Results 191 to 200 of about 1,615,435 (305)

Applying Deep-Learning-Driven <i>De Novo</i> Design to Hit Identification: A Case Study on A_2A Adenosine Receptor Antagonists. [PDF]

J Med Chem
Persico M, Micoli A, Salmaso V, Cianciulli A, Moro S, Spalluto G, Buccioni M, Marucci G, Volpini R, Pozzan A, Micheli F, Federico S.   +11 more
europepmc   +1 more source

A Fluorogenic Cysteine‐Tetrapeptide Tagging Strategy for Nonperturbative Protein Labeling and Protein–Ligand Interaction Tracking

Advanced Science, EarlyView.
A compact Phe‐Cys‐Pro‐Phe (FCPF) tag and an environment‐sensitive SBD‐Cl‐derived probe form a sequence‐selective fluorogenic pair for wash‐free live‐cell protein imaging. This minimally perturbing chemistry allows flexible insertion at termini or loops, produces strong fluorescence upon local microenvironment confinement, supports FRET‐assisted ...
Xiao Wang, Xingcan Pan, Yongling Ying, Ziqian Bai, Jingming Zhang, Zhuang Shao, Jialiang Qian, Hongwei Li, Ning Zhang, Fan Yang, Yuan Liu, Xing Yang   +11 more
wiley   +1 more source

Evaluating 7‑Aminopyrazolo[4,3‑<i>d</i>]pyrimidines as Human A₁ and A₃ Adenosine Receptor Antagonists. [PDF]

ACS Omega
Georgiou K, Lamprakopoulou M, Buthmann H, Böing S, Pousias A, Dexter A, Chew EXY, Huang X, Michalettou EI, Pearce A, Dotsikas Y, Pouli N, Marakos P, Kolocouris A, Ladds G, Lougiakis N.   +15 more
europepmc   +1 more source

Polyphosphate Copper Nanospheres Drive Mitochondrial Metabolic Reprogramming via Calcium Phase Separation for Self‐Sensitizing Cuproptosis

Advanced Science, EarlyView.
This study developed polyphosphate (polyP)‐based nanostructures that enable calcium‐mediated metabolic reprogramming via liquid–liquid phase separation (LLPS). Released polyP undergoes LLPS with Ca2+, suppressing glycolytic flux and enhancing mitochondrial metabolism effectively.
Jing Wang, Xinyang Zhao, Zifeng Huang, Jingyi Zhang, Yucheng Tao, Yong Huang, Zijian Guo, Lei Dong, Xiuxiu Wang, Jing Zhao, Wei Wei   +10 more
wiley   +1 more source

Molecular basis of ligand binding and receptor activation at the human A₃ adenosine receptor. [PDF]

Nat Commun
Zhang L, Mobbs JI, Bennetts FM, Venugopal H, Nguyen ATN, Christopoulos A, van der Es D, Heitman LH, May LT, Glukhova A, Thal DM.   +10 more
europepmc   +1 more source

Donor‐Cell Senescence Redirects PINK1‐Marked Mitochondrial Cargo From Mitophagy to Microvesicle Transfer Through SUMO3‐Stabilized HSPA9

Advanced Science, EarlyView.
ABSTRACT Extracellular vesicle therapies have been developed for tissue repair, but how donor‐cell senescence reshapes vesicle‐mediated mitochondrial transfer remains unclear. Here, we show that senescent adipose‐derived stem cells (ADSCs) redirect damaged mitochondria into microvesicles (MVs), converting protective vesicles into pro‐degenerative ...
Zixuan Ou, Mingke Zhao, Zhiwei Ling, Lianqi Peng, Bide Tong, Huaizhen Liang, Hongchuan Wang, Di Wu, Yifan Du, Zhi Du, Shihao Zhang, Yuyuan Jia, Yifan Qian, Gan Xu, Liuliang He, Gang Li, Shun Zhang, Lei Tan, Kun Wang, Xiaobo Feng, Cao Yang, Zhiwei Liao   +21 more
wiley   +1 more source

The long march towards testing the adenosine receptor agonism hypothesis for human cerebroprotection: The story of the A₁R/A₃R receptor agonist AST-004. [PDF]

Purinergic Signal
Liston TE, Korinek WS, Jacobson KA, Lechleiter JD.   +3 more
europepmc   +1 more source

Spatiotemporally Precise Rheumatoid Arthritis Therapy via a Triple‐Locked Cascaded Nanoplatform With Dual‐Channel Self‐Reporting

Advanced Science, EarlyView.
An orthogonally programmable nanotheranostic (MB@YW NPs) enables precision therapy for rheumatoid arthritis. A triple‐locked (pH, HOCl/ONOO−, light) independently drives the release of methotrexate and sulfasalazine. Trackable by dual‐channel fluorescence, this coordinated drug delivery remodels the inflammatory microenvironment to markedly suppress ...
Jihong Liu, Wendi Zhu, Shiyun Xu, Shichang Liu, Wenjun Tang, Xiaoyu Ma, Ting Yang, Haojian Yang, Hongtong Wang, Lu Cao, Lijie Tan, Qi Wang   +11 more
wiley   +1 more source

Bitopic A₃ Adenosine Receptor Molecular Probes: Positive Allosteric Modulation and Noncanonical Activation. [PDF]

J Med Chem
Kurma SH, Pavan M, Wan TC, Pradhan B, López-Cano M, Ciruela F, Gao ZG, Auchampach JA, Jacobson KA.   +8 more
europepmc   +1 more source

BRCA1 Mutation‐Recognizing Tetrahedral Framework Nucleic Acid Nanoplatform Enables Coordinated PARP/WEE1 Inhibition and STING‐Associated Antitumor Immunity in Ovarian Cancer

Advanced Science, EarlyView.
BRCA1 mutation‐responsive FBOA‐tFNA selectively recognizes mutant transcripts and coordinates reduction‐responsive intracellular delivery of olaparib and adavosertib, amplifying DNA damage and weakening G2/M checkpoint protection. These effects are accompanied by STING‐associated immune activation and stronger antitumor immunity, while sequential anti ...
Chenyi Wang, Mengying Yao, Jinhui Xie, Dingjie Wang, Yashi Shi, Xiaodan Mao, Chunhua Lu, Pengming Sun   +7 more
wiley   +1 more source