Destabilizers of the thymidylate synthase homodimer accelerate its proteasomal degradation and inhibit cancer growth

Constantino Luca; Stefania Ferrari; Matteo Santucci; Outi MH Salo-Ahen; Emanuele Carosati; Silvia Franchini; Angela Lauriola; Cecilia Pozzi; Matteo Trande; Gozzi Gaia; Puneet Saxena; Giuseppe Cannazza; Lorena Losi; Daniela Cardinale; Alberto Venturelli; Antonio Quotadamo; Pasquale Linciano; Tagliazucchi Lorenzo; Maria Gaetana Moshella; Remo Guerrini; Salvatore Pacifico; Rosaria Luciani; Filippo Genovese; Henrich Stefan; Alboni Silvia; Nuno Santarem; Anabela Cordeiro-da-Silva; Elisa Giovannetti; Godefridus Peters; Paolo Pinton; Alessandro Rimessi; Gabriele Cruciani; Robert Stroud; Rebecca C. Wade; Stefano Mangani; Gaetano Marverti; Domenico D'Arca; Glauco Ponterini; Maria Paola Costi

doi:10.7554/eLife.73862

Destabilizers of the thymidylate synthase homodimer accelerate its proteasomal degradation and inhibit cancer growth

Constantino Luca, Stefania Ferrari, Matteo Santucci, Outi MH Salo-Ahen, Emanuele Carosati, Silvia Franchini, Angela Lauriola, Cecilia Pozzi, Matteo Trande, Gozzi Gaia, Puneet Saxena, Giuseppe Cannazza, Lorena Losi, Daniela Cardinale, Alberto Venturelli, Antonio Quotadamo, Pasquale Linciano, Tagliazucchi Lorenzo, Maria Gaetana Moshella, Remo GuerriniSalvatore Pacifico, Rosaria Luciani, Filippo Genovese, Henrich Stefan, Alboni Silvia, Nuno Santarem, Anabela Cordeiro-da-Silva, Elisa Giovannetti, Godefridus Peters, Paolo Pinton, Alessandro Rimessi, Gabriele Cruciani, Robert Stroud, Rebecca C. Wade, Stefano Mangani, Gaetano Marverti, Domenico D'Arca^*, Glauco Ponterini^*, Maria Paola Costi^*

^*Corresponding author for this work

Pharmacy

Research output: Contribution to journal › Article › Scientific › peer-review

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Original language	English
Article number	e73862
Journal	eLife
Volume	11
Issue number	e73862
DOIs	https://doi.org/10.7554/eLife.73862
Publication status	Published - 7 Dec 2022
MoE publication type	A1 Journal article-refereed

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This output contributes to the following UN Sustainable Development Goals (SDGs)

Access to Document

10.7554/eLife.73862

Destabilizers of the thymidylate synthaseAccepted author manuscript, 6.67 MBLicence: CC BY

https://urn.fi/URN:NBN:fi-fe2023022228186

Cite this

Luca, C., Ferrari, S., Santucci, M., Salo-Ahen, O. MH., Carosati, E., Franchini, S., Lauriola, A., Pozzi, C., Trande, M., Gaia, G., Saxena, P., Cannazza, G., Losi, L., Cardinale, D., Venturelli, A., Quotadamo, A., Linciano, P., Lorenzo, T., Moshella, M. G., ... Costi, M. P. (2022). Destabilizers of the thymidylate synthase homodimer accelerate its proteasomal degradation and inhibit cancer growth. eLife, 11(e73862), Article e73862. https://doi.org/10.7554/eLife.73862

@article{dce0a05a89a141c0849298a31519865f,

title = "Destabilizers of the thymidylate synthase homodimer accelerate its proteasomal degradation and inhibit cancer growth",

keywords = "thymidylate synthase, homodimer, protein-protein interface, Anticancer drug resistance, drug discovery, medicinal chemistry, Inhibitor",

author = "Constantino Luca and Stefania Ferrari and Matteo Santucci and Salo-Ahen, {Outi MH} and Emanuele Carosati and Silvia Franchini and Angela Lauriola and Cecilia Pozzi and Matteo Trande and Gozzi Gaia and Puneet Saxena and Giuseppe Cannazza and Lorena Losi and Daniela Cardinale and Alberto Venturelli and Antonio Quotadamo and Pasquale Linciano and Tagliazucchi Lorenzo and Moshella, {Maria Gaetana} and Remo Guerrini and Salvatore Pacifico and Rosaria Luciani and Filippo Genovese and Henrich Stefan and Alboni Silvia and Nuno Santarem and Anabela Cordeiro-da-Silva and Elisa Giovannetti and Godefridus Peters and Paolo Pinton and Alessandro Rimessi and Gabriele Cruciani and Robert Stroud and Wade, {Rebecca C.} and Stefano Mangani and Gaetano Marverti and Domenico D'Arca and Glauco Ponterini and Costi, {Maria Paola}",

year = "2022",

month = dec,

day = "7",

doi = "10.7554/eLife.73862",

language = "English",

volume = "11",

journal = "eLife",

issn = "2050-084X",

publisher = "eLife Sciences Publications",

number = "e73862",

}

Luca, C, Ferrari, S, Santucci, M, Salo-Ahen, OMH, Carosati, E, Franchini, S, Lauriola, A, Pozzi, C, Trande, M, Gaia, G, Saxena, P, Cannazza, G, Losi, L, Cardinale, D, Venturelli, A, Quotadamo, A, Linciano, P, Lorenzo, T, Moshella, MG, Guerrini, R, Pacifico, S, Luciani, R, Genovese, F, Stefan, H, Silvia, A, Santarem, N, Cordeiro-da-Silva, A, Giovannetti, E, Peters, G, Pinton, P, Rimessi, A, Cruciani, G, Stroud, R, Wade, RC, Mangani, S, Marverti, G, D'Arca, D, Ponterini, G & Costi, MP 2022, 'Destabilizers of the thymidylate synthase homodimer accelerate its proteasomal degradation and inhibit cancer growth', eLife, vol. 11, no. e73862, e73862. https://doi.org/10.7554/eLife.73862

TY - JOUR

T1 - Destabilizers of the thymidylate synthase homodimer accelerate its proteasomal degradation and inhibit cancer growth

AU - Luca, Constantino

AU - Ferrari, Stefania

AU - Santucci, Matteo

AU - Salo-Ahen, Outi MH

AU - Carosati, Emanuele

AU - Franchini, Silvia

AU - Lauriola, Angela

AU - Pozzi, Cecilia

AU - Trande, Matteo

AU - Gaia, Gozzi

AU - Saxena, Puneet

AU - Cannazza, Giuseppe

AU - Losi, Lorena

AU - Cardinale, Daniela

AU - Venturelli, Alberto

AU - Quotadamo, Antonio

AU - Linciano, Pasquale

AU - Lorenzo, Tagliazucchi

AU - Moshella, Maria Gaetana

AU - Guerrini, Remo

AU - Pacifico, Salvatore

AU - Luciani, Rosaria

AU - Genovese, Filippo

AU - Stefan, Henrich

AU - Silvia, Alboni

AU - Santarem, Nuno

AU - Cordeiro-da-Silva, Anabela

AU - Giovannetti, Elisa

AU - Peters, Godefridus

AU - Pinton, Paolo

AU - Rimessi, Alessandro

AU - Cruciani, Gabriele

AU - Stroud, Robert

AU - Wade, Rebecca C.

AU - Mangani, Stefano

AU - Marverti, Gaetano

AU - D'Arca, Domenico

AU - Ponterini, Glauco

AU - Costi, Maria Paola

PY - 2022/12/7

Y1 - 2022/12/7

KW - thymidylate synthase

KW - homodimer

KW - protein-protein interface

KW - Anticancer drug resistance

KW - drug discovery

KW - medicinal chemistry

KW - Inhibitor

U2 - 10.7554/eLife.73862

DO - 10.7554/eLife.73862

M3 - Article

SN - 2050-084X

VL - 11

JO - eLife

JF - eLife

IS - e73862

M1 - e73862

ER -