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Development of a 1:1-binding biparatopic anti-TNFR2 antagonist by reducing signaling activity through epitope selection
Conventional bivalent antibodies against cell surface receptors often initiate unwanted signal transduction by crosslinking two antigen molecules....
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Synthesis of the Antagonist of the GalR2 Galanin Receptor and Studies of Its Biological Activity in Ischemia and Reperfusion of the Rat Heart In Vivo
AbstractThe dose-dependent action of the M871 synthetic peptide antagonist of the GalR2 galanin receptor...
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Structural insights into human ABCC4-mediated transport of platelet agonist and antagonist
Human platelets contribute to hemostasis and thrombosis, the imbalance of which can cause cardiovascular diseases. The activation and accumulation of...
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Vemurafenib inhibits necroptosis in normal and pathological conditions as a RIPK1 antagonist
Necroptosis, a programmed cell death with necrotic-like morphology, has been recognized as an important driver in various inflammatory diseases....
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Neuroprotective effects of the PPARβ/δ antagonist GSK0660 in in vitro and in vivo Parkinson’s disease models
BackgroundThe underlying mechanism of Parkinson’s disease are still unidentified, but excitotoxicity, oxidative stress, and neuroinflammation are...
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The dopamine transporter antagonist vanoxerine inhibits G9a and suppresses cancer stem cell functions in colon tumors
Cancer stem cells (CSCs), functionally characterized by self-renewal and tumor-initiating activity, contribute to decreased tumor immunogenicity,...
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A GIPR antagonist conjugated to GLP-1 analogues promotes weight loss with improved metabolic parameters in preclinical and phase 1 settings
Obesity is a major public health crisis. Multi-specific peptides have emerged as promising therapeutic strategies for clinical weight loss....
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TRAF2/3 deficient B cells resist DNA damage-induced apoptosis via NF-κB2/XIAP/cIAP2 axis and IAP antagonist sensitizes mutant lymphomas to chemotherapeutic drugs
Deletion of TRAF2 or TRAF3 in B cells prolongs their survival. However, it remains unknown whether deletion of such factors affects B cells’ ability...
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Tumor-derived interleukin-1 receptor antagonist exhibits immunosuppressive functions and promotes pancreatic cancer
BackgroundPancreatic ductal adenocarcinoma (PDA) is a pernicious disease characterized by an immunosuppressive milieu that is unresponsive to current...
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An Atomic Level Investigation of Sodium Ions Regulating Agonist and Antagonist Binding in the Active Site of a Novel Target 5HT2BR Against Drug-Resistant Epilepsy
The study investigates the movement of sodium ions inside the ligand-binding pocket of the class-A GPCR serotonin receptor (5HT 2B R), a primary target...
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The Influence of Kappa Opioid Receptor Antagonist 5'-Guanidinonaltrindole during Reproductive Stress Response in the Mozambique Tilapia Oreochromis mossambicus (Cichlidae)
AbstractThe endogenous opioidergic system is known to exert its effect on various physiological processes through specific opioid receptors. In this...
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The Effects of Ghrelin on Spike Activity of the Suprachiasmatic Nucleus Neurones of the Rat
AbstractIn one of the most important non-photic mechanisms of the circadian biological clock synchronization of the hypothalamus...
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Unveiling the transcriptomic landscape and the potential antagonist feedback mechanisms of TGF-β superfamily signaling module in bone and osteoporosis
BackgroundTGF-β superfamily signaling is indispensable for bone homeostasis. However, the global expression profiles of all the genes that make up...
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Case Study #6: [177Lu]Lu-DOTA-JR11: A Somatostatin Receptor Subtype 2 Antagonist for Radiopharmaceutical Therapy
Peptide receptor radionuclide therapy (PRRT) is a special type of radiopharmaceutical therapy (RPT) that employs peptide-based radiopharmaceuticals...
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Inhibition of p38 MAPK or immunoproteasome overcomes resistance of chronic lymphocytic leukemia cells to Bcl-2 antagonist venetoclax
Chronic lymphocytic leukemia (CLL) is a hematological neoplasm of CD19-positive mature-appearing B lymphocytes. Despite the clinical success of...
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A novel prostaglandin E receptor 4 (EP4) small molecule antagonist induces articular cartilage regeneration
Articular cartilage repair and regeneration is an unmet clinical need because of the poor self-regeneration capacity of the tissue. In this study, we...
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The NMDA receptor antagonist ketamine impairs and delays context-dependent decision making in the parietal cortex
Flexible decision making is an indispensable ability for humans. A subanesthetic dose of ketamine, an N-methyl-D-aspartate receptor antagonist,...
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Investigating the relationship between the VNTR variant of the interleukin-1 receptor antagonist gene and coronary in-stent restenosis
ObjectiveThis study aimed to examine the association between the interleukin-1 receptor antagonist gene (IL-1RN) and coronary in-stent restenosis...
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