Targeted protein degradation: A promise for undruggable proteins

KTG Samarasinghe, CM Crews - Cell chemical biology, 2021 - cell.com
Summary Protein homeostasis, or" proteostasis," is indispensable for a balanced, healthy
environment within the cell. However, when natural proteostasis mechanisms are …

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 …

Crystal structures and nuclear magnetic resonance studies of the apo form of the c-MYC: MAX bHLHZip complex reveal a helical basic region in the absence of DNA

S Sammak, N Hamdani, F Gorrec, MD Allen… - Biochemistry, 2019 - ACS Publications
The c-MYC transcription factor is a master regulator of cell growth and proliferation and is an
established target for cancer therapy. This basic helix–loop–helix Zip protein forms a …

[HTML][HTML] Mechanistic roles of protein disorder within transcription

SL Shammas - Current opinion in structural biology, 2017 - Elsevier
Highlights•Protein disorder is highly over-represented within transcriptional
processes.•Protein disorder may accelerate binding, unbinding and/or DNA search …

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 …

The topology of data: opportunities for cancer research

CF Loughrey, P Fitzpatrick, N Orr… - …, 2021 - academic.oup.com
Motivation Topological methods have recently emerged as a reliable and interpretable
framework for extracting information from high-dimensional data, leading to the creation of a …

Therapeutic interventions of cancers using intrinsically disordered proteins as drug targets: c-Myc as model system

D Kumar, N Sharma, R Giri - Cancer Informatics, 2017 - journals.sagepub.com
The concept of protein intrinsic disorder has taken the driving seat to understand regulatory
proteins in general. Reports suggest that in mammals nearly 75% of signalling proteins …

TGIF1 homeodomain interacts with Smad MH1 domain and represses TGF-β signaling

E Guca, D Sunol, L Ruiz, A Konkol… - Nucleic Acids …, 2018 - academic.oup.com
TGIF1 is a multifunctional protein that represses TGF-β-activated transcription by interacting
with Smad2-Smad4 complexes. We found that the complex structure of TGIF1–HD bound to …

Development of Cell‐Permeable, Non‐Helical Constrained Peptides to Target a Key Protein–Protein Interaction in Ovarian Cancer

MM Wiedmann, YS Tan, Y Wu, S Aibara… - Angewandte Chemie …, 2017 - Wiley Online Library
There is a lack of current treatment options for ovarian clear cell carcinoma (CCC) and the
cancer is often resistant to platinum‐based chemotherapy. Hence there is an urgent need for …

Role of backbone dynamics in modulating the interactions of disordered ligands with the TAZ1 domain of the CREB-binding protein

RB Berlow, MA Martinez-Yamout, HJ Dyson… - Biochemistry, 2019 - ACS Publications
The intrinsically disordered transactivation domains of HIF-1α and CITED2 compete for
binding of the TAZ1 domain of the CREB-binding protein by a unidirectional allosteric …