Dr Elena De Vita
Lecturer in Synthetic Biology and Biotechnology
School of Biological and Behavioural Sciences
Queen Mary University of London
Queen Mary University of London
Research
Chemical Biology, Covalent ligands, Induced Proximity, PHOSTACs, Drug Discovery, High throughput screening
Interests
Building on a track-record in covalent drug discovery (The Future of Covalent Drugs, Discovery Report Q3, C&EN, 2022), the De Vita group aims at integrating the advantages of small molecule covalent ligands to advance novel applications in Chemical Biology and Drug Discovery. We are interested in developing novel assays and techniques to discover and optimise small molecule covalent binders for challenging targets, which have potential applications in the rising field of chemically induced proximity. Furthermore, we are constantly on the look for Chemical Biology methodologies that will enable understanding of small molecule and protein function in cells with a translational perspective.Current research lines are focused on PHOSphorylation TArgeting Chimeras (PHOSTACs), a chemically induced proximity approach that employs bifunctional ligands to recruit a protein phosphatase (PP) in the proximity of a phosphorylated protein of interest to drive targeted protein dephosphorylation. Small molecule PHOSTACs will be developed to uncover the role of the unknown phosphoproteome, which still represents the majority of all known phosphosites profiled in humans to date. Mainly focusing on cancer research, we aim to further study the mechanism of action of PHOSTACs and develop ligands with improved pharmacological properties to explore novel therapeutic opportunities in cancer, where protein hyperphosphorylation is a well-known driver of disease.
Publications
2022
Zhang L, Lovell S, De Vita E, Jagtap PKA, Lucy D, Grocin AG, Kjær S, Borg A, Hennig J, Miller AK and Tate EW (2022). A KLK6 Activity-Based Probe Reveals a Role for KLK6 Activity in Pancreatic Cancer Cell Invasion. Journal of the American Chemical Society, American Chemical Society (ACS) vol. 144 (49), 22493-22504. 22-11-2022
Jamshidiha M, Lanyon-Hogg T, Sutherell CL, Craven GB, Tersa M, De Vita E, Brustur D, Pérez-Dorado I, Hassan S, Petracca R, Morgan RM, Sanz-Hernández M, Norman JC, Armstrong A, Mann DJ, Cota E and Tate EW (2022). Identification of the first structurally validated covalent ligands of the small GTPase RAB27A. RSC Medicinal Chemistry, Royal Society of Chemistry (RSC) vol. 13 (2), 150-155. 01-01-2022
Zhang Q, Kounde CS, Mondal M, Greenfield JL, Baker JR, Kotelnikov S, Ignatov M, Tinworth CP, Zhang L, Conole D, De Vita E, Kozakov D, McCluskey A, Harling JD, Fuchter MJ and Tate EW (2022). Light-mediated multi-target protein degradation using arylazopyrazole photoswitchable PROTACs (AP-PROTACs). Chemical Communications, Royal Society of Chemistry (RSC) vol. 58 (78), 10933-10936. 01-01-2022
2021
Yoon H, Triplet EM, Simon WL, Choi C, Kleppe LS, De Vita E, Miller AK and Scarisbrick IA (2021). Blocking Kallikrein 6 promotes developmental myelination. Glia, Wiley vol. 70 (3), 430-450. 09-10-2021
De Vita E, Lucy D and Tate EW (2021). Beyond targeted protein degradation: LD·ATTECs clear cellular lipid droplets. Cell Research, Springer Nature vol. 31 (9), 945-946. 05-08-2021
Lovell S, Zhang L, Kryza T, Neodo A, Bock N, De Vita E, Williams ED, Engelsberger E, Xu C, Bakker AT, Maneiro M, Tanaka RJ, Bevan CL, Clements JA and Tate EW (2021). A Suite of Activity-Based Probes To Dissect the KLK Activome in Drug-Resistant Prostate Cancer. Journal of the American Chemical Society, American Chemical Society (ACS) vol. 143 (23), 8911-8924. 04-06-2021
Santamaria S, Buemi F, Nuti E, Cuffaro D, De Vita E, Tuccinardi T, Rossello A, Howell S, Mehmood S, Snijders AP and de Groot R (2021). Development of a fluorogenic ADAMTS-7 substrate. Journal of Enzyme Inhibition and Medicinal Chemistry, Taylor & Francis vol. 36 (1), 2160-2169. 01-01-2021
Maneiro M, De Vita E, Conole D, Kounde CS, Zhang Q and Tate EW (2021). PROTACs, molecular glues and bifunctionals from bench to bedside: Unlocking the clinical potential of catalytic drugs. 67-190. 01-01-2021
2020
De Vita E (2020). 10 years into the resurgence of covalent drugs. Future Medicinal Chemistry, Future Science Group vol. 13 (2), 193-210. 04-12-2020
De Vita E, Maneiro M and Tate EW (2020). The Missing Link between (Un)druggable and Degradable KRAS. ACS Central Science, American Chemical Society (ACS) vol. 6 (8), 1281-1284. 03-08-2020
2019
De Vita E, Smits N, van den Hurk H, Beck EM, Hewitt J, Baillie G, Russell E, Pannifer A, Hamon V, Morrison A, McElroy SP, Jones P, Ignatenko NA, Gunkel N and Miller AK (2019). Synthesis and Structure‐Activity Relationships of N‐(4‐Benzamidino)‐Oxazolidinones: Potent and Selective Inhibitors of Kallikrein‐Related Peptidase 6. ChemMedChem, Wiley vol. 15 (1), 79-95. 18-11-2019
D'Andrea F, Nuti E, Becherini S, Cuffaro D, Husanu E, Camodeca C, De Vita E, Zocchi MR, Poggi A, D'Arrigo C, Cappello V, Gemmi M, Nencetti S, Chiappe C and Rossello A (2019). Design and Synthesis of Ionic Liquid‐Based Matrix Metalloproteinase Inhibitors (MMPIs): A Simple Approach to Increase Hydrophilicity and to Develop MMPI‐Coated Gold Nanoparticles. ChemMedChem, Wiley vol. 14 (6), 686-698. 14-02-2019
2018
De Vita E, Schüler P, Lovell S, Lohbeck J, Kullmann S, Rabinovich E, Sananes A, Heßling B, Hamon V, Papo N, Hess J, Tate EW, Gunkel N and Miller AK (2018). Depsipeptides Featuring a Neutral P1 Are Potent Inhibitors of Kallikrein-Related Peptidase 6 with On-Target Cellular Activity. Journal of Medicinal Chemistry, American Chemical Society (ACS) vol. 61 (19), 8859-8874. 13-09-2018
Sananes A, Cohen I, Shahar A, Hockla A, De Vita E, Miller AK, Radisky ES and Papo N (2018). A potent, proteolysis-resistant inhibitor of kallikrein-related peptidase 6 (KLK6) for cancer therapy, developed by combinatorial engineering. Journal of Biological Chemistry, Elsevier vol. 293 (33), 12663-12680. 22-06-2018
Longuespée R, Wefers AK, De Vita E, Miller AK, Reuss DE, Wick W, Herold-Mende C, Kriegsmann M, Schirmacher P, von Deimling A and Pusch S (2018). Rapid detection of 2-hydroxyglutarate in frozen sections of IDH mutant tumors by MALDI-TOF mass spectrometry. Acta Neuropathologica Communications, Springer Nature vol. 6 (1) 02-03-2018
Grants
Grants of specific relevance to the Centre for Molecular Cell BiologyDevelopment of covalent probes for protein phosphatase 1 (PP1)Elena De Vita
£11,000 Royal Society (31-03-2024 - 30-03-2026)
Covalent PHOSTACs for targeted protein dephosphorylation against K-Ras driven tumoursElena De Vita
£69,401 Royal Society (01-03-2024 - 31-08-2025)