Ligandability assessment of the C‐terminal Rel‐homology domain of NFAT1
Sign Up to like & getrecommendations! Published in 2024 at "Archiv der Pharmazie"
DOI: 10.1002/ardp.202300649
Abstract: Transcription factors are generally considered challenging, if not “undruggable”, targets but they promise new therapeutic options due to their fundamental involvement in many diseases. In this study, we aim to assess the ligandability of the… read more here.
Keywords: ligandability; terminal rel; rel homology; homology domain ... See more keywords
The iRhom homology domain is indispensable for ADAM17-mediated TNFα and EGF receptor ligand release
Sign Up to like & getrecommendations! Published in 2021 at "Cellular and Molecular Life Sciences"
DOI: 10.1007/s00018-021-03845-3
Abstract: Membrane-tethered signalling proteins such as TNFα and many EGF receptor ligands undergo shedding by the metalloproteinase ADAM17 to get released. The pseudoproteases iRhom1 and iRhom2 are important for the transport, maturation and activity of ADAM17.… read more here.
Keywords: adam17; egf receptor; irhd; homology domain ... See more keywords
Identification of phostensin in association with Eps 15 homology domain-containing protein 1 (EHD1) and EHD4.
Sign Up to like & getrecommendations! Published in 2020 at "Biochemical and biophysical research communications"
DOI: 10.1016/j.bbrc.2020.07.030
Abstract: Phostensin (PTS) encoded by KIAA1949 is a protein phosphatase 1 (PP1)-binding protein. In order to explore the cellular functions of PTS, we have searched PTS-binding proteins by using co-immunoprecipitation in combination with shotgun proteomics. Here,… read more here.
Keywords: protein; domain containing; protein ehd1; homology domain ... See more keywords
Targeting Oncogenic Src Homology 2 Domain-Containing Phosphatase 2 (SHP2) by Inhibiting Its Protein–Protein Interactions
Sign Up to like & getrecommendations! Published in 2021 at "Journal of Medicinal Chemistry"
DOI: 10.1021/acs.jmedchem.1c01371
Abstract: We developed a new class of inhibitors of protein–protein interactions of the SHP2 phosphatase, which is pivotal in cell signaling and represents a central target in the therapy of cancer and rare diseases. Currently available… read more here.
Keywords: protein; shp2; src homology; protein interactions ... See more keywords
Discovery of Novel Src Homology-2 Domain-Containing Phosphatase 2 and Histone Deacetylase Dual Inhibitors with Potent Antitumor Efficacy and Enhanced Antitumor Immunity.
Sign Up to like & getrecommendations! Published in 2022 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.2c00866
Abstract: Both Src homology-2 domain-containing phosphatase 2 (SHP2) and histone deacetylase (HDAC) are important oncoproteins and potential immunomodulators. In this study, we first observed a synergistic antiproliferation effect of an allosteric SHP2 inhibitor (SHP099) and HDAC… read more here.
Keywords: dual inhibitors; src homology; containing phosphatase; homology domain ... See more keywords
First Results of Migoprotafib, a Potent and Highly Selective Src Homology-2 Domain–Containing Phosphatase 2 Inhibitor in Patients with Advanced Solid Tumors
Sign Up to like & getrecommendations! Published in 2024 at "Molecular Cancer Therapeutics"
DOI: 10.1158/1535-7163.mct-24-0466
Abstract: Abstract Src homology-2 domain–containing phosphatase 2 promotes rat sarcoma viral oncogene homolog–MAPK signaling and tumorigenesis and is a promising therapeutic target for multiple solid tumors. Migoprotafib is a potent and highly selective Src homology-2 domain–containing… read more here.
Keywords: solid tumors; domain containing; src homology; containing phosphatase ... See more keywords
The expression of Eps15 homology domain 1 is negatively correlated with disease-free survival and overall survival of osteosarcoma patients
Sign Up to like & getrecommendations! Published in 2019 at "Journal of Orthopaedic Surgery and Research"
DOI: 10.1186/s13018-019-1137-6
Abstract: BackgroundOsteosarcoma was locally aggressive and frequently metastasizes to the lung. However, the etiology of osteosarcoma was unknown. Thus, exploring the mechanisms behind the occurrence of osteosarcoma was important for its prediction and prevention. To investigate… read more here.
Keywords: osteosarcoma; homology domain; expression ehd1; eps15 homology ... See more keywords
Regulation of AKT activity by inhibition of the pleckstrin homology domain-PtdIns(3,4,5)P3 interaction using flavonoids.
Sign Up to like & getrecommendations! Published in 2018 at "Journal of microbiology and biotechnology"
DOI: 10.4014/jmb.1805.04051
Abstract: The serine-threonine kinase AKT plays a pivotal role in tumor progression and is frequently overactivated in cancer cells; this protein is therefore a critical therapeutic target for cancer intervention. We aimed to identify small molecule… read more here.
Keywords: akt; pleckstrin homology; inhibition; homology domain ... See more keywords