22 papers · ranked by Valyu relevance
Brandon W. Lewis, Sonika Patial, Yogesh Saini, Chojiro Kojima
Macrophage activation refers to the enhanced functionality of macrophages in response to endogenous or exogenous stimuli. Due to the existence of limitless stimuli and a multitude of receptors on macrophage surfaces, the nature of activation (or acquired functioning) can be specific to the encountering stimulus. This…
G. J. Schmidt, C. M. Reumiller, H. Ercan, U. Resch + 8 more
'S. Heber' 'Z. Liutkevičiūte' 'J. Basílio' 'J. A. Schmid' 'A. Assinger' 'B. Jilma' 'M. Zellner'] There is a need to assess platelet activation in patients with thrombotic disorders. P-selectin and activated integrin αIIbβ3 are usually quantified by flow cytometry to measure platelet activation. Monitoring changes in…
Shirin Nouraein, Sangsin Lee, Honghao Li, Vidal A. Saenz + 3 more
Gene expression in the brain is typically evaluated using invasive biopsy or postmortem histology. Serum markers provide an alternative way to monitor the brain, but relatively few such markers exist. Additionally, the origin of serum markers often cannot be localized to a specific cell population, and monitoring…
Marcin Poreba, Katarzyna Groborz, Wioletta Rut, Milind Pore + 6 more
The activome can be considered as a subset of the proteome that contains enzymes in their catalytically active form and can be interrogated by using probes targeted towards individual specific enzymes. A subset of such enzymes are proteases that are frequently studied with activity-based probes, small inhibitors…
Paulina Kasperkiewicz
Proteases catalyze the hydrolysis of peptide bonds. Products of this breakdown mediate signaling in an enormous number of biological processes. Serine proteases constitute the most numerous group of proteases, accounting for 40%, and they are prevalent in many physiological functions, both normal and disease-related…
Seiya Ishii, Mayano Minoda, Tadahaya Mizuno, Takumi Iwasaka + 4 more
Single-molecule enzyme activity assays have proven their potential in elucidating aberrant protein function at the proteoform level. However, the limited number of targetable enzymes is the major drawback of such assays. Here, we report the development of single-molecule enzyme activity assays utilizing activity-based…
Timo Burster, Fabian Gärtner, Uwe Knippschild, Anuar Zhanapiya
Neutrophils, migrating to the site of infection, are able to release serine proteases after being activated. These serine proteases comprise cathepsin G (CatG), neutrophil elastase protease 3 (PR3), and neutrophil serine protease 4 (NSP4). A disadvantage of the uncontrolled proteolytic activity of proteases is the…
Muhammad Kazim, Arghya Ganguly, Sebastian M. Malespini, Lai Thang + 5 more
Molecular imaging of immune activation holds tremendous potential for the development of novel immunotherapy. In particular, chemical probes capable of detecting immune responses before changes in tumor size occur can guide early therapeutic strategies. Here, we present quenched activity-based probes targeting…
Muhammad Kazim, Arghya Ganguly, Sebastian M. Malespini, Lai Thang + 5 more
Molecular imaging of immune activation holds tremendous potential for the development of novel immunotherapy. In particular, chemical probes capable of detecting immune responses before changes in tumor size occur can guide early therapeutic strategies. Here, we present quenched activity-based probes targeting…
Authors not listed
Microglia, the innate immune cells of the central nervous system (CNS), act as first responders in the context of brain injury or neurodegeneration. Their ability to switch between different neuroprotective and neurotoxic phenotypes, plays a central role in maintaining brain homeostasis. Recently, the P2Y12 receptor…
Gabriele Stephan, Joshua D. Frenster, Ines Liebscher, Dimitris G. Placantonakis
We recently demonstrated that GPR133 (ADGRD1), an adhesion G protein-coupled receptor (aGPCR) whose canonical signaling raises cytosolic cAMP, is necessary for growth of glioblastoma (GBM) and is de novo expressed in GBM relative to normal brain tissue. We showed that dissociation of autoproteolytically generated…
Chad Plumet, Spyridon D. Katsakos, Mélissa Girard, Israa Al Jamal + 4 more
'Jonathan Clarhaut' 'Brigitte Renoux' 'Isabelle Opalinski' 'Sébastien Papot'] Title: Abstract The development of innovative strategies for cell membranes engineering is of prime interest to explore and manipulate cell-cell interactions. Herein, an enzyme-sensitive recognition marker that can be introduced on cell…
Jigang Fan, Chunhao Zhu, Xiaobing Lan, Haiming Zhuang + 3 more
'Jian Zhang' 'Shaoyong Lu'] Neurotensin receptor 1 (NTSR1), a member of the Class A G protein-coupled receptor superfamily, plays an important role in modulating dopaminergic neuronal activity and eliciting opioid-independent analgesia. Recent studies suggest that promoting βarrestin-biased signaling in NTSR1 may…
Ali Tourani, Deniz Işınsu Avşar, Hriday Bavle, José Luis Sánchez-López + 2 more
Advanced Robotics Authors: ['Ali Tourani' 'Deniz Işınsu Avşar' 'Hriday Bavle' 'José Luis Sánchez-López' 'Jan P. F. Lagerwall' 'Holger Voos'] Fiducial markers are widely used in various robotics tasks, facilitating enhanced navigation, object recognition, and scene understanding. Despite their advantages for robots and…
Devon Field, Stuart Warriner, Megan Wright
Fluorescent ligands for G-protein coupled receptors (GPCRs) are valuable tools for studying the expression, pharmacology and modulation of these therapeutically important proteins in living cells. Here we report a photocrosslinking fluorescent chemical probe for Formyl peptide receptor 1 (FPR1), a critical component of…
Exequiel Porta, Karunakaran Kalesh, Jaime Isern, Patrick Steel
Identifying new enzymes and gaining insights into their mode of action (and inhibition) is a critical step in drug discovery. In this chapter, we describe a novel methodology that accelerates this process by combining the precision of Activity-Based Protein Profiling (ABPP) with the efficiency of microplate assay…
Xiang Cheng, Lina Merchan, Martin Tchernookov, Ilya Nemenman
Cells often have tens of thousands of receptors, even though only a few activated receptors can trigger full cellular responses. Reasons for the overabundance of receptors remain unclear. We suggest that, in certain conditions, the large number of receptors results in a competition among receptors to be the first to…
Shanshan Wu, Ao Ma
An activated process consists of energy activation and barrier crossing; the former is a prerequisite for the latter. Barrier crossing has been studied extensively, but energy activation has been overlooked due to a lack of means to gauge its progress. We define reaction stability ! as the probability that reactive…
Rienk Eelkema, Benjamin Klemm, Magherita Tavasso, Irene Piergentili + 3 more
We present a new method to obtain tertiary amine-based prodrugs with dual functionality, enabling (i) signal-triggered drug activation and (ii) covalent incorporation in polymer materials through a clickable azido-group unit on the molecular prodrug scaffold. Using nucleophilic substitution on an electron deficient…
Justin Eilertsen, Wylie Stroberg, Santiago Schnell
The determination of a substrate or enzyme activity by coupling of one enzymatic reaction with another easily detectable (indicator) reaction is a common practice in the biochemical sciences. Usually, the kinetics of enzyme reactions is simplified with singular perturbation analysis to derive rate or time course…
Xinchen HE, Quoc Bao Pham, Yi CHEN, Yuyao GUO
Hydrogen is a widely used reductive reagent in organic synthesis. The direct reactions between dihydrogen and other organic compounds are very difficult, due to the high stability of hydrogen molecules. To solve this problem, some strategies for dihydrogen activation have been developed. In this review, we are going to…
Yoshihiko Hasegawa
Cells use temporal dynamical patterns to transmit information via signaling pathways. As optimality with respect to the environment plays a fundamental role in biological systems, organisms have evolved optimal ways to transmit information. Here, we use optimal control theory to obtain the dynamical signal patterns for…