Search Results - "Abbott, Belinda M."
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1
A novel small molecule inhibitor of human Drp1
Published in Scientific reports (13-12-2022)“…Mitochondrial dynamin-related protein 1 (Drp1) is a large GTPase regulator of mitochondrial dynamics and is known to play an important role in numerous…”
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Recent progress towards an effective treatment of amyotrophic lateral sclerosis using the SOD1 mouse model in a preclinical setting
Published in European journal of medicinal chemistry (04-10-2016)“…Amyotrophic lateral sclerosis (ALS) is a progressive, fatal and incurable neurodegenerative disorder. Motor neurone degeneration can be caused by genetic…”
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3
The Fragment-Based Development of a Benzofuran Hit as a New Class of Escherichia coli DsbA Inhibitors
Published in Molecules (Basel, Switzerland) (18-10-2019)“…A fragment-based drug discovery approach was taken to target the thiol-disulfide oxidoreductase enzyme DsbA from ( DsbA). This enzyme is critical for the…”
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4
Towards novel herbicide modes of action by inhibiting lysine biosynthesis in plants
Published in eLife (27-07-2021)“…Weeds are becoming increasingly resistant to our current herbicides, posing a significant threat to agricultural production. Therefore, new herbicides with…”
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Enhancing allosteric inhibition of dihydrodipicolinate synthase through the design and synthesis of novel dimeric compounds
Published in RSC medicinal chemistry (19-09-2023)“…The synthesis of the first dimeric inhibitor of E. coli dihydrodipicolinate synthase (DHDPS) is reported herein. Inspired by 2,4-thiazolidinedione based…”
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6
A dual-target herbicidal inhibitor of lysine biosynthesis
Published in eLife (20-06-2022)“…Herbicides with novel modes of action are urgently needed to safeguard global agricultural industries against the damaging effects of herbicide-resistant…”
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7
Structural Determinants Defining the Allosteric Inhibition of an Essential Antibiotic Target
Published in Structure (London) (02-08-2016)“…Dihydrodipicolinate synthase (DHDPS) catalyzes the first committed step in the lysine biosynthesis pathway of bacteria. The pathway can be regulated by…”
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A total synthesis of a highly N-methylated cyclodepsipeptide [2S,3S-Hmp]-aureobasidin L using solid-phase methods
Published in Tetrahedron (01-04-2014)“…[2S,3S-Hmp]-Aureobasidin L 2 has been successfully synthesised through a combination of solution- and solid-phase peptide synthesis. All of the Fmoc-protected…”
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9
Exploration of 3-methylisoquinoline-4-carbonitriles as protein kinase A inhibitors of Plasmodium falciparum
Published in Bioorganic & medicinal chemistry (01-06-2016)“…[Display omitted] A series of isoquinolines have been evaluated in a homology model of Plasmodium falciparum Protein Kinase A (PfPKA) using molecular dynamics…”
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Elaboration of a benzofuran scaffold and evaluation of binding affinity and inhibition of Escherichia coli DsbA: A fragment-based drug design approach to novel antivirulence compounds
Published in Bioorganic & medicinal chemistry (01-09-2021)“…[Display omitted] Bacterial thiol-disulfide oxidoreductase DsbA is essential for bacterial virulence factor assembly and has been identified as a viable…”
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11
Synthesis and structure-activity relationship studies of 2,4-thiazolidinediones and analogous heterocycles as inhibitors of dihydrodipicolinate synthase
Published in Bioorganic & medicinal chemistry (15-12-2021)“…[Display omitted] Dihydrodipicolinate synthase (DHDPS), responsible for the first committed step of the diaminopimelate pathway for lysine biosynthesis, has…”
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Synthesis of novel 1,2,5-oxadiazoles and evaluation of action against Acinetobacter baumannii
Published in Bioorganic & medicinal chemistry (15-12-2017)“…[Display omitted] With multidrug resistant bacteria on the rise, novel antibiotics are becoming highly sought after. In 2008, eleven compounds were identified…”
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13
Discovery, synthesis and exploration of N-benzylsulfonyl-2-phenylazepanes as inhibitors of Bim expression in a mouse embryonic fibroblast model
Published in Bioorganic chemistry (01-03-2022)“…[Display omitted] •First example of compounds able to reduce Bim expression levels in a mouse embryonic fibroblast model.•Novel analogues have been designed…”
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14
A 4-cyano-3-methylisoquinoline inhibitor of Plasmodium falciparum growth targets the sodium efflux pump PfATP4
Published in Scientific reports (16-07-2019)“…We developed a novel series of antimalarial compounds based on a 4-cyano-3-methylisoquinoline. Our lead compound MB14 achieved modest inhibition of the growth…”
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15
Synthesis and biological evaluation of substituted 3-anilino-quinolin-2(1H)-ones as PDK1 inhibitors
Published in Bioorganic & medicinal chemistry (15-07-2014)“…PDK1 is an important regulator of the PI3K/Akt pathway, which has been found frequently activated in a large number of human cancers. Herein we described the…”
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Synthesis and effects of conjugated tocopherol analogues on peptide nucleic acid hybridisation
Published in Organic & biomolecular chemistry (21-10-2013)“…To the N-terminus of a nonamer peptide nucleic acid sequence, H-GCACGACTT-NH2, was attached a number of lipophilic conjugate molecules including three…”
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Pursuing DHDPS: an enzyme of unrealised potential as a novel antibacterial target
Published in MedChemComm (18-09-2019)“…Antibiotic resistance is only set to increase if significant action is not taken to combat the imminent threat of multidrug resistant pathogens. The…”
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Molecular evolution of an oligomeric biocatalyst functioning in lysine biosynthesis
Published in Biophysical reviews (01-04-2018)“…Dihydrodipicolinate synthase (DHDPS) is critical to the production of lysine through the diaminopimelate (DAP) pathway. Elucidation of the function, regulation…”
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Synthesis and biological evaluation of 2-anilino-4-substituted-7H-pyrrolopyrimidines as PDK1 inhibitors
Published in Bioorganic & medicinal chemistry (01-08-2014)“…PDK1, a biological target that has attracted a large amount of attention recently, is responsible for the positive regulation of the PI3K/Akt pathway that is…”
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Efficacy of peptide nucleic acid and selected conjugates against specific cellular pathologies of amyotrophic lateral sclerosis
Published in Bioorganic & medicinal chemistry (01-04-2016)“…[Display omitted] Cellular studies have been undertaken on a nonamer peptide nucleic acid (PNA) sequence, which binds to mRNA encoding superoxide dismutase 1,…”
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