PhD, Chemical Engineer
Laurent Trembleau received his undergraduate education at the "Institut Universitaire de Technologie" of Orléans (France) and obtained a "Diplôme d'Ingénieur" in Fine Chemistry and Engineering, and a "Diplôme d'Etudes Approfondies" (DEA) in Chemistry at the "Institut National des Sciences Appliquées" of Rouen, France (1993). In 1994, he moved to Louvain-la-Neuve (Belgium) to undertake a PhD in the group of Professor Léon Ghosez. His work, financed by Rhône-Poulenc Rorer, involved the development of new Diels-Alder reactions and methods towards the synthesis of ottelione A, a natural product inhibitor of tubulin polymerisation. In 2001, he moved to the Scripps Research Institute (USA) for a 2-year post-doctoral position in the group of Professor Julius Rebek where he designed a water-soluble receptor of acetylcholine, described the helical conformation of alkanes in synthetic receptors, and was involved in the synthesis of oxazole-based macrocycles. In 2004, he did a short post-doctoral position in the group of Dr Simon Webb, where he worked on the synthesis of novel lipids designed to mimic cell adhesion molecules. At the end of 2004, he accepted a Lectureship in Medicinal Chemistry at the University of Aberdeen, where he is currently studying the total synthesis and SAR of bioactive molecules, the development of organic catalysts and novel methods for application in Organic Synthesis and Medicinal Chemistry.
We are interested in the development of efficient solution and solid-phase syntheses of peptides. We have recently optimized a repetitive procedure that contains features from both solid-phase and solution-phase methods, making it an effective method for the synthesis of short peptides. We are currently modifying resins to improve the synthesis of "difficult peptide sequences".
1) We are investigating the properties of novel organocatalysts that mimic the residues of enzymes involved in catalysis.
2) We are developing new foldamers with the aim to bind anions (especially fluoride) in aqueous media.
2) Medicinal Chemistry
Inhibitors of Protein-Protein Interactions (PPI): This project involves the design and synthesis of inhibitors of protein-protein interactions. We are developing macrocyclic molecules possessing large surface areas in the aim to inhibit specific protein-protein interactions (in collaboration with Prof M. Jaspars, Dr W. Houssen, and Prof J. Naismith).
Funding and Grants
- European Commission "New Chemical Biology for Tayloring Novel Therapeutics - PDRA (2014-2019) (with Prof Marcel Jaspars and Prof Jim Naismith)
- Scottish Enterprise "Validation of the Commercial Potential of Diversity-Oriented Biosynthesis to Create Novel Macrocycle Drugs" - (2015-2016) with Prof Marcel Jaspars, Prof Jim Naismith and Dr Wael Houssen.
Dr Trembleau teaches in the following courses
- CM1022 Elements of Chemistry 1 (2 lectures)
- CM2512 Organic and Biological Chemistry (8 lectures)
- CM3521 Organic and Biological Chemistry (12 lectures)
- CM4516 Honours/Advanced Chemistry (12 lectures)
- CM5003 MChem Chemistry Applications (10 lectures)
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Design, Synthesis, and Biological Evaluation of Indole-2-carboxamides as Potential Multi-Target Antiproliferative AgentsPharmaceuticals, vol. 16, no. 7, 1039Contributions to Journals: Articles
Design, synthesis, apoptotic, and antiproliferative effects of 5-chloro-3- (2-methoxyvinyl)-indole-2-carboxamides and pyrido[3,4-b]indol-1-ones as potent EGFRWT/EGFRT790M inhibitorsJournal of enzyme inhibition and medicinal chemistry, vol. 38, no. 1, 2218602Contributions to Journals: Articles
Discovery of new 5-substituted-indole-2-carboxamides as dual epidermal growth factor receptor (EGFR)/cyclin dependent kinase-2 (CDK2) inhibitors with potent antiproliferative actionRSC Medicinal Chemistry, vol. 14, no. 4, pp. 734-744Contributions to Journals: Articles
Design, Synthesis, and Antiproliferative Activity of New 5-Chloro-indole-2-carboxylate and Pyrrolo[3,4-b]indol-3-one Derivatives as Potent Inhibitors of EGFRT790M/BRAFV600E PathwaysMolecules, vol. 28, no. 3, 1269Contributions to Journals: Articles
A ribosomally synthesised and post-translationally modified peptide containing a β-enamino acid and a macrocyclic motifNature Communications, vol. 13, no. 1, 5044Contributions to Journals: Articles
Synthesis and Biological Evaluation of Indole-2-Carboxamides with Potent Apoptotic Antiproliferative Activity as EGFR/CDK2 Dual InhibitorsPharmaceuticals, vol. 15, no. 8, 1006Contributions to Journals: Articles
Optimization and SAR investigation of novel 2,3-dihydropyrazino[1,2-a]indole-1,4-dione derivatives as EGFR and BRAFV600E dual inhibitors with potent antiproliferative and antioxidant activitiesBioorganic Chemistry, vol. 120, 105616Contributions to Journals: Articles
Characterization of a class II ketol-acid reductoisomerase from Mycobacterium tuberculosisRSC Advances, vol. 12, no. 17, pp. 10540-10544Contributions to Journals: Articles
Discovery of novel oxazole-based macrocycles as anti-coronaviral agents targeting SARS-CoV-2 main proteaseBioorganic Chemistry, vol. 116, 105363Contributions to Journals: Articles
Novel 1,5-diaryl pyrazole-3-carboxamides as selective COX-2/sEH inhibitors with analgesic, anti-inflammatory, and lower cardiotoxicity effectsBioorganic Chemistry, vol. 116, 105302Contributions to Journals: Articles