Results 121 to 130 of about 130,472 (328)

Probing the activity modification space of the cysteine peptidase cathepsin K with novel allosteric modifiers.

PLoS ONE, 2014
Targeting allosteric sites is gaining increasing recognition as a strategy for modulating the activity of enzymes, especially in drug design. Here we investigate the mechanisms of allosteric regulation of cathepsin K as a representative of cysteine ...
Marko Novinec, Brigita Lenarčič, Antonio Baici   +2 more
doaj   +1 more source

Integrating Spatial Proteogenomics in Cancer Research

Advanced Science, EarlyView.
Xx xx. ABSTRACT Background: Spatial proteogenomics marks a paradigm shift in oncology by integrating molecular analysis with spatial information from both spatial proteomics and other data modalities (e.g., spatial transcriptomics), thereby unveiling tumor heterogeneity and dynamic changes in the microenvironment.
Yida Wang, Yang Wu, Feng Zhang, Parthiban Periasamy, Haiyue You, Denise Goh, Rachel Elizabeth Ann Fincham, Xin Ning, Danping Wu, Lu Liu, Ying Jiang, Zhiwen Qian, Joe Yeong, Yan Zhang   +13 more
wiley   +1 more source

Robust photoregulation of GABA(A) receptors by allosteric modulation with a propofol analogue. [PDF]

, 2012
Photochemical switches represent a powerful method for improving pharmacological therapies and controlling cellular physiology. Here we report the photoregulation of GABA(A) receptors (GABA(A)Rs) by a derivative of propofol (2,6-diisopropylphenol), a ...
Bruzik, Karol S, Dellal, Shlomo S, Feng, Feng, Otis, Thomas S, Pawlowski, Michal, Pepperberg, David R, Qian, Haohua, Xie, An, Yue, Lan   +8 more
core   +2 more sources

Allosteric Regulation of the EphA2 Receptor Intracellular Region by Serine/Threonine Kinases [PDF]

, 2021
Bernhard C. Lechtenberg, Marina P. Gehring, Taylor P. Light, Mike W. Matsumoto, Kalina Hristova, Elena B. Pasquale   +5 more
openalex   +1 more source

Targeted Degradation of eEF2K by a Structure‐Guided PROTAC Strategy for the Treatment of Triple‐Negative Breast Cancer

Advanced Science, EarlyView.
This study developed an eEF2K‐targeting PROTAC, A6, that efficiently degrades eEF2K in TNBC cells, inhibiting tumor growth in vitro and in vivo. To enhance tumor‐specific delivery, we engineered A6@ZIF‐8, a pH‐sensitive nanocarrier, which improved drug accumulation at tumor sites, offering a promising therapeutic strategy for TNBC through targeted ...
Shijun Cao, Changxin Zhong, Shilong Jiang, Yungui Li, Yang Xi, Mingxuan Xiao, Ting Jiang, Xiaoya Wan, Zonglin Chen, Xiaohui Yu, Yan Cheng   +10 more
wiley   +1 more source

Eigenvector Centrality Distribution for Characterization of Protein Allosteric Pathways

, 2018
Determining the principal energy pathways for allosteric communication in biomolecules, that occur as a result of thermal motion, remains challenging due to the intrinsic complexity of the systems involved.
Batista, Victor S., Hendrickson, Heidi, Ho, Junming, Lisi, George P., Loria, J. Patrick, Morzan, Uriel N., Negre, Christian F. A., Pal, Rhitankar, Rivalta, Ivan   +8 more
core  

Parsimonious evolutionary scenario for the origin of allostery and coevolution patterns in proteins

, 2019
Proteins display generic properties that are challenging to explain by direct selection, notably allostery, the capacity to be regulated through long-range effects, and evolvability, the capacity to adapt to new selective pressures.
Rivoire, Olivier
core   +1 more source

Biological Information, Causality and Specificity - an Intimate Relationship [PDF]

, 2017
In this chapter we examine the relationship between biological information, the key biological concept of specificity, and recent philosophical work on causation.
Griffiths, Paul E., Stotz, Karola
core   +2 more sources

TRIM40 Drives Pathological Cardiac Hypertrophy and Heart Failure via Ubiquitination of PKN2

Advanced Science, EarlyView.
This study identifies the E3 ligase TRIM40 as a key driver of pathological cardiac hypertrophy. TRIM40 binds PKN2 via its B‐box domain and, through its C29‐dependent catalytic activity, mediates K63‐linked ubiquitination of PKN2. This modification enhances PKN2 phosphorylation at Ser815, thereby driving hypertrophy.
Risheng Zhao, Xiaoli Cui, Huizhu Du, Zhuoqun Wang, Chang Liu, Linxin Zhang, Jianing Qi, Di Yang, Hui Yu, Shuang Yan, Wei Liu, Haiming Sun, Mengyang Wang   +12 more
wiley   +1 more source

Automatically Defining Protein Words for Diverse Functional Predictions Based on Attention Analysis of a Protein Language Model

Advanced Science, EarlyView.
Understanding protein sequence–function relationships remains challenging due to poorly defined motifs and limited residue‐level annotations. An annotation‐agnostic framework is introduced that segments protein sequences into “protein words” using attention patterns from protein language models.
Hedi Chen, Jingrui Zhong, Xiaochun Zhang, Jingke Chen, Lin Guo, Xiaoliang Xiong, Xiaonan Zhang, Xiangyu Liu, Bailong Xiao, Boxue Tian   +9 more
wiley   +1 more source