Triazole-Based Thiamine Analogues as Inhibitors of Thiamine Pyrophosphate-Dependent Enzymes: 1,3-Dicarboxylate for Metal Binding
TCS Ho, AHY Chan, FJ Leeper
– ACS Omega
(2024)
9,
42245
(DOI: 10.1021/acsomega.4c04594)
Structural and Functional Basis of GenB2 Isomerase Activity from Gentamicin Biosynthesis
GSD Oliveira, P Dos S Bury, F Huang, Y Li, NCD Araújo, J Zhou, Y Sun, FJ Leeper, PF Leadlay, MVB Dias
– ACS Chem Biol
(2024)
19,
2002
(DOI: 10.1021/acschembio.4c00334)
Evaluation of ketoclomazone and its analogues as inhibitors of 1-deoxy-d-xylulose 5-phosphate synthases and other thiamine diphosphate (ThDP)-dependent enzymes.
AHY Chan, TCS Ho, I Fathoni, R Hamid, AKH Hirsch, KJ Saliba, FJ Leeper
– RSC Medicinal Chemistry
(2024)
15,
1773
(DOI: 10.1039/d4md00083h)
Thiamine analogues featuring amino-oxetanes as potent and selective inhibitors of pyruvate dehydrogenase
AHY Chan, TCS Ho, FJ Leeper
– Bioorg Med Chem Lett
(2023)
98,
129571
(DOI: 10.1016/j.bmcl.2023.129571)
Open-chain thiamine analogues as potent inhibitors of thiamine pyrophosphate (TPP)-dependent enzymes
AHY Chan, TCS Ho, FJ Leeper
– Organic & biomolecular chemistry
(2023)
21,
6531
(DOI: 10.1039/d3ob00884c)
Design of thiamine analogues for inhibition of thiamine diphosphate (ThDP)-dependent enzymes: Systematic investigation through Scaffold-Hopping and C2-Functionalisation.
AHY Chan, TCS Ho, R Irfan, RAA Hamid, ES Rudge, A Iqbal, A Turner, AKH Hirsch, FJ Leeper
– Bioorganic Chemistry
(2023)
138,
106602
(DOI: 10.1016/j.bioorg.2023.106602)
Biosynthesis of Antifungal Solanimycin May Involve an Iterative Nonribosomal Peptide Synthetase Module.
AC Murphy, M Corney, RE Monson, MA Matilla, GPC Salmond, FJ Leeper
– ACS Chemical Biology
(2023)
18,
1148
(DOI: 10.1021/acschembio.2c00947)
Inhibition of Thiamine Diphosphate-Dependent Enzymes by Triazole-Based Thiamine Analogues.
AHY Chan, TCS Ho, I Fathoni, R Pope, KJ Saliba, FJ Leeper
– ACS medicinal chemistry letters
(2023)
14,
621
Preclinical PET Imaging of Tumor Cell Death following Therapy Using Gallium-68-Labeled C2Am
F Bulat, F Hesse, B Attili, C Solanki, IA Mendichovszky, F Aigbirhio, FJ Leeper, KM Brindle, AA Neves
– Cancers (Basel)
(2023)
15,
1564
(DOI: 10.3390/cancers15051564)
Furan-based Thiamine Antagonists for Pyruvate Dehydrogenase: SAR Investigation, Biochemical Evaluation and Computational Analysis
F Leeper, AHY Chan, TCS Ho, DR Parle
– Organic & biomolecular chemistry
(2023)
21,
1755
(DOI: 10.1039/D2OB02272A)
Synthesis of pyrrothiamine, a novel thiamine analogue, and evaluation of derivatives as potent and selective inhibitors of pyruvate dehydrogenase.
FJ Leeper, AHY Chan, TCS Ho, K Agyei-Owusu
– Organic & biomolecular chemistry
(2022)
64,
8855
(DOI: 10.1039/D2OB01819E)
Solanimycin: Biosynthesis and Distribution of a New Antifungal Antibiotic Regulated by Two Quorum-Sensing Systems.
MA Matilla, RE Monson, A Murphy, M Schicketanz, A Rawlinson, C Duncan, J Mata, F Leeper, GPC Salmond
– mBio
(2022)
13,
e0247222
(DOI: 10.1128/mbio.02472-22)
Enzyme-Catalyzed Spiroacetal Formation in Polyketide Antibiotic Biosynthesis
O Bilyk, GS Oliveira, RM de Angelo, MO Almeida, KM Honório, FJ Leeper, MVB Dias, PF Leadlay
– Journal of the American Chemical Society
(2022)
144,
14555
(DOI: 10.1021/jacs.2c03313)
Metabolic Glycan Labelling of Cancer Cells using Variably Acetylated Monosaccharides
DR Parle, F Bulat, S Fouad, H Zecchini, KM Brindle, AA Neves, FJ Leeper
– Bioconjugate chemistry
(2022)
33,
1467
Thiamine analogues as inhibitors of pyruvate dehydrogenase and discovery of a thiamine analogue with non-thiamine related antiplasmodial activity
AHY Chan, I Fathoni, TCS Ho, KJ Saliba, FJ Leeper
– RSC Medicinal Chemistry
(2022)
13,
817
(DOI: 10.1039/d2md00085g)
Prodrugs of pyrophosphates and bisphosphonates: disguising phosphorus oxyanions.
FJ Leeper, ES Rudge, AHY Chan
– RSC Med Chem
(2022)
13,
375
(DOI: 10.1039/D1MD00297J)
Mechanistic Insights into Dideoxygenation in Gentamicin Biosynthesis
S Li, PD Santos Bury, F Huang, J Guo, G Sun, A Reva, C Huang, X Jian, Y Li, J Zhou, Z Deng, FJ Leeper, PF Leadlay, MVB Dias, Y Sun
– ACS Catalysis
(2021)
11,
12274
(DOI: 10.1021/acscatal.1c03508)
Revision in the first steps of the biosynthesis of the red antibiotic prodigiosin: Use of a synthetic thioester to validate a new intermediate
M Couturier, HD Bhalara, RE Monson, GPC Salmond, FJ Leeper
– RSC chemical biology
(2021)
2,
551
(DOI: 10.1039/d0cb00173b)
18F-C2Am: a targeted imaging agent for detecting tumor cell death in vivo using positron emission tomography
F Bulat, F Hesse, D-E Hu, S Ros, W-H Connor, B Xie, B Attili, D Soloviev, F Aigbirhio, F Leeper, K Brindle, A Neves
– EJNMMI Research
(2020)
(DOI: 10.1186/s13550-020-00738-7)