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 …

Genomic regulation of transcription and RNA processing by the multitasking Integrator complex

SA Welsh, A Gardini - Nature Reviews Molecular Cell Biology, 2023 - nature.com
In higher eukaryotes, fine-tuned activation of protein-coding genes and many non-coding
RNAs pivots around the regulated activity of RNA polymerase II (Pol II). The Integrator …

[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 …

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 …

Targeting transcription cycles in cancer

SJ Vervoort, JR Devlin, N Kwiatkowski, M Teng… - Nature Reviews …, 2022 - nature.com
Accurate control of gene expression is essential for normal development and dysregulation
of transcription underpins cancer onset and progression. Similar to cell cycle regulation …

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 …

Defining molecular glues with a dual-nanobody cannabidiol sensor

S Cao, S Kang, H Mao, J Yao, L Gu, N Zheng - Nature communications, 2022 - nature.com
Abstract “Molecular glue”(MG) is a term coined to describe the mechanism of action of the
plant hormone auxin and subsequently used to characterize synthetic small molecule …

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 …

Loss of LCMT1 and biased protein phosphatase 2A heterotrimerization drive prostate cancer progression and therapy resistance

R Rasool, CM O'Connor, CK Das, M Alhusayan… - Nature …, 2023 - nature.com
Loss of the tumor suppressive activity of the protein phosphatase 2A (PP2A) is associated
with cancer, but the underlying molecular mechanisms are unclear. PP2A holoenzyme …

Modulation of phosphoprotein activity by phosphorylation targeting chimeras (PhosTACs)

PH Chen, Z Hu, E An, I Okeke, S Zheng… - ACS chemical …, 2021 - ACS Publications
Protein phosphorylation, which regulates many critical aspects of cell biology, is dynamically
governed by kinases and phosphatases. Many diseases are associated with dysregulated …