Serafini Lab
Publications
Preprints
2025
-
Full List of Publications
The full list of publications can be found on Google Scholar.
Selected Publications
1. Indolequinone-based hypoxia-activated PROTACs (HAP-TACs) selectively degrade BRD4 in hypoxic cancer cells.
Serafini M, Twigger SA, Delfas G, Mallerman M, Bailey EP, Calder EDD, Hammond EM, Conway SJ.
J Am Chem Soc. 2025, 147, 36352-36364.
DOI: 10.1021/jacs.5c10240
Preprint: 10.26434/chemrxiv-2025-hm6l5
2. Orthogonal IMiD-degron pairs induce selective protein degradation in cells.
Brennan PJ, Saunders RE, Spanou M, Singleton SE, Serafini M, Sun L, Heger GP, Konopacka A, Beveridge RD, Taylor CC, DePaola P 4th, Gordon L, Bunally SB, Saudemont A, Benowitz AB, Martinez-Fleites C, Schmitt DL, Damoiseaux R, Queisser MA, An H, Deane CM, Hann MM, Brayshaw LL, Conway SJ.
ACS Chem Biol. 2025, 20, 2827-2843.
DOI: 10.1021/acschembio.5c00751
Preprint: 10.1101/2024.03.15.585309
3. The multicomponent Passerini reaction as a means of accessing diversity in structure, activity and properties: Soft and hard vanilloid/cannabinoid modulators.
Lamberti A,# Serafini M,# Aprile S, Bhela IP, Goutsiou G, Pessolano E, Fernandez-Ballester G, Ferrer-Montiel A, Di Martino RMC, Fernandez-Carvajal A, Pirali T.
Eur J Med Chem. 2024, 279,116845. (#equal contribution)

4. Mutate and conjugate: A new method for rapid in cell validation of epigenetic targets.
Thomas AM, Serafini M, Grant EK, Coombs EAJ, Bluck JP, Schiedel M, McDonough MA, Reynolds JK, [...], Biggin PC, Duarte F, Milne TA, Bush JT, Conway SJ.
ACS Chem Biol 2023, 18, 2405–2417.
DOI: 10.1021/acschembio.3c00437
Preprint: 10.26434/chemrxiv-2023-8qnvr

5. A Versatile and Sustainable Multicomponent Platform for the Synthesis of Protein Degraders: Proof-of-Concept Application to BRD4-Degrading PROTACs.
Bhela IP, Ranza A, Balestrero FC, Serafini M, Aprile S, Di Martino RMC, Condorelli F, Pirali T. J Med Chem. 2022, 65, 15282–15299.

6. An Unexpected Deuterium-Induced Metabolic Switch in Doxophylline.
Aprile S,# Colombo G,# Serafini M,# Di Paola R, [...] Pirali T.
ACS Med Chem Lett. 2022, 13, 1278-1285. (#equal contribution)
DOI: 10.1021/acsmedchemlett.2c00166
(Erratum in 10.1021/acsmedchemlett.3c00497).

7. What's in a Name? Drug Nomenclature and Medicinal Chemistry Trends using INN Publications.
Serafini M, Cargnin S, Massarotti A, Tron GC, Pirali T, Genazzani AA.
J Med Chem. 2021, 64, 4410-4429.

8. Store-Operated Calcium Entry as a Therapeutic Target in Acute Pancreatitis: Discovery and Development of Drug-Like SOCE Inhibitors.
Serafini M, Cordero-Sanchez C, Di Paola R, Bhela IP, Aprile S, Purghè B, Fusco R, Cuzzocrea S, Genazzani AA, Riva B, Pirali T.
J Med Chem. 2020, 63, 14761-14779.

9. Discovery of Highly Potent Benzimidazole Derivatives as Indoleamine 2,3-Dioxygenase-1 (IDO1) Inhibitors: From Structure-Based Virtual Screening to in Vivo Pharmacodynamic Activity.
Serafini M, Torre E, Aprile S, Grosso ED, Gesù A, Griglio A, Colombo G, Travelli C, Paiella S, Adamo A, Orecchini E, Coletti A, Pallotta MT, Ugel S, Massarotti A, Pirali T, Fallarini S.
J Med Chem. 2020, 63, 3047-3065.

10. Essential Medicinal Chemistry of Essential Medicines.
Serafini M, Cargnin S, Massarotti A, Pirali T, Genazzani AA.
J Med Chem. 2020, 63, 10170-10187.

11. Applications of Deuterium in Medicinal Chemistry.
Pirali T, Serafini M, Cargnin S, Genazzani AA.
J Med Chem. 2019, 62, 5276-5297.

12. Targeting Transient Receptor Potential Vanilloid 1 (TRPV1) Channel Softly: The Discovery of Passerini Adducts as a Topical Treatment for Inflammatory Skin Disorders. Serafini M, Griglio A, Aprile S, Seiti F, Travelli C, Pattarino F, Grosa G, Sorba G, [...] Devesa I, Fernandez-Carvajal A, Pirali T, Ferrer-Montiel A.
J Med Chem. 2018, 61, :4436-4455.


