Search Results - "Holyer, Ian"
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Resistance to anti-PD-1/anti-PD-L1: galectin-3 inhibition with GB1211 reverses galectin-3-induced blockade of pembrolizumab and atezolizumab binding to PD-1/PD-L1
Published in Frontiers in immunology (28-08-2023)“…Background Galectin-3 (Gal-3) is a β-galactoside-binding lectin that is highly expressed within the tumor microenvironment of aggressive cancers and has been…”
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Design, Synthesis, and Characterization of I‑BET567, a Pan-Bromodomain and Extra Terminal (BET) Bromodomain Oral Candidate
Published in Journal of medicinal chemistry (10-02-2022)“…Through regulation of the epigenome, the bromodomain and extra terminal (BET) family of proteins represent important therapeutic targets for the treatment of…”
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The galectin-3 inhibitor selvigaltin reduces liver inflammation and fibrosis in a high fat diet rabbit model of metabolic-associated steatohepatitis
Published in Frontiers in pharmacology (31-07-2024)“…Galectin-3 is a pro-fibrotic β-galactoside binding lectin highly expressed in fibrotic liver and implicated in hepatic fibrosis. Selvigaltin (previously known…”
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Structure- and Property-Based Optimization of Efficient Pan-Bromodomain and Extra Terminal Inhibitors to Identify Oral and Intravenous Candidate I‑BET787
Published in Journal of medicinal chemistry (27-06-2024)“…The bromodomain and extra terminal (BET) family of bromodomain-containing proteins are important epigenetic regulators that elicit their effect through binding…”
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Preclinical Evaluation of a Food-Derived Functional Ingredient to Address Skeletal Muscle Atrophy
Published in Nutrients (29-07-2020)“…Skeletal muscle is the metabolic powerhouse of the body, however, dysregulation of the mechanisms involved in skeletal muscle mass maintenance can have…”
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Discovery through Machine Learning and Preclinical Validation of Novel Anti-Diabetic Peptides
Published in Biomedicines (09-03-2021)“…While there have been significant advances in drug discovery for diabetes mellitus over the past couple of decades, there is an opportunity and need for…”
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BET bromodomain inhibitors show anti-papillomavirus activity in vitro and block CRPV wart growth in vivo
Published in Antiviral research (01-06-2018)“…The DNA papillomaviruses infect squamous epithelium and can cause persistent, benign and sometimes malignant hyperproliferative lesions. Effective antiviral…”
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Abstract LB173: A bioinformatics approach to determine the potential benefit of blocking both Galectin-1 and Galectin-3 in cancer
Published in Cancer research (Chicago, Ill.) (14-04-2023)“…Abstract Galectins are a family of Beta-galactoside-binding lectins that control numerous cellular processes in health and disease, including fibrosis,…”
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Galectin-1 Induces the Production of Immune-Suppressive Cytokines in Human and Mouse T Cells
Published in International journal of molecular sciences (07-11-2024)“…Galectin-1 is implicated in several pro-tumourigenic mechanisms and is considered immune-suppressive. The pharmacological inhibition of galectin-1 may be…”
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Abstract LB104: Preclinical evaluation of the role of Galectin-1 in tumor immune evasion associated mechanisms using a highly selective Galectin-1 small molecule inhibitor
Published in Cancer research (Chicago, Ill.) (14-04-2023)“…Abstract Galectin-1 (Gal-1) is a β-galactoside-binding lectin that is highly expressed within the tumor microenvironment (TME) of some aggressive cancers and…”
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Journal Article -
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Discovery of the Selective and Orally Available Galectin‑1 Inhibitor GB1908 as a Potential Treatment for Lung Cancer
Published in Journal of medicinal chemistry (13-06-2024)“…We have previously described a new series of selective and orally available galectin-1 inhibitors resulting in the thiazole-containing glycomimetic GB1490…”
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Effect of GB1107, a novel galectin-3 inhibitor on pro-fibrotic signalling in the liver
Published in European journal of pharmacology (01-12-2024)“…Galectin-3 (Gal-3) is a pro-fibrotic β-galactoside binding lectin highly expressed in fibrotic liver and implicated in hepatic fibrosis. GB1107 is a novel…”
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Relative bioavailability and food effect of the galectin-3 inhibitor selvigaltin (GB1211) administered as a tablet in healthy participants (GALBA-1)
Published in Cancer chemotherapy and pharmacology (01-11-2024)“…Purpose Overexpression of galectin-3, a β-galactoside-binding lectin, is associated with fibrotic diseases and cancer. Selvigaltin is an oral galectin-3…”
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The role of platelets and their associated recruitment mechanisms, in intestinal ischaemia reperfusion injury
Published 01-01-2011“…Recent studies have demonstrated a key role for platelets and microthrombi in the pathophysiology of intestinal ischaemia-reperfusion (IR) injury. The research…”
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Dissertation -
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Towards Secure SPARQL Queries in Semantic Web Applications Using PHP
Published in 2017 IEEE 11th International Conference on Semantic Computing (ICSC) (2017)“…The Semantic Web (SW) is a significant advancement in the field of Internet technologies and an uncharted territory as far as security is concerned. In this…”
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Conference Proceeding -
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Towards Secure SPARQL Queries in Semantic Web Applications using PHP (Extended Version)
Published 26-01-2017“…The Semantic Web (SW) is a significant advancement in the field of Internet technologies and an uncharted territory as far as security is concerned. In this…”
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Journal Article -
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A Recovery Mechanism for Shells
Published in Computer journal (01-01-2000)“…An undo facility is an essential component of most interactive applications. In current operating system shells, whether textual or graphical, such facilities…”
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Journal Article