Targeting transcription factors in cancer—from undruggable to reality

JH Bushweller - Nature Reviews Cancer, 2019 - nature.com
Mutated or dysregulated transcription factors represent a unique class of drug targets that
mediate aberrant gene expression, including blockade of differentiation and cell death gene …

Therapeutics—how to treat phase separation-associated diseases

RJ Wheeler - Emerging Topics in Life Sciences, 2020 - portlandpress.com
Liquid–liquid phase separation has drawn attention as many neurodegeneration or cancer-
associated proteins are able to form liquid membraneless compartments (condensates) by …

Targeting intrinsically disordered proteins at the edge of chaos

H Ruan, Q Sun, W Zhang, Y Liu, L Lai - Drug discovery today, 2019 - Elsevier
Highlights•Intrinscially disordered proteins (IDPs) are abundant and involved in many
diseases.•Advances and challenges in drug design targeting IDPs are discussed.•Known …

[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 …

[HTML][HTML] Structure-based inhibitor design for the intrinsically disordered protein c-Myc

C Yu, X Niu, F Jin, Z Liu, C Jin, L Lai - Scientific reports, 2016 - nature.com
Intrinsically disordered proteins (IDPs) are associated with various diseases and have been
proposed as promising drug targets. However, conventional structure-based approaches …

[HTML][HTML] Modulation of disordered proteins with a focus on neurodegenerative diseases and other pathologies

AHS Martinelli, FC Lopes, EBO John… - International journal of …, 2019 - mdpi.com
Intrinsically disordered proteins (IDPs) do not have rigid 3D structures, showing changes in
their folding depending on the environment or ligands. Intrinsically disordered proteins are …

Discovery of drugs that directly target the intrinsically disordered region of the androgen receptor

MD Sadar - Expert opinion on drug discovery, 2020 - Taylor & Francis
ABSTRACT Introduction: Intrinsically disordered proteins (IDPs) and regions (IDRs) lack
stable three-dimensional structure making drug discovery challenging. A validated …

Rational drug design targeting intrinsically disordered proteins

H Wang, R Xiong, L Lai - Wiley Interdisciplinary Reviews …, 2023 - Wiley Online Library
Intrinsically disordered proteins (IDPs) are proteins that perform important biological
functions without well‐defined structures under physiological conditions. IDPs can form …

[HTML][HTML] Recent advances in computational protocols addressing intrinsically disordered proteins

S Bhattacharya, X Lin - Biomolecules, 2019 - mdpi.com
Intrinsically disordered proteins (IDP) are abundant in the human genome and have recently
emerged as major therapeutic targets for various diseases. Unlike traditional proteins that …

[HTML][HTML] Targeting intrinsically disordered proteins through dynamic interactions

J Chen, X Liu, J Chen - Biomolecules, 2020 - mdpi.com
Intrinsically disordered proteins (IDPs) are over-represented in major disease pathways and
have attracted significant interest in understanding if and how they may be targeted using …