Results 141 to 150 of about 130,849 (328)

Boosting Reversible Photocontrol of a Photoxenase by an Engineered Conformational Shift

Angewandte Chemie, EarlyView.
Photocontrol of enzymes with photoswitchable unnatural amino acids hitherto yielded only limited light‐regulation factors (LRFs). Here we boosted the LRF of an imidazole glycerol phosphate synthase variant from ∼15 to ∼100 in a semi‐rational design approach and unraveled the mechanistic fundamentals of this effect via biophysical and computational ...
Sabrina Mandl, Janet Sánchez, Miquel Estévez, Astrid Bruckmann, Caroline Hiefinger, Sílvia Osuna, Andrea Hupfeld   +6 more
wiley   +2 more sources

GPCRs in CAR‐T Cell Immunotherapy: Expanding the Target Landscape and Enhancing Therapeutic Efficacy

Advanced Science, EarlyView.
Chimeric antigen receptor T cell therapy faces dual challenges of target scarcity and an immunosuppressive microenvironment in solid tumors. This review highlights how G protein‐coupled receptors can serve as both novel targets to expand the therapeutic scope and functional modules to enhance CAR‐T cell efficacy.
Zhuoqun Liu, Yuchen Xiao, Yamin Zhao, Lihe Dai, David J.H. Shih, Shikang Liang, Honglei Tian, Liu Liu, Feng Tian, Bing Liu, Lei Chang, Chao Zhang   +11 more
wiley   +1 more source

Unnatural Amino Acid and Emerging Chemistry Approaches to Map RNA–Protein Interactions

Angewandte Chemie, EarlyView.
This review highlights emerging chemistries for mapping RNA–protein interactions, including genetically encoded unnatural amino acids, novel photocrosslinkers, and non‐photoactivatable crosslinking systems. We compare their mechanisms, reactivity and applications, outlining how these next‐generation tools enable higher‐resolution, site‐specific ...
Eryn Lundrigan, Parrish Evers, Elexa Scott, John Paul Pezacki   +3 more
wiley   +2 more sources

Dissecting a novel allosteric mechanism of cruzain: A computer-aided approach.

PLoS ONE, 2019
Trypanosoma cruzi is the causative agent of Chagas disease, a neglected infection affecting millions of people in tropical regions. There are several chemotherapeutic agents for the treatment of this disease, but most of them are highly toxic and ...
Lilian Hernández Alvarez, Diego Enry Barreto Gomes, Jorge Enrique Hernández González, Pedro Geraldo Pascutti   +3 more
doaj   +1 more source

Allosteric Regulation of Caspase-6 Proteolytic Activity

, 2022
Elih M. Velázquez-Delgado
openalex   +1 more source

CD147/Basigin: From Integrative Molecular Hub to Translational Therapeutic Target

Advanced Science, EarlyView.
This review conceptualizes CD147 as a fundamental “Energy‐Structure Coupler,” physically bridging metabolic flux (via MCTs) with morphogenetic plasticity (via integrins/MMPs) to drive cancer, infection, and autoimmunity. Addressing the “specificity paradox” that limits current translation, the authors chart a strategic roadmap—spanning logic‐gated ...
Xiang‐Min Yang, Huijie Bian, Zhi‐Nan Chen   +2 more
wiley   +1 more source

Discovery of a First‐in‐Class Covalent Allosteric SHP1 Inhibitor with Immunotherapeutic Activity

Angewandte Chemie, EarlyView.
A covalent allosteric inhibitor M029 was discovered for SHP1, a novel target for immunotherapy. M029 binds to a cryptic Cys remote from the active site, exhibits robust target engagement, and blocks tumor progression by stimulating antitumor immune response.
Zihan Qu, Frederick Nguele Meke, Zheng Zhang, Aaron D. Krabill, Christine S. Muli, Brenson A. Jassim, Jiajun Dong, Quyen D. Nguyen, Yunpeng Bai, Jinyue Li, Yiming Miao, Bardia Asadi, Levi M. Johnson, Jinmin Miao, Darci J. Trader, W. Andy Tao, Zhong‐Yin Zhang   +16 more
wiley   +2 more sources

Ligand‐Induced Electronic Response Enables Predictive QM/MM Simulations

Advanced Science, EarlyView.
Quantum mechanics/molecular mechanics (QM/MM) simulations are powerful tools for modeling complex molecular systems; however, their predictability has been constrained by the ambiguous definition of the QM region. An electronically informed protocol is introduced that defines QM regions by quantifying guest‐induced orbital shifts and charge ...
Nichika Ozawa, Nahoko Kuroki, Hirotoshi Mori   +2 more
wiley   +1 more source

GSH as an A‐A Type Allosteric Activator of PKM2: Modulating Cancer Cell Homeostasis and Ferroptosis Susceptibility

Advanced Science, EarlyView.
Glutathione (GSH) defines oxidative balance, but can it directly tune central metabolism? The research reveals that GSH binds and potently activates pyruvate kniase M2 (PKM2), rewiring glycolysis and dictating ferroptosis sensitivity. Combining GSH depletion with PKM2 activation triggers mitochondrial damage and lipid peroxidation, profoundly ...
Tsan‐Jan Chen, Chi‐Jen Lo, Meng‐Jen Wu, Wei Yang Sit, Hsin‐Yu Hsu, Yi‐Cheng Huang, Chien‐Hung Lu, Yu‐Lun Chen, Wei‐Kai Fang, Shan‐Min Yang, Pei‐Lien Chen, Tokuko Haraguchi, Yasushi Hiraoka, Chun‐Yu Lin, Mei‐Ling Cheng, Muh‐Hwa Yang, Hsing‐Jien Kung, Wen‐Ching Wang   +17 more
wiley   +1 more source

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