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Identification of Flavonoid-based Hypoxia-inducible Factor-2 Alpha Inhibitors for the Treatment of Breast Cancer– In silico and In vitro Evidence

Shahinaz, Baba, M., Gor, R., Ramamurthy, C., Mohideen, H. S., Ramalingam, S., & Vijayakumar, T. M. (2025) · Anti-Cancer Agents in Medicinal Chemistry · doi:10.2174/0118715206377378250414052656 · Cited by 1

SET1B Drives Sustained HIF Activity and Disease Progression in Clear-Cell Renal Cell Carcinoma

Ortmann, B. M., Pauzaite, T., Bertlin, J. A. C., Seear, R., Arnaiz, E., Marzec, L. W., Handyside, A., Bowker, L. M., Barnett, S. E., Harcourt, K., et al. (2026) · Cancer Research · doi:10.1158/0008-5472.can-25-1076 · Cited by 1

Conditional Stabilization of the Hypoxia‐Inducible Factor HIF1α— Photoswitchable Stapled Peptides Prevent Elongin BC–Mediated Degradation

Trinh, V. T., Fischer, S., Zhang, L., Geisler, H., Pardo, B., Liefke, R., Abendroth, F., & Vázquez, O. (2025) · Angewandte Chemie International Edition · doi:10.1002/anie.202511183 · Cited by 1

HIF2α negatively regulates MYCN protein levels and promotes a low-risk noradrenergic phenotype in neuroblastoma

Yuan, J., Maitra, S., Antoniou, E., Zhu, J., Li, W., Demirel, I. S., Toskas, K., Martinez, I. L., Ozcimen, L., Lindehell, H., et al. (2025) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.2516922122 · Cited by 1

EGLN1 (PHD2) role in tumor microenvironment: insights for therapeutic targeting

Verna, G., Fantini, V., Grieco, A., Ciarrocchi, A., & Sancisi, V. (2025) · Experimental & Molecular Medicine · doi:10.1038/s12276-025-01602-1 · Cited by 1

Targeting and dissociating HIF2α from the molecular chaperone Hsp70 triggers apoptosis in kidney cancer

Heritz, J. A., Backe, S. J., Pacherille, A., Cayaban, S. J., Basin, M. F., Smith, B. M., Sager, R., Daneshvar, M., Post, D. E., Woodford, M. R., et al. (2026) · Communications Medicine · doi:10.1038/s43856-025-01356-x · Cited by 1

Structure-guided optimization of SLC1A1/EAAT3-selective inhibitors targeting renal cancer metabolism

Koochaki, P., Qiu, B., Coker, J. A., Earsley, A., Wang, N. S., Romigh, T., Goins, C. M., Salem, C., Mi, D., Days, E., et al. (2026) · The EMBO Journal · doi:10.1038/s44318-026-00776-2 · Cited by 1

IL-1β/EPAS1-Associated Ferroptotic Stress Impairs Skeletal Stem/Progenitor Cell Function in Inflammation-Associated Fracture Nonunion

Wang, R., Li, J., Zhai, Y., Song, Q. X., Xia, P., Jiang, B., Chen, M., Liu, M., & Li, C. (2026) · Current Issues in Molecular Biology · doi:10.3390/cimb48060606 · Cited by 1

Translating the undruggable target

Dart, A. (2016) · Nature reviews. Cancer · doi:10.1038/nrc.2016.107 · Cited by 1

An order-to-disorder structural switch regulates HIF-1 transcription through S247 phosphorylation in the HIF1α PAS-B domain

Hsu, C.-H., Chen, Y.-J., & Yang, C. (2022) · Computers in Biology and Medicine · doi:10.1016/j.compbiomed.2022.106006 · Cited by 1

THE JEREMIAH METZGER LECTURE:VON HIPPEL-LINDAU DISEASE: INSIGHTS INTO OXYGEN SENSING, CANCER AND DRUGGING THE UNDRUGGABLE.

Kaelin, W. G. (2022) · PubMed Central · Cited by 1

Adipocyte-specific deletion of the oxygen-sensor PHD2 sustains elevated energy expenditure at thermoneutralityPreprint

Gomez-Salazar, M. A., Cervera, I. P., Wang, R., French, K. L., García-Martín, R., Blüher, M., Schofield, C. J., Stimson, R. H., Chavakis, T., Gudmundsson, E. F., et al. (2021) · bioRxiv (Cold Spring Harbor Laboratory) · doi:10.1101/2021.01.05.425401 · Cited by 1

Hypoxia drives HIF2-dependent macrophage cell cycle entry and susceptibility to lentiviral transductionPreprint

Meng, B., Zhao, N., Mlčochová, P., Ferreira, I. A. T. M., Ortmann, B. M., Davis, T., Wit, N., Rehwinkel, J., Cook, S. J., Maxwell, P. H., et al. (2023) · bioRxiv (Cold Spring Harbor Laboratory) · doi:10.1101/2023.12.15.571908 · Cited by 1

Erythropoietin production in embryonic neural cells is controlled by hypoxia-inducible factors and histone deacetylases in an undifferentiated statePreprint

Iwamura, Y., Nakai, T., Kato, K., Ishioka, H., Yamamoto, M. P., Hirano, I., & Suzuki, N. (2024) · bioRxiv (Cold Spring Harbor Laboratory) · doi:10.1101/2024.02.28.582479 · Cited by 1

Rescuing the Function of Missense-Mutated Tumor Suppressor VHL using Stabilizing Small MoleculesPreprint

Fouad, M. A., Parry, C. S., Miller, S. A., Malhotra, S., Doyle, G. A. R., Shimabenga, E., Nurilloeva, M., Bondarenko, E., Andrianov, G. V., Childers, W. E., et al. (2026) · eLife · doi:10.7554/elife.110305.2 · Cited by 1

Translating the undruggable target

Dart, A. (2016) · Nature Reviews Drug Discovery · doi:10.1038/nrd.2016.214

Basic/Translational Science Survey Section: Kidney Cancer

Maranchie, J. K. (2017) · Urologic Oncology Seminars and Original Investigations · doi:10.1016/j.urolonc.2017.01.009

Endogenous Reporter Systems for High-Throughput Functional Screening in Clear Cell Renal Cell Carcinoma

Zaini, M. N. (2019) · Apollo (University of Cambridge) · doi:10.17863/cam.41223

Studies on the biological functions of interaction between components in Wnt, TGF-β and HIF pathways for cancer progression

Aripaka, K. (2019) · KTH Publication Database DiVA (KTH Royal Institute of Technology)

Basic/Translational Science Survey Section: Kidney Cancer

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Augmented anti-cancer effect of hypoxia-inducible factor 2α (HIF2α)- targeting PT2385 delivered in α-synuclein-AuNP microcapsules for clear cell renal carcinoma mouse model

Nam, E.-J., Kong, S.-K., Cho, I., Paik, S. R., & Kim, Y. (2023) · Journal of Drug Delivery Science and Technology · doi:10.1016/j.jddst.2023.105179

Targeting HIF-2 α in clear cell renal cell carcinoma: A promising therapeutic strategy

Martínez‐Sáez, O., Borau, P. G., Alonso‐Gordoa, T., Molina‐Cerrillo, J., & Grande, E. (2017) · Critical Reviews in Oncology/Hematology · doi:10.1016/j.critrevonc.2017.01.013 · Cited by 111

Abstract DDT01-01: PT2385: First-in-class HIF-2α antagonist for the treatment of renal cell carcinoma

Wallace, E. M., Cao, Z., Cheng, T., Czerwiński, R., Dixon, D. D., Du, X., Goggin, B. S., Grina, J. A., Halfmann, M. M., Han, G., et al. (2015) · Cancer Research · doi:10.1158/1538-7445.am2015-ddt01-01 · Cited by 1

Hypoxia-Inducible Factor-2α as a Novel Target in Renal Cell Carcinoma

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Targeting HIF2 in Clear Cell Renal Cell CarcinomaPreprint

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Abstract 494: BPI-452080: A potent and selective HIF-2α inhibitor for the treatment of clear cell renal cell carcinoma, von Hippel-Lindau disease, and other solid tumors

Wang, P., Yang, R., Sun, Y., Ju, X., Zhao, J., Liu, Y., Liu, X., Zou, Z., Ren, J., Wang, M., et al. (2023) · Cancer Research · doi:10.1158/1538-7445.am2023-494 · Cited by 2