Results 121 to 130 of about 137,279 (309)

The mesenchymal stem cell differentiation to osteoblasts is potentiate by the allosteric modulation of A2B adenosine receptors. [PDF]

, 2015
The A2B adenosine receptor (A2BAR) has been recently emerged as the major adenosine receptor involved in the mesenchymal stem cell differentiation to osteoblast and bone formation, highlighting this receptor as a new target in bone diseases.
GIACOMELLI, CHIARA, MARTINI, CLAUDIA, DANIELE, SIMONA, Greco, G, Cosimelli, B, Novellino, E, TALIANI, SABRINA, TRINCAVELLI, MARIA LETIZIA, NATALI, LETIZIA, DA SETTIMO PASSETTI, FEDERICO   +9 more
core  

SDS‐CRISPR for Single‐Nucleotide Variant Detection

Advanced Science, EarlyView.
Structure‐disruption‐sensitive CRISPR (SDS‐CRISPR) converts structural instability into single‐nucleotide precision, thereby overcoming mismatch tolerance in canonical Cas12a and enabling versatile diagnostics across DNA, RNA, and microRNA targets. When applied to rapid IDH1 mutation detection for glioma genotyping and integrated with lateral‐flow ...
Xin Guan, Chong Guo, Jiongyu Zhang, Rui Yang, Yerramsetti Ramachandra, Chengyu Hou, Minjie Pei, Shuo Zhang, Kurt T. Schalper, Xingye Liu, Qian Wu, Ketan R. Bulsara, Changchun Liu   +12 more
wiley   +1 more source

Progress toward allosteric ligands of metabotropic glutamate 7 (mGlu7) receptor: 2008-present

, 2019
Metabotropic glutamate type (7) (mGlu(7)) receptor is a member of the group III family of mGlu receptors. It is widely distributed in the central nervous system (CNS) and is preferentially expressed on presynaptic nerve terminals where it is thought to ...
Vázquez Villa, María Del Henar, Trabanco, Andrés A.   +1 more
core   +1 more source

Mechanozyme: An Artificial Enzyme With a Mechanophore Framework

Advanced Science, EarlyView.
Mechanical destabilization of a G‐quadruplex mechanophore in a DNAzyme markedly boosts its catalytic activity, demonstrating “mechanozymes” as artificial enzymes whose functions are modulated by mechanical stress exerted by ultrasonication. This mechanozyme principle is broadly applicable to control biomolecular activities.
Jiahao Ji, Pravin Pokhrel, Sajan Shakya, Bishal Pokhrel, Grinsun Sharma, Pratiksha Chaudhary, Hao Shen, Hanbin Mao   +7 more
wiley   +1 more source

Review on allosteric modulators of dopamine receptors so far

Health Science Reports
Background Contemporary research is predominantly directed towards allosteric modulators, a class of compounds designed to interact with specific sites distinct from the orthosteric site on G protein‐coupled receptors.
Fentaw Girmaw
doaj   +1 more source

Discovery of a Potent Fluorescence Polarization Probe for Identifying USP1 Allosteric Inhibitors

Advanced Science, EarlyView.
This study presents the first ubiquitin‐specific protease 1 (USP1) allosteric fluoroprobe and fluorescence polarization assay, enabling the differentiation of allosteric and catalytic site inhibitors. Further, a novel class of tetrahydroisoquinoline‐based USP1 inhibitors is designed, with compound 14a (USP1 IC50 = 29.9 nM) showing strong selectivity ...
Jiawei Cheng, Peipei Wang, Pengfei Wang, Jiamin Wang, Baiyang Li, Daqing Fang, Jian He, Xiaobei Hu, Weijuan Kan, Yubo Zhou, Chunpu Li, Jia Li, Hong Liu   +12 more
wiley   +1 more source

Exploiting protein flexibility to predict the location of allosteric sites

BMC Bioinformatics, 2012
Background Allostery is one of the most powerful and common ways of regulation of protein activity. However, for most allosteric proteins identified to date the mechanistic details of allosteric modulation are not yet well understood.
Panjkovich Alejandro, Daura Xavier
doaj   +1 more source

The Action of Positive Allosteric Modulators of the GABAAR Can Be Reversed by Novel Spiro Barbiturates

GABAARs are pentameric ligand-gated ion channels that play a major role in mediating inhibition in the CNS. They are the target of many widely used positive allosteric modulators (PAMs) of GABAARs such as general anesthetics, sedatives, antiepileptics ...
Keith W., Miller, Karol S., Bruzik, Dimosthenis, Koinas, Xiaojuan, Zhou, Bo, Wu   +4 more
core   +1 more source

Boosting Sensory Nerve‐to‐Bone Interactions Enhances Hedgehog Mediated Calvarial Bone Repair

Advanced Science, EarlyView.
Boosting sensory nerve activity via TrkA agonism strongly accelerates calvarial bone repair in adult mice. Furthermore, single‐cell RNA sequencing and neuron–bone interactome analyses identify these sensory neurons as a direct neural source of Hedgehog pathway ligands. Consequently, these ligands drive osteoblast differentiation of skeletal progenitors,
Zhao Li, Xin Xing, Beicheng Du, Myles Zhou, Austin Z. Chen, Mary Archer, Chunbao Rao, Manyu Zhu, Masnsen Cherief, Aaron W. James   +9 more
wiley   +1 more source

Revisiting Target‐Aware de novo Molecular Generation with TarPass: Between Rational Design and Texas Sharpshooter

Advanced Science, EarlyView.
TarPass provides a rigorous benchmark for target‐aware de novo molecular generation by jointly evaluating protein‐ligand interactions, molecular plausibility, and drug‐likeness on 18 well‐studied targets. Results show that current models often fail to consistently surpass random baseline in target‐specific enrichment, while post hoc multi‐tier virtual ...
Rui Qin, Zijie Chen, Yurong Li, Meijing Fang, Longji Shen, Yilong Su, Odin Zhang, Qinghan Wang, Qun Su, Jike Wang, Tingjun Hou, Yu Kang   +11 more
wiley   +1 more source