A5011783348- Lysosomal Storage Disorders Research
- Molecular Sensors and Ion Detection
- Lanthanide and Transition Metal Complexes
- Chemical Synthesis and Analysis
- Synthesis and biological activity
- Synthesis and Catalytic Reactions
- Synthesis and Characterization of Heterocyclic Compounds
- Calcium signaling and nucleotide metabolism
- Catalytic Cross-Coupling Reactions
- Carbohydrate Chemistry and Synthesis
- Asymmetric Hydrogenation and Catalysis
- Asymmetric Synthesis and Catalysis
- Electron Spin Resonance Studies
- Cellular transport and secretion
- Chemical Synthesis and Reactions
- Receptor Mechanisms and Signaling
- Sulfur-Based Synthesis Techniques
- Catalytic C–H Functionalization Methods
- Analytical Chemistry and Sensors
- Quinazolinone synthesis and applications
- Neuroendocrine regulation and behavior
- Catalytic Alkyne Reactions
- Nitric Oxide and Endothelin Effects
- Proteoglycans and glycosaminoglycans research
- Maternal Mental Health During Pregnancy and Postpartum
De Montfort University
2015-2024
Loughborough University
2021-2023
Pfizer (United States)
2015
University of Nottingham
2015
Park University
2015
Pfizer (United Kingdom)
2009-2011
University of Glasgow
2002
We present two new europium-based anion receptors that selectively bind to inorganic phosphate and AMP in aqueous media. Their sensing selectivity follows the order > ADP ATP, representing a reversal of observed for most nucleoside receptors.
A series of 4-substituted pyrimido[4,5-d]azepines that are potent, selective 5-HT2C receptor partial agonists is described. rational medicinal chemistry design strategy to deliver CNS penetration coupled with SAR-based optimization selectivity and agonist potency provided compounds the desired balance preclinical properties. Lead 17 (PF-4479745) 18 (PF-4522654) displayed robust pharmacology in a canine model stress urinary incontinence (SUI) no measurable functional agonism at key targets...
The accumulation of lipids in the late endosomes and lysosomes Niemann–Pick type C disease (NPCD) cells is a consequence dysfunction one protein (usually NPC1) but induces many proteins. We used molecular docking to propose (a) that NPC1 exports not just cholesterol, also sphingosine, (b) cholesterol sensitivity big potassium channel (BK) can be traced previously unappreciated site on channel’s voltage sensor, (c) transient receptor potential mucolipin 1 (TRPML1) inhibition by sphingomyelin...
This contribution describes the initial preparation of two potent β-3 receptor agonists 1 and 2. Subsequent scale up these compounds was required for further evaluation proceeded via a common key amine intermediate 24. Synthesis this by way Ritter reaction vital step in sequence. Enantioselective Noyori hydrogenation reactions gave access to chiral epoxides necessary make target compounds. Chemistry developed selective dehalogenation 2-chloropyridyl group presence sensitive isoxazole unit provide 1.
We report the first molecular probe for selective detection of most abundant cellular inositol pyrophosphate 5-PP-InsP 5 , supported by computational chemistry, as well an efficient new synthesis.
Linifanib (<bold>1</bold>), a multi-targeted receptor tyrosine kinase inhibitor, self-assembles into hydrogel in the presence of low amounts solvent.
Sulfotransferases constitute a ubiquitous class of enzymes which are poorly understood due to the lack convenient tool for screening their activity. These use anion PAPS (adenosine-3'-phosphate-5'-phosphosulfate) as donor broad range acceptor substrates, including carbohydrates, producing sulfated compounds and PAP (adenosine-3',5'-diphosphate) side product. We present europium(III)-based probe that binds reversibly both PAP, larger luminescence enhancement with latter anion. exploit this...
Abstract Lanthanide complexes have a range of photophysical properties – large pseudo‐Stokes shifts, narrow linewidths, long emission lifetimes that make them ideal as emissive probes. These same also render excellent donors in assays relying on Förster resonance energy transfer (FRET). Over the last 20 years these increased sophistication so biological applications has now been demonstrated. from easy‐to‐use quantitation proteins (a practical alternative to western blotting) sophisticated...
The title compounds are prepared from S-methylisothioureas and acyl hydrazides in moderate to good yields. reaction is characterized by relatively mild conditions very broad functional group tolerance.
N-methylimidazole (NMI) is used as the base in triflic anhydride (Tf2O)–mediated formation of oxadiazoles from diacyl hydrazines. This reagent superior to pyridine-derived bases terms cost and reaction profile.
ABSTRACT Absorption of the 4, 10 and 34 amino acid forms gastrin from small intestine has been investigated in anaesthetized rats. The method assessment successful absorption hormone into systemic circulation was when amount secreted by stomach over consecutive 15‐min periods increased. When natural hormones were infused ileum a relatively high dose, there no increase gastric secretion, indicating that they had not absorbed. Each conjugated at free terminus to carboxyl group cholic acid....
Gaucher disease is caused by mutations in the Gba1 gene encoding an acid β-glucocerebrosidase (GBA1), lysosomal hydrolase which breaks down glucosylceramide (GlcCer). In type 1 accumulation of this simple glycolipid mainly restricted to tissue phagocyte lysosomes resulting ultimately hepatomegaly, splenomegaly and osteopenia. Lower residual GBA1 levels leads neuronal storage, types 2 3 neurological symptoms are characterised acute (death at age 2) or sub-acute onset, respectively. The links...
Abstract Commercial tea tree oil (TTO) has to conform chemically the international standard ISO4730: 2017, which defines acceptable ranges for 15 main terpenoids therein. Lack of in‐house capacity technology typically required terpenoid quantification (GC‐FID) necessitates that Australian TTO producers outsource analyses commercial service providers. This is associated with high cost and slow turnaround times, have been recognized as limiting factors process optimization in areas quality...
Niemann–Pick type C disease (NPCD) is a rare neurodegenerative disorder most commonly caused by mutations in the lysosomal protein C1 (NPC1), which implicated cholesterol export. Mitochondrial insufficiency forms significant feature of pathology this disease, yet studies attempting to address are rare. The working hypothesis that mitochondria become overloaded with renders them dysfunctional. We examined two potential targets—translocator (TSPO) and steroidogenic acute regulatory D1...
The performance of many known fluorescent sensors for Ca
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