A patch of positively charged residues regulates the efficacy of clinical DR5 antibodies in solid tumors.
Sign Up to like & getrecommendations! Published in 2021 at "Cell reports"
DOI: 10.1016/j.celrep.2021.109953
Abstract: Receptor clustering is the first and critical step to activate apoptosis by death receptor-5 (DR5). The recent discovery of the autoinhibitory DR5 ectodomain has challenged the long-standing view of its mechanistic activation by the natural… read more here.
Keywords: residues regulates; dr5 antibodies; positively charged; charged residues ... See more keywords
BIX-01294 sensitizes renal cancer Caki cells to TRAIL-induced apoptosis through downregulation of survivin expression and upregulation of DR5 expression
Sign Up to like & getrecommendations! Published in 2018 at "Cell Death Discovery"
DOI: 10.1038/s41420-018-0035-8
Abstract: BIX-01294 (BIX), a G9a histone methyltransferase inhibitor, has been reported for its anti-proliferative and anticancer activities against various cancer cell lines. In this study, we investigated whether BIX could sensitize TRAIL-mediated apoptosis in various cancer… read more here.
Keywords: apoptosis; induced apoptosis; expression; dr5 ... See more keywords
A New Efficient Method for Production of Recombinant Antitumor Cytokine TRAIL and Its Receptor-Selective Variant DR5-B
Sign Up to like & getrecommendations! Published in 2019 at "Biochemistry (Moscow)"
DOI: 10.1134/s0006297919060051
Abstract: The cytokine TRAIL induces apoptosis in tumor cells of various origin without affecting normal cells. Clinical trials of TRAIL-receptor (DR4 and DR5) agonists (recombinant TRAIL or death receptors antibodies) have largely failed because most human… read more here.
Keywords: efficient method; cytokine trail; dr5; trail ... See more keywords
Abstract 518: Agonistic Death Receptor 5 (DR5) IgM antibody IGM-8444 induces tumor cell apoptosisin vitroandin vivoand has a favorablein vitrosafety profile
Sign Up to like & getrecommendations! Published in 2020 at "Cancer Research"
DOI: 10.1158/1538-7445.am2020-518
Abstract: Death receptor 5 (DR5) is a member of the tumor necrosis factor (TNF) receptor superfamily that binds TNF-related apoptosis inducing ligand (TRAIL) to induce receptor trimerization and activate extrinsic apoptotic pathways. DR5 is expressed on… read more here.
Keywords: igm 8444; dr5; receptor; cell ... See more keywords
Indirubin Inhibits TRAIL-Induced Activation of Death Receptor 5 in Jurkat Cells
Sign Up to like & getrecommendations! Published in 2023 at "Natural Product Communications"
DOI: 10.1177/1934578x221144580
Abstract: Death receptor 5 (DR5) is an apoptosis-inducing membrane receptor that mediates cell death in several life-threatening conditions. There is a crucial need for the discovery of DR5 antagonists for the therapeutic intervention of conditions in… read more here.
Keywords: death receptor; death; dr5; trail induced ... See more keywords
Tubulin couples death receptor 5 to regulate apoptosis
Sign Up to like & getrecommendations! Published in 2018 at "Oncotarget"
DOI: 10.18632/oncotarget.26407
Abstract: Activation of death receptor 5 (DR5) to induce apoptosis in cancer cells is an attractive strategy for cancer therapy. However, many tumor cell lines and primary tumors are resistant to DR5 targeted agents including recombinant… read more here.
Keywords: dr5; death receptor; tubulin; apoptosis ... See more keywords
Optimized Heterologous Expression and Efficient Purification of a New TRAIL-Based Antitumor Fusion Protein SRH–DR5-B with Dual VEGFR2 and DR5 Receptor Specificity
Sign Up to like & getrecommendations! Published in 2022 at "International Journal of Molecular Sciences"
DOI: 10.3390/ijms23115860
Abstract: In the last two decades, bifunctional proteins have been created by genetic and protein engineering methods to increase therapeutic effects in various diseases, including cancer. Unlike conventional small molecule or monotargeted drugs, bifunctional proteins have… read more here.
Keywords: trail; srh dr5; fusion protein; dr5 ... See more keywords
Restoring TRAILR2/DR5-Mediated Activation of Apoptosis upon Endoplasmic Reticulum Stress as a Therapeutic Strategy in Cancer
Sign Up to like & getrecommendations! Published in 2022 at "International Journal of Molecular Sciences"
DOI: 10.3390/ijms23168987
Abstract: The uncontrolled proliferation of malignant cells in growing tumors results in the generation of different stressors in the tumor microenvironment, such as nutrient shortage, hypoxia and acidosis, among others, that disrupt endoplasmic reticulum (ER) homeostasis… read more here.
Keywords: endoplasmic reticulum; stress; apoptosis; dr5 ... See more keywords
Pharmacological Small Molecules against Prostate Cancer by Enhancing Function of Death Receptor 5
Sign Up to like & getrecommendations! Published in 2022 at "Pharmaceuticals"
DOI: 10.3390/ph15081029
Abstract: Death receptor 5 (DR5) is a membrane protein that mediates exogenous apoptosis. Based on its function, it is considered to be a target for the treatment of cancers including prostate cancer. It is encouraging to… read more here.
Keywords: function; prostate cancer; molecules prostate; small molecules ... See more keywords
Amphiphilic Poly(N-vinylpyrrolidone) Nanoparticles Conjugated with DR5-Specific Antitumor Cytokine DR5-B for Targeted Delivery to Cancer Cells
Sign Up to like & getrecommendations! Published in 2021 at "Pharmaceutics"
DOI: 10.3390/pharmaceutics13091413
Abstract: Nanoparticles based on the biocompatible amphiphilic poly(N-vinylpyrrolidone) (Amph-PVP) derivatives are promising for drug delivery. Amph-PVPs self-aggregate in aqueous solutions with the formation of micellar nanoscaled structures. Amph-PVP nanoparticles are able to immobilize therapeutic molecules under… read more here.
Keywords: delivery; amph pvp; dr5; antitumor ... See more keywords