Search Results - "Harris, Jonathan M"
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Correlation of Experimental and Calculated Inhibition Constants of Protease Inhibitor Complexes
Published in International journal of molecular sciences (01-02-2024)“…Predicting the potency of inhibitors is key to in silico screening of promising synthetic or natural compounds. Here we describe a predictive workflow that…”
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Engineered protease inhibitors based on sunflower trypsin inhibitor-1 (SFTI-1) provide insights into the role of sequence and conformation in Laskowski mechanism inhibition
Published in Biochemical journal (15-07-2015)“…Laskowski inhibitors regulate serine proteases by an intriguing mode of action that involves deceiving the protease into synthesizing a peptide bond. Studies…”
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3
Substrate-Guided Design of Selective FXIIa Inhibitors Based on the Plant-Derived Momordica cochinchinensis Trypsin Inhibitor-II (MCoTI-II) Scaffold
Published in Journal of medicinal chemistry (11-08-2016)“…Thrombosis is a leading cause of morbidity and mortality associated with cardiovascular diseases. Inhibition of factor XIIa (FXIIa) provides thrombus…”
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Plasmin Substrate Binding Site Cooperativity Guides the Design of Potent Peptide Aldehyde Inhibitors
Published in Biochemistry (Easton) (04-10-2011)“…Perioperative bleeding is a cause of major blood loss and is associated with increased rates of postoperative morbidity and mortality. To combat this,…”
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Functional analysis and theoretical modeling of ferroportin reveals clustering of mutations according to phenotype
Published in American Journal of Physiology: Cell Physiology (01-01-2010)“…Ferroportin disease is a heterogeneous iron release disorder resulting from mutations in the ferroportin gene. Ferroportin protein is a multitransmembrane…”
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Discrimination of Methionine Sulfoxide and Sulfone by Human Neutrophil Elastase
Published in Molecules (Basel, Switzerland) (02-09-2021)“…Human neutrophil elastase (HNE) is a uniquely destructive serine protease with the ability to unleash a wave of proteolytic activity by destroying the…”
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Paclitaxel resistance and multicellular spheroid formation are induced by kallikrein-related peptidase 4 in serous ovarian cancer cells in an ascites mimicking microenvironment
Published in PloS one (25-02-2013)“…High tumor kallikrein-related-peptidase 4 (KLK4) levels are associated with a poor outcome for women with serous epithelial ovarian cancer (EOC), for which…”
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Potent, multi-target serine protease inhibition achieved by a simplified β-sheet motif
Published in PloS one (2019)“…Engagement of an extended β-sheet is a common substrate/inhibitor interaction at the active site of serine proteases and is an important feature of Laskowski…”
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A TriAdj-Adjuvanted Chlamydia trachomatis CPAF Protein Vaccine Is Highly Immunogenic in Pigs
Published in Vaccines (Basel) (16-04-2024)“…( ) infections are the most common sexually transmitted infection (STI). Despite effective antibiotics for , undetected infections or delayed treatment can…”
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Mastering the canonical loop of serine protease inhibitors: enhancing potency by optimising the internal hydrogen bond network
Published in PloS one (27-04-2011)“…Canonical serine protease inhibitors commonly bind to their targets through a rigid loop stabilised by an internal hydrogen bond network and disulfide bond(s)…”
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Natural and Engineered Plasmin Inhibitors: Applications and Design Strategies
Published in Chembiochem : a European journal of chemical biology (13-02-2012)“…The serine protease plasmin is ubiquitously expressed throughout the human body in the form of the zymogen plasminogen. Conversion to active plasmin occurs…”
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An androgen receptor mutation in the MDA-MB-453 cell line model of molecular apocrine breast cancer compromises receptor activity
Published in Endocrine-related cancer (01-08-2012)“…Recent evidence indicates that the estrogen receptor-α-negative, androgen receptor (AR)-positive molecular apocrine subtype of breast cancer is driven by AR…”
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13
Mutation of the Androgen Receptor Causes Oncogenic Transformation of the Prostate
Published in Proceedings of the National Academy of Sciences - PNAS (25-01-2005)“…Recent evidence demonstrates that the androgen receptor (AR) continues to influence prostate cancer growth despite medical therapies that reduce circulating…”
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Non-combinatorial library screening reveals subsite cooperativity and identifies new high-efficiency substrates for kallikrein-related peptidase 14
Published in Biological chemistry (01-05-2012)“…An array of substrates link the tryptic serine protease, kallikrein-related peptidase 14 (KLK14), to physiological functions including desquamation and…”
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Increased Prefrontal Gyrification in a Large High-Risk Cohort Characterizes Those Who Develop Schizophrenia and Reflects Abnormal Prefrontal Development
Published in Biological psychiatry (1969) (01-10-2007)“…Background In our cohort considered at high risk (HR) of developing schizophrenia, we previously found a significant difference in extent of right prefrontal…”
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Proteases and proteomics: Cutting to the core of human skin pathologies
Published in Proteomics. Clinical applications (01-06-2014)“…Preserving the integrity of the skin's outermost layer (the epidermis) is vital for humans to thrive in hostile surroundings. Covering the entire body, the…”
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Aprataxin Forms a Discrete Branch in the HIT (Histidine Triad) Superfamily of Proteins with Both DNA/RNA Binding and Nucleotide Hydrolase Activities
Published in The Journal of biological chemistry (19-05-2006)“…Ataxia with oculomotor apraxia type 1 (AOA1) is an early onset autosomal recessive spinocerebellar ataxia with a defect in the protein Aprataxin, implicated in…”
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The AF-1 Domain of the Orphan Nuclear Receptor NOR-1 Mediates Trans-activation, Coactivator Recruitment, and Activation by the Purine Anti-metabolite 6-Mercaptopurine
Published in The Journal of biological chemistry (04-07-2003)“…NOR-1/NR4A3 is an âorphan memberâ of the nuclear hormone receptor superfamily. NOR-1 and its close relatives Nurr1 and Nur77 are members of the NR4A…”
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Abnormal cortical folding in high-risk individuals: a predictor of the development of schizophrenia?
Published in Biological psychiatry (1969) (01-08-2004)“…A number of studies have found localized differences in the appearance and extent of cortical folding between the brains of schizophrenic patients and healthy…”
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Pre-frontal lobe gyrification index in schizophrenia, mental retardation and comorbid groups: An automated study
Published in NeuroImage (Orlando, Fla.) (01-04-2007)“…In this paper, we describe the application of an automated method of calculating Gyrification Index (GI) – the Automated GI (A-GI) – to a total of 95…”
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