Results 81 to 90 of about 3,018,689 (332)

Ligand-Binding Kinetics on Histamine Receptors

, 2017
Equilibrium-binding affinities of ligands for a drug target do not always accurately reflect the success of drug candidates in the clinic. Affinity-based predictions concerning competitive antagonism on the target will only be accurate if equilibrium binding of both ligands is allowed. Unless equilibrium for ligand bind- ing is obtained really quickly,
Bosma, Reggie, Mocking, T.A.M., Leurs, R., Vischer, H.F.   +3 more
openaire   +1 more source

β‐TrCP overexpression enhances cisplatin sensitivity by depleting BRCA1

Molecular Oncology, EarlyView.
Low levels of β‐TrCP (Panel A) allow the accumulation of BRCA1 and CtIP, which facilitate the repair of cisplatin‐induced DNA damage via homologous recombination (HR) and promote tumor cell survival. In contrast, high β‐TrCP expression (Panel B) leads to BRCA1 and CtIP degradation, impairing HR repair, resulting in persistent DNA damage and apoptosis ...
Rocío Jiménez‐Guerrero, Alejandro Belmonte‐Fernández, Mónica González‐Moreno, Laura Rodríguez‐Cordero, Begoña Pérez‐Valderrama, Joaquín Herrero‐Ruíz, Francisco Romero, Carmen Sáez, Miguel Á. Japón   +8 more
wiley   +1 more source

Repurposing the mammalian RNA-binding protein Musashi-1 as an allosteric translation repressor in bacteria

eLife
The RNA recognition motif (RRM) is the most common RNA-binding protein domain identified in nature. However, RRM-containing proteins are only prevalent in eukaryotic phyla, in which they play central regulatory roles.
Roswitha Dolcemascolo, María Heras-Hernández, Lucas Goiriz, Roser Montagud-Martínez, Alejandro Requena-Menéndez, Raúl Ruiz, Anna Pérez-Ràfols, R Anahí Higuera-Rodríguez, Guillermo Pérez-Ropero, Wim F Vranken, Tommaso Martelli, Wolfgang Kaiser, Jos Buijs, Guillermo Rodrigo   +13 more
doaj   +1 more source

Rapid, High Affinity Binding by a Fluorescein Templated Copolymer Combining Covalent, Hydrophobic, and Acid–Base Noncovalent Crosslinks

Sensors, 2018
A new type of biomimetic templated copolymer has been prepared by reverse addition fragmentation chain transfer polymerization (RAFT) in dioxane.
Casey J. Grenier, Anthony Timberman, Rongfang Yang, John Csoros, Alex Papantones, Leila F. Deravi, W. Rudolf Seitz   +6 more
doaj   +1 more source

Measuring Ligand Binding Kinetics to Membrane Proteins Using Virion Nano-oscillators.

Journal of the American Chemical Society, 2018
Membrane proteins play vital roles in cellular signaling processes and serve as the most popular drug targets. A key task in studying cellular functions and developing drugs is to measure the binding kinetics of ligands with the membrane proteins ...
Guangzhong Ma, Guan-Da Syu, X. Shan, Brandon W. Henson, Shaopeng Wang, P. Desai, Heng Zhu, Yuyuan Tian   +7 more
semanticscholar   +1 more source

YAP1::TFE3 mediates endothelial‐to‐mesenchymal plasticity in epithelioid hemangioendothelioma

Molecular Oncology, EarlyView.
The YAP1::TFE3 fusion protein drives endothelial‐to‐mesenchymal transition (EndMT) plasticity, resulting in the loss of endothelial characteristics and gain of mesenchymal‐like properties, including resistance to anoikis, increased migratory capacity, and loss of contact growth inhibition in endothelial cells.
Ant Murphy, Samuel Hartzler, Paula A. Vargas Carranza, Shyaman Jayasundara, Madison E. Yates, Nimod D. Janson, Bozhi Liu, Annaleigh Benton, Majid Kazemian, Jason A. Hanna   +9 more
wiley   +1 more source

Evaluation of the Toxin-to-Protein Binding Rates during Hemodialysis Using Sorbent-Loaded Mixed-Matrix Membranes

Applied Sciences, 2018
The transport and reaction phenomena that take place in multi-layered mixed-matrix membranes with activated carbon (AC) sorbents that are expected to improve extra-corporeal blood purification, are studied at the macroscopic scale.
Christos S. Stiapis, Eugene D. Skouras, Denys Pavlenko, Dimitrios Stamatialis, Vasilis N. Burganos   +4 more
doaj   +1 more source

Prediction of Drug–Target Binding Kinetics by Comparative Binding Energy Analysis

ACS Medicinal Chemistry Letters, 2018
A growing consensus is emerging that optimizing the drug–target affinity alone under equilibrium conditions does not necessarily translate into higher potency in vivo and that instead binding kinetic parameters should be optimized to ensure better ...
Gaurav K. Ganotra, R. Wade
semanticscholar   +1 more source

Intein‐based modular chimeric antigen receptor platform for specific CD19/CD20 co‐targeting

Molecular Oncology, EarlyView.
CARtein is a modular CAR platform that uses split inteins to splice antigen‐recognition modules onto a universal signaling backbone, enabling precise, scarless assembly without re‐engineering signaling domains. Deployed here against CD19 and CD20 in B‐cell malignancies, the design supports flexible multi‐antigen targeting to boost T‐cell activation and
Pablo Gonzalez‐Garcia, Noelia Moares, Wenjie Yi‐He, Rosa Luna‐Espejo, Ricardo Fernandez‐Cisnal, Javier Ocaña‐Cuesta, Juan P. Muñoz‐Miranda, Antonio Gabucio, Cecilia M. Fernandez‐Ponce, Francisco Garcia‐Cozar   +9 more
wiley   +1 more source

Rapid measurement of inhibitor binding kinetics by isothermal titration calorimetry

Nature Communications, 2018
Although drug development typically focuses on binding thermodynamics, recent studies suggest that kinetic properties can strongly impact a drug candidate’s efficacy.
Justin M. Di Trani, Stephane De Cesco, Rebecca O'Leary, J. Plescia, Claudia Jorge do Nascimento, N. Moitessier, A. Mittermaier   +6 more
semanticscholar   +1 more source