MYC protein interactors in gene transcription and cancer

C Lourenco, D Resetca, C Redel, P Lin… - Nature Reviews …, 2021 - nature.com
The transcription factor and oncoprotein MYC is a potent driver of many human cancers and
can regulate numerous biological activities that contribute to tumorigenesis. How a single …

Therapeutic inhibition of Myc in cancer. Structural bases and computer-aided drug discovery approaches

LA Carabet, PS Rennie, A Cherkasov - International journal of molecular …, 2018 - mdpi.com
Myc (avian myelocytomatosis viral oncogene homolog) represents one of the most sought
after drug targets in cancer. Myc transcription factor is an essential regulator of cell growth …

A positive role of c-Myc in regulating androgen receptor and its splice variants in prostate cancer

S Bai, S Cao, L Jin, M Kobelski, B Schouest, X Wang… - Oncogene, 2019 - nature.com
Increased expression of the full-length androgen receptor (AR-FL) and AR splice variants
(AR-Vs) drives the progression of castration-resistant prostate cancer (CRPC). The levels of …

[HTML][HTML] Drugging the 'undruggable'. Therapeutic targeting of protein–DNA interactions with the use of computer-aided drug discovery methods

M Radaeva, AT Ton, M Hsing, F Ban, A Cherkasov - Drug discovery today, 2021 - Elsevier
Transcription factors (TFs) act as major oncodrivers in many cancers and are frequently
regarded as high-value therapeutic targets. The functionality of TFs relies on direct protein …

MYC the oncogene from hell: Novel opportunities for cancer therapy

A Papadimitropoulou, M Makri, G Zoidis - European Journal of Medicinal …, 2024 - Elsevier
Cancer comprises a heterogeneous disease, characterized by diverse features such as
constitutive expression of oncogenes and/or downregulation of tumor suppressor genes …

ETS transcription factors as emerging drug targets in cancer

M Hsing, Y Wang, PS Rennie, ME Cox… - Medicinal research …, 2020 - Wiley Online Library
The ETS family of proteins consists of 28 transcription factors, many of which have been
implicated in development and progression of a variety of cancers. While one family …

Novel dual-targeting c-Myc inhibitor D347-2761 represses myeloma growth via blocking c-Myc/Max heterodimerization and disturbing its stability

R Yao, M Zhang, J Zhou, L Liu, Y Zhang, J Gao… - Cell Communication and …, 2022 - Springer
Abstract Background Transcription factor c-Myc plays a critical role in various physiological
and pathological events. c-Myc gene rearrangement is closely associated with multiple …

The implication of topoisomerase II inhibitors in synthetic lethality for cancer therapy

VM Matias-Barrios, X Dong - Pharmaceuticals, 2023 - mdpi.com
DNA topoisomerase II (Top2) is essential for all eukaryotic cells in the regulation of DNA
topology through the generation of temporary double-strand breaks. Cancer cells acquire …

The slow but steady rise of binding free energy calculations in drug discovery

H Xu - Journal of Computer-Aided Molecular Design, 2023 - Springer
Binding free energy calculations are increasingly used in drug discovery research to predict
protein-ligand binding affinities and to prioritize candidate drug molecules accordingly. It has …

Turning up the heat on MYC: progress in small-molecule inhibitors

MI Truica, MC Burns, H Han, SA Abdulkadir - Cancer research, 2021 - AACR
MYC is a highly validated oncogenic transcription factor and cancer target. However, the
disordered nature of this protein has made it a challenging target, with no clinical stage …