Therapeutic targeting of “undruggable” MYC

V Llombart, MR Mansour - EBioMedicine, 2022 - thelancet.com
Summary c-MYC controls global gene expression and regulates cell proliferation, cell
differentiation, cell cycle, metabolism and apoptosis. According to some estimates, MYC is …

Targeting protein phosphatases in cancer immunotherapy and autoimmune disorders

SM Stanford, N Bottini - Nature Reviews Drug Discovery, 2023 - nature.com
Protein phosphatases act as key regulators of multiple important cellular processes and are
attractive therapeutic targets for various diseases. Although extensive effort has been …

[HTML][HTML] The PP2A-Integrator-CDK9 axis fine-tunes transcription and can be targeted therapeutically in cancer

SJ Vervoort, SA Welsh, JR Devlin, E Barbieri… - Cell, 2021 - cell.com
Gene expression by RNA polymerase II (RNAPII) is tightly controlled by cyclin-dependent
kinases (CDKs) at discrete checkpoints during the transcription cycle. The pausing …

Molecular glue discovery: current and future approaches

JA Dewey, C Delalande, SA Azizi, V Lu… - Journal of medicinal …, 2023 - ACS Publications
The intracellular interactions of biomolecules can be maneuvered to redirect signaling,
reprogram the cell cycle, or decrease infectivity using only a few dozen atoms. Such …

[HTML][HTML] Combination of hypoglycemia and metformin impairs tumor metabolic plasticity and growth by modulating the PP2A-GSK3β-MCL-1 axis

M Elgendy, M Ciro, A Hosseini, J Weiszmann… - Cancer cell, 2019 - cell.com
Tumor cells may adapt to metabolic challenges by alternating between glycolysis and
oxidative phosphorylation (OXPHOS). To target this metabolic plasticity, we combined …

Hyperphosphorylation of BCL-2 family proteins underlies functional resistance to venetoclax in lymphoid malignancies

SJF Chong, F Zhu, O Dashevsky… - The Journal of …, 2023 - Am Soc Clin Investig
The B cell leukemia/lymphoma 2 (BCL-2) inhibitor venetoclax is effective in chronic
lymphocytic leukemia (CLL); however, resistance may develop over time. Other lymphoid …

Communication between mitochondria and other organelles: a brand-new perspective on mitochondria in cancer

MF Xia, YZ Zhang, K Jin, ZT Lu, Z Zeng, W Xiong - Cell & bioscience, 2019 - Springer
Mitochondria are energy factories of cells and are important pivots for intracellular
interactions with other organelles. They interact with the endoplasmic reticulum …

Selective PP2A enhancement through biased heterotrimer stabilization

D Leonard, W Huang, S Izadmehr, CM O'Connor… - Cell, 2020 - cell.com
Impairment of protein phosphatases, including the family of serine/threonine phosphatases
designated PP2A, is essential for the pathogenesis of many diseases, including cancer. The …

MYC and therapy resistance in cancer: risks and opportunities

G Donati, B Amati - Molecular oncology, 2022 - Wiley Online Library
The MYC transcription factor, encoded by the c‐MYC proto‐oncogene, is activated by
growth‐promoting signals, and is a key regulator of biosynthetic and metabolic pathways …

Mission possible: advances in MYC therapeutic targeting in cancer

BL Allen-Petersen, RC Sears - BioDrugs, 2019 - Springer
MYC is a master transcriptional regulator that controls almost all cellular processes. Over the
last several decades, researchers have strived to define the context-dependent …