HaloTag technology: a versatile platform for biomedical applications

CG England, H Luo, W Cai - Bioconjugate chemistry, 2015 - ACS Publications
Exploration of protein function and interaction is critical for discovering links among
genomics, proteomics, and disease state; yet, the immense complexity of proteomics found …

A complex task? Direct modulation of transcription factors with small molecules

AN Koehler - Current opinion in chemical biology, 2010 - Elsevier
Transcription factors with aberrant activity in disease are promising yet untested targets for
therapeutic development, particularly in oncology. Directly inhibiting or activating the …

Stabilization of the Max homodimer with a small molecule attenuates Myc-driven transcription

NB Struntz, A Chen, A Deutzmann, RM Wilson… - Cell chemical …, 2019 - cell.com
The transcription factor Max is a basic-helix-loop-helix leucine zipper (bHLHLZ) protein that
forms homodimers or interacts with other bHLHLZ proteins, including Myc and Mxd proteins …

Targeting intrinsically disordered transcription factors: changing the paradigm

K Tsafou, PB Tiwari, JD Forman-Kay, SJ Metallo… - Journal of molecular …, 2018 - Elsevier
Increased understanding of intrinsically disordered proteins (IDPs) and protein regions has
revolutionized our view of the relationship between protein structure and function. Data now …

[HTML][HTML] The i-motif as a molecular target: more than a complementary DNA secondary structure

SL Brown, S Kendrick - Pharmaceuticals, 2021 - mdpi.com
Stretches of cytosine-rich DNA are capable of adopting a dynamic secondary structure, the i-
motif. When within promoter regions, the i-motif has the potential to act as a molecular switch …

[HTML][HTML] Modulating androgen receptor-driven transcription in prostate cancer with selective CDK9 inhibitors

A Richters, SK Doyle, DB Freeman, C Lee, BS Leifer… - Cell chemical …, 2021 - cell.com
Castration-resistant prostate cancers (CRPCs) lose sensitivity to androgen-deprivation
therapies but frequently remain dependent on oncogenic transcription driven by the …

[HTML][HTML] Encoding and display technologies for combinatorial libraries in drug discovery: the coming of age from biology to therapy

Y Fan, R Feng, X Zhang, ZL Wang, F **ong… - … Pharmaceutica Sinica B, 2024 - Elsevier
Drug discovery is a sophisticated process that incorporates scientific innovations and cutting-
edge technologies. Compared to traditional bioactivity-based screening methods, encoding …

Colitis-associated colorectal cancer driven by T-bet deficiency in dendritic cells

WS Garrett, S Punit, CA Gallini, M Michaud, D Zhang… - Cancer cell, 2009 - cell.com
We previously described a mouse model of ulcerative colitis linked to T-bet deficiency in the
innate immune system. Here, we report that the majority of T-bet−/− RAG2−/− ulcerative …

Designing strategies of small-molecule compounds for modulating non-coding RNAs in cancer therapy

R Zhao, J Fu, L Zhu, Y Chen, B Liu - Journal of hematology & oncology, 2022 - Springer
Non-coding RNAs (ncRNAs) have been defined as a class of RNA molecules transcribed
from the genome but not encoding proteins, such as microRNAs, long non-coding RNAs …

Affinity-based target identification for bioactive small molecules

M Kawatani, H Osada - MedChemComm, 2014 - pubs.rsc.org
Identification of the cellular targets of bioactive small molecules is a crucial step in drug
discovery and chemical genetics. Classical affinity purification with small-molecule affinity …