Unbiased Drug Target Prediction Reveals Sensitivity to Ferroptosis Inducers, HDAC and RTK Inhibitors in Melanoma Subtypes
(2025) In International Journal of Dermatology 64(5). p.870-881- Abstract
Background: The utilization of PD1 and CTLA4 inhibitors has revolutionized the treatment of malignant melanoma (MM). However, resistance to targeted and immune-checkpoint-based therapies still poses a significant problem. Objective: Here, we mine large-scale MM proteogenomic data to identify druggable targets and forecast treatment efficacy and resistance. Methods: Leveraging protein profiles from established MM subtypes and molecular structures of 82 cancer treatment drugs, we identified nine candidate hub proteins, mTOR, FYN, PIK3CB, EGFR, MAPK3, MAP4K1, MAP2K1, SRC, and AKT1, across five distinct MM subtypes. These proteins are potential drug targets applicable to one or multiple MM subtypes. Additionally, by integrating... (More)
Background: The utilization of PD1 and CTLA4 inhibitors has revolutionized the treatment of malignant melanoma (MM). However, resistance to targeted and immune-checkpoint-based therapies still poses a significant problem. Objective: Here, we mine large-scale MM proteogenomic data to identify druggable targets and forecast treatment efficacy and resistance. Methods: Leveraging protein profiles from established MM subtypes and molecular structures of 82 cancer treatment drugs, we identified nine candidate hub proteins, mTOR, FYN, PIK3CB, EGFR, MAPK3, MAP4K1, MAP2K1, SRC, and AKT1, across five distinct MM subtypes. These proteins are potential drug targets applicable to one or multiple MM subtypes. Additionally, by integrating proteogenomic profiles obtained from MM subtypes with MM cell line dependency and drug sensitivity data, we identified a total of 162 potentially targetable genes. Lastly, we identified 20 compounds exhibiting potential drug impact in at least one melanoma subtype. Results: Employing these unbiased approaches, we have uncovered compounds targeting ferroptosis demonstrating a striking 30× fold difference in sensitivity among different subtypes. Conclusions: Our results suggest innovative and novel therapeutic strategies by stratifying melanoma samples through proteomic profiling, offering a spectrum of novel therapeutic interventions and prospects for combination therapy.
(Less)
- author
- organization
- publishing date
- 2025
- type
- Contribution to journal
- publication status
- published
- subject
- keywords
- drug target prediction, ferroptosis, HDAC, malignant melanoma, RTK inhibitor, skin cancer
- in
- International Journal of Dermatology
- volume
- 64
- issue
- 5
- pages
- 12 pages
- publisher
- Wiley-Blackwell
- external identifiers
-
- scopus:85215807075
- pmid:39722169
- ISSN
- 0011-9059
- DOI
- 10.1111/ijd.17586
- language
- English
- LU publication?
- yes
- id
- 2820d9c3-2f7c-4de9-ac9f-bec261f966c8
- date added to LUP
- 2025-06-03 09:01:22
- date last changed
- 2025-07-01 12:01:25
@article{2820d9c3-2f7c-4de9-ac9f-bec261f966c8, abstract = {{<p>Background: The utilization of PD1 and CTLA4 inhibitors has revolutionized the treatment of malignant melanoma (MM). However, resistance to targeted and immune-checkpoint-based therapies still poses a significant problem. Objective: Here, we mine large-scale MM proteogenomic data to identify druggable targets and forecast treatment efficacy and resistance. Methods: Leveraging protein profiles from established MM subtypes and molecular structures of 82 cancer treatment drugs, we identified nine candidate hub proteins, mTOR, FYN, PIK3CB, EGFR, MAPK3, MAP4K1, MAP2K1, SRC, and AKT1, across five distinct MM subtypes. These proteins are potential drug targets applicable to one or multiple MM subtypes. Additionally, by integrating proteogenomic profiles obtained from MM subtypes with MM cell line dependency and drug sensitivity data, we identified a total of 162 potentially targetable genes. Lastly, we identified 20 compounds exhibiting potential drug impact in at least one melanoma subtype. Results: Employing these unbiased approaches, we have uncovered compounds targeting ferroptosis demonstrating a striking 30× fold difference in sensitivity among different subtypes. Conclusions: Our results suggest innovative and novel therapeutic strategies by stratifying melanoma samples through proteomic profiling, offering a spectrum of novel therapeutic interventions and prospects for combination therapy.</p>}}, author = {{Pla, Indira and Szabolcs, Botond L. and Péter, Petra Nikolett and Ujfaludi, Zsuzsanna and Kim, Yonghyo and Horvatovich, Peter and Sanchez, Aniel and Pawlowski, Krzysztof and Wieslander, Elisabet and Kuras, Magdalena and Murillo, Jimmy Rodriguez and Guedes, Jéssica and Pál, Dorottya M.P. and Ascsillán, Anna A. and Betancourt, Lazaro Hiram and Németh, István Balázs and Gil, Jeovanis and de Almeida, Natália Pinto and Szeitz, Beáta and Szadai, Leticia and Doma, Viktória and Woldmar, Nicole and Bartha, Áron and Pahi, Zoltan and Pankotai, Tibor and Győrffy, Balázs and Szasz, A. Marcell and Domont, Gilberto and Nogueira, Fábio and Kwon, Ho Jeong and Appelqvist, Roger and Kárpáti, Sarolta and Fenyö, David and Malm, Johan and Marko-Varga, György and Kemény, Lajos V.}}, issn = {{0011-9059}}, keywords = {{drug target prediction; ferroptosis; HDAC; malignant melanoma; RTK inhibitor; skin cancer}}, language = {{eng}}, number = {{5}}, pages = {{870--881}}, publisher = {{Wiley-Blackwell}}, series = {{International Journal of Dermatology}}, title = {{Unbiased Drug Target Prediction Reveals Sensitivity to Ferroptosis Inducers, HDAC and RTK Inhibitors in Melanoma Subtypes}}, url = {{http://dx.doi.org/10.1111/ijd.17586}}, doi = {{10.1111/ijd.17586}}, volume = {{64}}, year = {{2025}}, }