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

Author

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

Subjects
Biochemistry and Cell Biology, Biomedical and Clinical Sciences, Oncology and Carcinogenesis, Biological Sciences, Cancer, Orphan Drug, Rare Diseases, Biotechnology, Development of treatments and therapeutic interventions, 5.1 Pharmaceuticals, Female, Animals, Mice, Humans, Binding Sites, Thymidylate Synthase, Fluorouracil, Ovarian Neoplasms, Enzyme Inhibitors, thymidylate synthase, protein dimer destabilizers, cancer growth inhibition, proteasomal degradation, enzyme dissociative inhibition mechanism, target engagement, Human, biochemistry, cancer biology, chemical biology, human, Biological sciences, Biomedical and clinical sciences, Health sciences
Abstract

Drugs that target human thymidylate synthase (hTS), a dimeric enzyme, are widely used in anticancer therapy. However, treatment with classical substrate-site-directed TS inhibitors induces over-expression of this protein and development of drug resistance. We thus pursued an alternative strategy that led us to the discovery of TS-dimer destabilizers. These compounds bind at the monomer-monomer interface and shift the dimerization equilibrium of both the recombinant and the intracellular protein toward the inactive monomers. A structural, spectroscopic, and kinetic investigation has provided evidence and quantitative information on the effects of the interaction of these small molecules with hTS. Focusing on the best among them, E7, we have shown that it inhibits hTS in cancer cells and accelerates its proteasomal degradation, thus causing a decrease in the enzyme intracellular level. E7 also showed a superior anticancer profile to fluorouracil in a mouse model of human pancreatic and ovarian cancer. Thus, over sixty years after the discovery of the first TS prodrug inhibitor, fluorouracil, E7 breaks the link between TS inhibition and enhanced expression in response, providing a strategy to fight drug-resistant cancers.

Published
2022

4. Cancer: A Complex Problem Requiring Interdisciplinary Research

Author

Yazdanpanah, Niloufar, Dochy, Filip, Darmstadt, Gary L., Peters, Godefridus J., Tsitlakidis, Abraham, Aifantis, Elias C., Cerda, Artemi, Comini, Elisabetta, Brand, Serge, Gupta, Manoj, Cheson, Bruce D., Thomas, Sabu, Tanzer, Michael, Weiskirchen, Ralf, Bella, Federico, Fereshtehnejad, Seyed-Mohammad, Nikita, Konstantina, Ali, Imran, Kato, Koichi, Poggi, Alessandro, Jon, Ernest Chua Kian, Rao, Idupulapati M., Tao, Xiaoming, He, Ji-Huan, Rao, Lingamallu Jagan Mohan, Leemans, Alexander, Pomponio, Alessio, Hernandez, Alfredo Martínez, Ahmadieh, Hamid, Sahraian, Mohammad Ali, Kelishadi, Roya, Thongboonkerd, Visith, Bahinipati, Seema, Toi, Masakazu, von Herrath, Matthias, Sellke, Frank, Sherwood, Steven, Perry, George, Nieto, Juan J., Gupta, Sudhir, Dorigo, Tommaso, Mobasher, Bahram, Ochs, Hans D., Rezaei, Nima, Rezaei, Nima, Series Editor, Ahmed, Atif A., Editorial Board Member, Aguiar, Rodrigo, Editorial Board Member, Ambrosio, Maria R., Editorial Board Member, Artac, Mehmet, Editorial Board Member, Augustine, Tanya N., Editorial Board Member, Bambauer, Rolf, Editorial Board Member, Bhat, Ajaz Ahmad, Editorial Board Member, Bertolaccini, Luca, Editorial Board Member, Bianchini, Chiara, Editorial Board Member, Cavic, Milena, Editorial Board Member, Chakrabarti, Sakti, Editorial Board Member, Cho, William C. S., Editorial Board Member, Czarnecka, Anna M., Editorial Board Member, Domingues, Cátia, Editorial Board Member, Eşkazan, A. Emre, Editorial Board Member, Fares, Jawad, Editorial Board Member, Fonseca Alves, Carlos E., Editorial Board Member, Fru, Pascaline, Editorial Board Member, Da Gama Duarte, Jessica, Editorial Board Member, García, Mónica C., Editorial Board Member, Gener, Melissa A.H., Editorial Board Member, Estrada Guadarrama, José Antonio, Editorial Board Member, Hargadon, Kristian M., Editorial Board Member, Holvoet, Paul, Editorial Board Member, Jurisic, Vladimir, Editorial Board Member, Kabir, Yearul, Editorial Board Member, Katsila, Theodora, Editorial Board Member, Kleeff, Jorg, Editorial Board Member, Liang, Chao, Editorial Board Member, Tan, Mei Lan, Editorial Board Member, Li, Weijie, Editorial Board Member, Prado López, Sonia, Editorial Board Member, Macha, Muzafar A., Editorial Board Member, Malara, Natalia, Editorial Board Member, Orhan, Adile, Editorial Board Member, Prado-Garcia, Heriberto, Editorial Board Member, Pérez-Velázquez, Judith, Editorial Board Member, Rashed, Wafaa M., Editorial Board Member, Sanguedolce, Francesca, Editorial Board Member, Sorrentino, Rosalinda, Editorial Board Member, Shubina, Irina Zh., Editorial Board Member, de Araujo, Heloisa Sobreiro Selistre, Editorial Board Member, Torres-Suárez, Ana Isabel, Editorial Board Member, Włodarczyk, Jakub, Editorial Board Member, Yeong, Joe Poh Sheng, Editorial Board Member, Toscano, Marta A., Editorial Board Member, Wong, Tak-Wah, Editorial Board Member, Yin, Jun, Editorial Board Member, and Yu, Bin, Editorial Board Member

Published
2023
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5. Pegylated nanoliposomal cisplatin ameliorates chemotherapy-induced peripheral neuropathy

Author

Moetamani-Ahmadi, Mehrdad, Mahmoud Ahmadzadeh, Amir, Alaei, Maryam, Zafari, Nima, Negahbanzaferanloo, Zhara, Pourbagher-Shahri, Ali Mohammad, Forouzanfar, Fatemeh, Fiuji, Hamid, Mahaki, Hanie, Khazaei, Majid, Gataa, Ibrahim Saeed, Ferns, Gordon A., Peters, Godefridus J., Batra, Jyotsna, Lam, Alfred King-yin, Giovannetti, Elisa, TanzadehPanah, Hamid, and Avan, Amir

Published
2024
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9. Correction to: Cancer: A Complex Problem Requiring Interdisciplinary Research

Author

Yazdanpanah, Niloufar, primary, Dochy, Filip, additional, Darmstadt, Gary L., additional, Peters, Godefridus J., additional, Tsitlakidis, Abraham, additional, Aifantis, Elias C., additional, Cerda, Artemi, additional, Comini, Elisabetta, additional, Brand, Serge, additional, Gupta, Manoj, additional, Cheson, Bruce D., additional, Thomas, Sabu, additional, Tanzer, Michael, additional, Weiskirchen, Ralf, additional, Bella, Federico, additional, Fereshtehnejad, Seyed-Mohammad, additional, Nikita, Konstantina, additional, Ali, Imran, additional, Kato, Koichi, additional, Poggi, Alessandro, additional, Jon, Ernest Chua Kian, additional, Rao, Idupulapati M., additional, Tao, Xiaoming, additional, He, Ji-Huan, additional, Rao, Lingamallu Jagan Mohan, additional, Leemans, Alexander, additional, Pomponio, Alessio, additional, Hernandez, Alfredo Martínez, additional, Ahmadieh, Hamid, additional, Sahraian, Mohammad Ali, additional, Kelishadi, Roya, additional, Thongboonkerd, Visith, additional, Bahinipati, Seema, additional, Toi, Masakazu, additional, von Herrath, Matthias, additional, Sellke, Frank, additional, Sherwood, Steven, additional, Perry, George, additional, Nieto, Juan J., additional, Gupta, Sudhir, additional, Dorigo, Tommaso, additional, Mobasher, Bahram, additional, Ochs, Hans D., additional, and Rezaei, Nima, additional

Published
2023
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14. G-Protein Signaling Modulator 2 as a Potential Biomarker in Colorectal Cancer: Integrative Analysis Using Genetic Profiling and Pan-Cancer Studies

Author

Kadhim, Doaa Jawad, primary, Azari, Hanieh, additional, Sokhangouy, Saeideh Khorshid, additional, Hassanian, Seyed Mahdi, additional, Alshekarchi, Hawraa Ibrahim, additional, Goshayeshi, Ladan, additional, Goshayeshi, Lena, additional, Abbaszadegan, Mohammad Reza, additional, Khojasteh-Leylakoohi, Fatemeh, additional, Khazaei, Majid, additional, Gataa, Ibrahim Saeed, additional, Peters, Godefridus J., additional, A. Ferns, Gordon, additional, Batra, Jyotsna, additional, Lam, Alfred King-Yin, additional, Giovannetti, Elisa, additional, and Avan, Amir, additional

Published
2024
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15. Nucleo(s)tide metabolism as basis for drug development; the Anne Simmonds award lecture.

Author

Peters, Godefridus J.

Subjects
*DRUG development, *THERAPEUTICS, *METHOTREXATE, *PHARMACEUTICAL chemistry, *DRUG metabolism
Abstract

AbstractAberrant metabolism of purines and pyrimidines led to development of drugs for treatment of various diseases, such as inflammatory, neurological, cardiovascular, viral infections and cancer. Purine and Pyrimidine Symposia are characterized by close interactions, leading to extensive cross-fertilization on methodology and translating not only from bench-to-bedside, but also between various disciplines such as medicinal chemistry, pharmacology, oncology, virology, rheumatology, biochemistry, pediatrics, cardiology, surgery and immunology. This background was fundamental in our studies on how to optimize application of existing drugs (5-fluorouracil [5FU], thiopurines, antifolates such as methotrexate) but also to support development of novel drugs such as gemcitabine, novel antifolates, S-1, TAS-102 and fluorocyclopentenylcytosine. Knowledge of their metabolism helped to design rational combinations such as of gemcitabine with cisplatin, one of the most widely used drug combinations for various cancers. The combination of 5FU with uridine, led to the development of triacetyluridine registered for emergency treatment of patients with lethal 5FU toxicity. Mechanisms of action were studied by careful analysis of their metabolism, using classical enzyme assays with radioactive precursors and HPLC analysis. Drug metabolism moved from manually operated HPLC systems with UV-detection for peak identification and paper rolls for quantification, to computer-operated HPLC with automatic multi-wavelength and fluorometric peak detection and more recently to ultrasensitive, highly specific mass-spectrometry-based systems. Some aspects, however, never changed; careful analysis of the results and being prepared for the unexpected. The latter actually led to the most interesting results. Investigation of (nucleoside/nucleotide) metabolism remains an exciting field of research. [ABSTRACT FROM AUTHOR]

Published
2024
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16. Exploring Splicing Modulation as an Innovative Approach to Combat Pancreatic Cancer: SF3B1 Emerges as a Prognostic Indicator and Therapeutic Target.

Author

Sciarrillo, Rocco, Terrana, Francesca, Comandatore, Annalisa, Supadmanaba, I. Gede Putu, Bing Wang, El Hassouni, Btissame, Mantini, Giulia, Jansen, Gerrit, Avan, Amir, Carbone, Daniela, Diana, Patrizia, Peters, Godefridus J., Morelli, Luca, Cloos, Jacqueline, Assaraf, Yehuda G., and Giovannetti, Elisa

Published
2024
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17. Correction to: Cancer: A Complex Problem Requiring Interdisciplinary Research

Author

Yazdanpanah, Niloufar, Dochy, Filip, Darmstadt, Gary L., Peters, Godefridus J., Tsitlakidis, Abraham, Aifantis, Elias C., Cerda, Artemi, Comini, Elisabetta, Brand, Serge, Gupta, Manoj, Cheson, Bruce D., Thomas, Sabu, Tanzer, Michael, Weiskirchen, Ralf, Bella, Federico, Fereshtehnejad, Seyed-Mohammad, Nikita, Konstantina, Ali, Imran, Kato, Koichi, Poggi, Alessandro, Jon, Ernest Chua Kian, Rao, Idupulapati M., Tao, Xiaoming, He, Ji-Huan, Rao, Lingamallu Jagan Mohan, Leemans, Alexander, Pomponio, Alessio, Hernandez, Alfredo Martínez, Ahmadieh, Hamid, Sahraian, Mohammad Ali, Kelishadi, Roya, Thongboonkerd, Visith, Bahinipati, Seema, Toi, Masakazu, von Herrath, Matthias, Sellke, Frank, Sherwood, Steven, Perry, George, Nieto, Juan J., Gupta, Sudhir, Dorigo, Tommaso, Mobasher, Bahram, Ochs, Hans D., Rezaei, Nima, Rezaei, Nima, Series Editor, Ahmed, Atif A., Editorial Board Member, Aguiar, Rodrigo, Editorial Board Member, Ambrosio, Maria R., Editorial Board Member, Artac, Mehmet, Editorial Board Member, Augustine, Tanya N., Editorial Board Member, Bambauer, Rolf, Editorial Board Member, Bhat, Ajaz Ahmad, Editorial Board Member, Bertolaccini, Luca, Editorial Board Member, Bianchini, Chiara, Editorial Board Member, Cavic, Milena, Editorial Board Member, Chakrabarti, Sakti, Editorial Board Member, Cho, William C. S., Editorial Board Member, Czarnecka, Anna M., Editorial Board Member, Domingues, Cátia, Editorial Board Member, Eşkazan, A. Emre, Editorial Board Member, Fares, Jawad, Editorial Board Member, Fonseca Alves, Carlos E., Editorial Board Member, Fru, Pascaline, Editorial Board Member, Da Gama Duarte, Jessica, Editorial Board Member, García, Mónica C., Editorial Board Member, Gener, Melissa A.H., Editorial Board Member, Estrada Guadarrama, José Antonio, Editorial Board Member, Hargadon, Kristian M., Editorial Board Member, Holvoet, Paul, Editorial Board Member, Jurisic, Vladimir, Editorial Board Member, Kabir, Yearul, Editorial Board Member, Katsila, Theodora, Editorial Board Member, Kleeff, Jorg, Editorial Board Member, Liang, Chao, Editorial Board Member, Tan, Mei Lan, Editorial Board Member, Li, Weijie, Editorial Board Member, Prado López, Sonia, Editorial Board Member, Macha, Muzafar A., Editorial Board Member, Malara, Natalia, Editorial Board Member, Orhan, Adile, Editorial Board Member, Prado-Garcia, Heriberto, Editorial Board Member, Pérez-Velázquez, Judith, Editorial Board Member, Rashed, Wafaa M., Editorial Board Member, Sanguedolce, Francesca, Editorial Board Member, Sorrentino, Rosalinda, Editorial Board Member, Shubina, Irina Zh., Editorial Board Member, de Araujo, Heloisa Sobreiro Selistre, Editorial Board Member, Torres-Suárez, Ana Isabel, Editorial Board Member, Włodarczyk, Jakub, Editorial Board Member, Yeong, Joe Poh Sheng, Editorial Board Member, Toscano, Marta A., Editorial Board Member, Wong, Tak-Wah, Editorial Board Member, Yin, Jun, Editorial Board Member, and Yu, Bin, Editorial Board Member

Published
2023
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25. Exploring the role of oxidative stress and the effect of N‐acetylcysteine in thiopurine‐induced liver injury in inflammatory bowel disease: A randomized crossover pilot study.

Author

van Asseldonk, Dirk P., Crouwel, Femke, Seinen, Margien L., Scheffer, Peter G., Veldkamp, Agnes I., de Boer, Nanne K., Lissenberg‐Witte, Birgit, Peters, Godefridus J., and van Bodegraven, Adriaan A.

Subjects
INFLAMMATORY bowel diseases, OXIDATIVE stress, LIVER injuries, ACETYLCYSTEINE, XANTHINE oxidase, AMINE oxidase
Abstract

Thiopurine treatment is regularly complicated by drug‐induced liver injury. It has been suggested that oxidative stress may play a synergistic role. To assess whether thiopurine‐induced liver injury coincides with increased oxidative stress and whether co‐administration with N‐acetylcysteine is protective, we performed a randomized open label crossover pilot study in inflammatory bowel disease patients with thiopurine‐induced increased serum liver tests. The study comprised four stages of 4 weeks. Patients received no additional therapy followed by N‐acetylcysteine 1200 mg twice a day, or the other way around, alongside ongoing thiopurine treatment. The third and fourth stages comprised a washout period and thiopurine reintroduction period. Nine patients completed the study, and the addition of N‐acetylcysteine decreased myeloperoxidase concentrations (33.6–24.5 pmol/L, p = 0.038). The other biomarkers remained unchanged, including thiopurine metabolites, xanthine oxidase activity, thiopurine S‐methyltransferase activity and serum liver enzyme activity tests. Reintroduction of thiopurines led to an increase of F2‐isoprostanes (101–157 ng/mmol, p = 0.038), but not of serum liver enzyme activity tests. Results suggests that thiopurines may increase oxidative stress and although the addition of N‐acetylcysteine led to a decrease in plasma myeloperoxidase concentrations, it does not protect from thiopurine‐induced increase of serum liver tests. [ABSTRACT FROM AUTHOR]

Published
2024
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28. Impact of hypoxia on chemoresistance of mesothelioma mediated by the proton-coupled folate transporter, and preclinical activity of new anti-LDH-A compounds

Author

Li Petri, Giovanna, El Hassouni, Btissame, Sciarrillo, Rocco, Funel, Niccola, Mantini, Giulia, Zeeuw van der Laan, Eveline A., Cascioferro, Stella, Avan, Amir, Zucali, Paolo Andrea, Zaffaroni, Nadia, Lagerweij, Tonny, Parrino, Barbara, Smid, Kees, Deraco, Marcello, Granchi, Carlotta, Braczko, Alicja, Smolenski, Ryszard T., Matherly, Larry H., Jansen, Gerrit, Assaraf, Yehuda G., Diana, Patrizia, Cloos, Jacqueline, Peters, Godefridus J., Minutolo, Filippo, and Giovannetti, Elisa

Published
2020
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33. The Prognostic Value of ASPHD1 and ZBTB12 in Colorectal Cancer: A Machine Learning-Based Integrated Bioinformatics Approach

Author

Asadnia, Alireza, primary, Nazari, Elham, additional, Goshayeshi, Ladan, additional, Zafari, Nima, additional, Moetamani-Ahmadi, Mehrdad, additional, Goshayeshi, Lena, additional, Azari, Haneih, additional, Pourali, Ghazaleh, additional, Khalili-Tanha, Ghazaleh, additional, Abbaszadegan, Mohammad Reza, additional, Khojasteh-Leylakoohi, Fatemeh, additional, Bazyari, MohammadJavad, additional, Kahaei, Mir Salar, additional, Ghorbani, Elnaz, additional, Khazaei, Majid, additional, Hassanian, Seyed Mahdi, additional, Gataa, Ibrahim Saeed, additional, Kiani, Mohammad Ali, additional, Peters, Godefridus J., additional, Ferns, Gordon A., additional, Batra, Jyotsna, additional, Lam, Alfred King-yin, additional, Giovannetti, Elisa, additional, and Avan, Amir, additional

Published
2023
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34. Contributors

Author

Abu, Nadiah, primary, Al-Abd, Ahmed M., additional, Allam, Rasha M., additional, Chen, Xiuping, additional, El-Halawany, Ali M., additional, Fesler, Andrew, additional, Goka, Erik T., additional, Hanif, Ezanee Azlina Mohamad, additional, Hara, Akira, additional, Hon, Kha Wai, additional, Huang, Yongzhuo, additional, Jamal, Rahman, additional, Ju, Jingfang, additional, Li, Feng, additional, Liang, Xing-Jie, additional, Lippman, Marc E., additional, Ma, Xiaowei, additional, Nasir, Siti Nurmi, additional, Othman, Norahayu, additional, Peters, Godefridus J., additional, Razak, Nur Syahada Abd, additional, Safa, Ahmad R., additional, To, Kenneth K.W., additional, Tomita, Hiroyuki, additional, Tong, Christy W.S., additional, Wu, Mingxia, additional, Yan, Wei, additional, Yu, Jie, additional, Zhao, Pengfei, additional, Zhong, Bingling, additional, and Zhong, Jie, additional

Published
2020
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41. Target Therapy in Malignant Pleural Mesothelioma: Hope or Mirage?

Author

Borea, Federica, primary, Franczak, Marika A., additional, Garcia, Maria, additional, Perrino, Matteo, additional, Cordua, Nadia, additional, Smolenski, Ryszard T., additional, Peters, Godefridus J., additional, Dziadziuszko, Rafal, additional, Santoro, Armando, additional, Zucali, Paolo A., additional, and Giovannetti, Elisa, additional

Published
2023
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42. Metabolic Effects of New Glucose Transporter (GLUT-1) and Lactate Dehydrogenase-A (LDH-A) Inhibitors against Chemoresistant Malignant Mesothelioma

Author

Franczak, Marika A., primary, Krol, Oliwia, additional, Harasim, Gabriela, additional, Jedrzejewska, Agata, additional, Zaffaroni, Nadia, additional, Granchi, Carlotta, additional, Minutolo, Filippo, additional, Avan, Amir, additional, Giovannetti, Elisa, additional, Smolenski, Ryszard T., additional, and Peters, Godefridus J., additional

Published
2023
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44. Supplementary Figure 2 from Molecular Mechanisms Involved in the Synergistic Interaction of the EZH2 Inhibitor 3-Deazaneplanocin A with Gemcitabine in Pancreatic Cancer Cells

Author

Avan, Amir, primary, Crea, Francesco, primary, Paolicchi, Elisa, primary, Funel, Niccola, primary, Galvani, Elena, primary, Marquez, Victor E, primary, Honeywell, Richard J., primary, Danesi, Romano, primary, Peters, Godefridus J., primary, and Giovannetti, Elisa, primary

Published
2023
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45. Supplementary Figure 1 from Molecular Mechanisms Involved in the Synergistic Interaction of the EZH2 Inhibitor 3-Deazaneplanocin A with Gemcitabine in Pancreatic Cancer Cells

Author

Avan, Amir, primary, Crea, Francesco, primary, Paolicchi, Elisa, primary, Funel, Niccola, primary, Galvani, Elena, primary, Marquez, Victor E, primary, Honeywell, Richard J., primary, Danesi, Romano, primary, Peters, Godefridus J., primary, and Giovannetti, Elisa, primary

Published
2023
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46. Supplementary Figure Legend from Molecular Mechanisms Involved in the Synergistic Interaction of the EZH2 Inhibitor 3-Deazaneplanocin A with Gemcitabine in Pancreatic Cancer Cells

Author

Avan, Amir, primary, Crea, Francesco, primary, Paolicchi, Elisa, primary, Funel, Niccola, primary, Galvani, Elena, primary, Marquez, Victor E, primary, Honeywell, Richard J., primary, Danesi, Romano, primary, Peters, Godefridus J., primary, and Giovannetti, Elisa, primary

Published
2023
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