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Functional Linkers Support Targeting of Multivalent Tweezers to Taspase1.
Chemistry
October 2024
Molecular Biology II, Center of Medical Biotechnology (ZMB) and Center for Nanointegration (CENIDE), University of Duisburg-Essen, Universitätsstrasse 5, 45141, Essen, Germany.
Taspase 1 is a unique protease not only pivotal for embryonic development but also implicated in leukemias and solid tumors. As such, this enzyme is a promising while still challenging therapeutic target, and with its protein structure featuring a flexible loop preceding the active site a versatile model system for drug development. Supramolecular ligands provide a promising complementary approach to traditional small-molecule inhibitors.
View Article and Find Full Text PDFClosantel is an allosteric inhibitor of human Taspase1.
iScience
December 2021
Institute of Pharmaceutical Biology/DCAL, Goethe-University of Frankfurt, Biocenter, Max-von-Laue-Street 9, 60438 Frankfurt/Main, Germany.
Dimerization of Taspase1 activates an intrinsic serine protease function that leads to the catalytic Thr234 residue, which allows to catalyze the consensus sequence QXD⋅GXDD, present in Trithorax family members and TFIIA. Noteworthy, Taspase1 performs only a single hydrolytic step on substrate proteins, which makes it impossible to screen for inhibitors in a classical screening approach. Here, we report the development of an HTRF reporter assay that allowed the identification of an inhibitor, Closantel sodium, that inhibits Taspase1 in a noncovalent fashion (IC = 1.
View Article and Find Full Text PDFA Bivalent Supramolecular GCP Ligand Enables Blocking of the Taspase1/Importin α Interaction.
ChemMedChem
January 2022
Institute for Molecular Biology II, Center for Medical Biotechnology (ZMB), University of Duisburg-Essen, Universitätsstrasse 5, 45117, Essen, Germany.
Taspase1 is a unique protease not only pivotal for embryonic development but also implicated in leukemia as well as solid tumors. As such, it is a promising target in cancer therapy, although only a limited number of Taspase1 inhibitors lacking general applicability are currently available. Here we present a bivalent guanidiniocarbonyl-pyrrole (GCP)-containing supramolecular ligand that is capable of disrupting the essential interaction between Taspase1 and its cognate import receptor Importin α in a concentration-dependent manner in vitro with an IC of 35 μM.
View Article and Find Full Text PDFSilencing of circTASP1 inhibits proliferation and induces apoptosis of acute myeloid leukaemia cells through modulating miR-515-5p/HMGA2 axis.
J Cell Mol Med
August 2021
Jiangxi Institute of Urology, The First Affiliated Hospital of Nanchang University, Nanchang, China.
Acute myeloid leukaemia (AML) is a common hematopoietic disease that is harmful to the lives of children and adults. CircRNAs are aberrantly expressed in the haematologic malignancy cells. However, the expression of circTASP1 and its function in AML remain unclear.
View Article and Find Full Text PDFTASP1 Promotes Proliferation and Migration in Gastric Cancer via EMT and AKT/P-AKT Pathway.
J Immunol Res
November 2021
The Affiliated Huai'an Hospital of Xuzhou Medical University and The Second People's Hospital of Huai'an, No. 62, Huaihai Road (S.), Huaian 223002, China.
Threonine aspartase 1 (TASP1) was reported to function in the development of cancer. However, the regulatory mechanism of TASP1 in gastric cancer (GC) remains unclear. In this study, we determined the expression of TASP1 in tissues of GC patients, GC cells by qRT-PCR, and western blot and assessed the relationship between TASP1 and GC cell proliferation and migration via CCK-8 and transwell assay.
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