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 …
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 …
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 …
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
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 …
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
Intrinsically disordered proteins (IDPs) are associated with various diseases and have been
proposed as promising drug targets. However, conventional structure-based approaches …
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
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 …
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 …
stable three-dimensional structure making drug discovery challenging. A validated …
Rational drug design targeting intrinsically disordered proteins
Intrinsically disordered proteins (IDPs) are proteins that perform important biological
functions without well‐defined structures under physiological conditions. IDPs can form …
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 …
emerged as major therapeutic targets for various diseases. Unlike traditional proteins that …
[HTML][HTML] Targeting intrinsically disordered proteins through dynamic interactions
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 …
have attracted significant interest in understanding if and how they may be targeted using …