allergology, University Hospital RWTH Aachen, 52074 Aachen, Germany.
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Integrated Genetic and Cellular Analysis Reveals NLRP1 Activation in CD4+ T Lymphocytes During Chronic HIV Infection.
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Laboratório de Imunogenética, Departamento de Imunologia, Instituto de Ciências Biomédicas/ICB, Universidade de São Paulo/USP, São Paulo, Brazil.
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Institute of Innate Immunity, Department for Systems Immunology and Proteomics, Medical Faculty, University of Bonn, Bonn, Germany.
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Talabostat, fibroblast activation protein inhibitor, attenuates inflammation and fibrosis in systemic sclerosis.
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Department of Immunology, School of Medicine, Tehran University of Medical Sciences, Tehran, Iran.
Background: Systemic sclerosis (SSc) is a connective tissue disorder characterized by excessive fibrosis, where activated fibroblasts play a pivotal role in disease progression. This study aimed to investigate the potential of Talabostat, a small molecule inhibitor of dipeptidyl peptidases, in alleviating fibrosis and inflammation associated with SSc pathogenesis.
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Department of Clinical Pharmacology, Hunan Key Laboratory of Pharmacogenetics, and National Clinical Research Center for Geriatric Disorders, Xiangya Hospital, Central South University, Changsha 410008, China.
The remarkable efficacy of cancer immunotherapy has been established in several tumor types. Of the various immunotherapies, PD-1/PD-L1 inhibitors are most extensively used in the treatment of many cancers in clinics. These inhibitors restore the suppressed antitumor immune response and inhibit tumor progression by blocking the PD-1/PD-L1 signaling.
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