Results 71 to 80 of about 3,754,687 (312)

Τhiazolidine-4-One Derivatives with Variable Modes of Inhibitory Action Against DPP4, a Drug Target with Multiple Activities and Established Role in Diabetes Mellitus Type II

Pharmaceuticals
Background/Objectives: DPP4 is an enzyme with multiple natural substrates and probable involvement in various mechanisms. It constitutes a drug target for the treatment of diabetes II, although, also related to other disorders.
Dionysia Amanatidou, Phaedra Eleftheriou, Anthi Petrou, Athina Geronikaki, Theodoros Lialiaris   +4 more
doaj   +1 more source

The pH-dependence of the binding of competitive inhibitors to pepsin [PDF]

Biochemical Journal, 1969
1. The pH-dependence of the binding to pepsin of four dipeptide competitive inhibitors is reported. Values of Ki obtained from equilibrium-dialysis experiments agree closely with those from kinetic measurements. 2. The binding of uncharged N-acyl-dipeptide amides to pepsin is essentially independent of pH from 0·2 to 5·8.
J R, Knowles, H, Sharp, P, Greenwell
openaire   +2 more sources

EDNRB‐dependent endothelin signaling reduces proliferation and promotes proneural‐to‐mesenchymal transition in gliomas

Molecular Oncology, EarlyView.
Glioma cells mainly express the endothelin receptor EDNRB, while EDNRA is restricted to a perivascular tumor subpopulation. Endothelin signaling reduces glioma cell proliferation while promoting migration and a proneural‐to‐mesenchymal transition associated with poor prognosis. This pathway activates Ca2+, K+, ERK, and STAT3 signalings and is regulated
Donovan Pineau, Leonor Garcia, Hugo Arnold, Antonija Hanžek, Maialen Arrieta, Laurent R Gauthier, Christine Granotier‐Beckers, François D Boussin, Amaury Herbet, Marie Hautière, Valentin Asei‐Ceschino, Clémentin Jacques, Laura Brard, Thomas Harnois, Valérie Coronas, Bruno Constantin, Aurélien Chatelier, Jean Chemin, Serge Urbach, Martial Seveno, Szimonetta Hideg, Chantal Ripoll, Kasandra Aguilar‐Cázarez, Min Zheng, Guo‐Hao Huang, Sheng‐Qing Lv, Lei Zhang, Philippe Rondard, Laurent Prezeau, Jean‐Philippe Pin, Hugues Duffau, Luc Bauchet, Valérie Rigau, Franck Denat, Charles Truillet, Didier Boquet, Jean‐Philippe Hugnot   +36 more
wiley   +1 more source

Competition for zinc binding in the host-pathogen interaction [PDF]

Frontiers in Cellular and Infection Microbiology, 2013
Due to its favorable chemical properties, zinc is used as a structural or catalytic cofactor in a very large number of proteins. Despite the apparent abundance of this metal in all cell types, the intracellular pool of loosely bound zinc ions available for biological exchanges is in the picomolar range and nearly all zinc is tightly bound to proteins ...
Mauro eCerasi, Serena eAmmendola, Andrea eBattistoni, Andrea eBattistoni   +3 more
openaire   +4 more sources

Hippo pathway at the crossroads of stemness and therapeutic resistance in breast cancer

Molecular Oncology, EarlyView.
Dysregulation of the Hippo pathway drives nuclear accumulation of YAP/TAZ, activating stemness‐related transcriptional programs that sustain breast cancer stemness and fuel therapeutic resistance across subtypes, underscoring Hippo signaling as a targetable vulnerability. Figure created and edited with BioRender.com.
Giulia Schiavoni, Antonella Palmese, Stefano Scalera, Laura Cipriani, Davide Mascolo, Patrizia Vici, Teresa Arcuri, Lorena Filomeno, Eriseld Krasniqi, Giovanni Blandino, Giulia Bon, Marcello Maugeri‐Saccà   +11 more
wiley   +1 more source

Contribution of Active and Inactive States of the Human 5-HT4d Receptor to the Functional Activities of 5-HT4–Receptor Agonists

Journal of Pharmacological Sciences, 2008
In the present study, binding affinities of 5-hydroxytryptamine-4 (5-HT4) ligands for the human 5-HT4d receptor were determined using the agonist [3H]5-HT and the selective 5-HT4 antagonist [3H]GR113,808. We also compared the affinity differences between
Tadayoshi Mikami, Hiromi Sugimoto, Rie Naganeo, Takashi Ohmi, Toshiyuki Saito, Hiroyuki Eda   +5 more
doaj   +1 more source

competitive binding assay

, 2014
Citation: 'competitive binding assay' in the IUPAC Compendium of Chemical Terminology, 3rd ed.; International Union of Pure and Applied Chemistry; 2006. Online version 3.0.1, 2019. 10.1351/goldbook.C01199 • License: The IUPAC Gold Book is licensed under Creative Commons Attribution-ShareAlike CC BY-SA 4.0 International for individual terms.
openaire   +1 more source

CD47 promotes mitogen‐activated protein kinase and epithelial‐to‐mesenchymal transition molecular programs to drive prometastatic phenotypes in non‐small cell lung cancer

Molecular Oncology, EarlyView.
Beyond its role in immune evasion, this study identified that CD47 drives tumor‐intrinsic signaling in non‐small cell lung cancer (NSCLC). Transcriptomic profiling and functional studies revealed that CD47 regulates cell adhesion, migration, and metastasis through an ERK–EMT signaling axis.
Asa P.Y. Lau, Lilian G. Zhai, Ryunosuke Hoshi, Zackary Rousseau, Abraam Zakhary, Yin Fang Wu, Rola M. Saleeb, Heyu Ni, Kelsie L. Thu   +8 more
wiley   +1 more source

Selective Nitrate Binding in Competitive Hydrogen Bonding Solvents: Do Anion–π Interactions Facilitate Nitrate Selectivity?

Angewandte Chemie, 2013
New tripodal urea receptors demonstrate preferential binding of anions over competitive hydrogen bonding solvents. 1H NMR titrations in 10% DMSO-d6/CDCl3 show a higher affinity for nitrate over the halides for the fluorinated receptor, which is lost when
Michelle M Watt, L. Zakharov, M. Haley, Darren W. Johnson   +3 more
semanticscholar   +1 more source

ΔNp63 is a pioneer factor that binds inaccessible chromatin and elicits chromatin remodeling

Epigenetics & Chromatin, 2021
Background ΔNp63 is a master transcriptional regulator playing critical roles in epidermal development and other cellular processes. Recent studies suggest that ΔNp63 functions as a pioneer factor that can target its binding sites within inaccessible ...
Xinyang Yu, Prashant K. Singh, Shamira Tabrejee, Satrajit Sinha, Michael J. Buck   +4 more
doaj   +1 more source