Results 51 to 60 of about 151,004 (296)

In silico Insights on the Allosteric Modulation of the µ-Opioid Receptor and G protein Complex in the Presence of Agonist Ligand BU72 and Potential Positive Allosteric Modulator BMS-986121 [PDF]

, 2020
The G protein-coupled receptor (GPCR) µ-opioid receptor (µOR) is one of several drug targets of commercially available therapeutics for pain. Various opioid drugs like morphines have been associated to numerous substance abuse-related deaths around the ...
Ricky, Nellas, Mac Kevin, Braza
core   +1 more source

Resistance to Allosteric Inhibitors

Journal of Molecular Biology
Allosteric inhibitors have emerged as powerful therapeutic agents capable of overcoming resistance mutations that impair the efficacy of orthosteric inhibitors. However, resistance to allosteric inhibitors can also arise, posing a challenge to their long-term effectiveness.
Outhwaite, Ian R., Kwan, Isabelle, Leyte-Vidal, Ariel, Shah, Neil P., Bahar, Ivet, Seeliger, Markus A.   +5 more
openaire   +3 more sources

Engineering allosteric communication

Current Opinion in Structural Biology, 2020
Protein allostery is a vitally important protein function that has proven to be a vexing problem to understand at the molecular level. Allosteric communication is a hallmark of many protein functions. However, despite more than four decades of study the details regarding allosteric communication in protein systems are still being developed. Engineering
Zachary D, Herde, Andrew E, Short, Valerie E, Kay, Brian D, Huang, Matthew J, Realff, Corey J, Wilson   +5 more
openaire   +3 more sources

An allosteric synthetic DNA [PDF]

Nucleic Acids Research, 1999
Allosteric DNA oligonucleotides are potentially useful diagnostic reagents. Here we develop a model system for the study of allosteric interactions in DNAs. A DNA that binds either Cibacron blue or cholic acid was isolated and partially characterized. Isolation was performed using a multi-stage SELEX.
L, Wu, J F, Curran
openaire   +2 more sources

Allosteric Modulation of PCSK9-LDLR Interaction: Can Structureless Loops be Drug Targets? [PDF]

, 2022
While most of the drugs available in the market are competitive inhibitors, there is a rapidly growing interest in development of allosteric drugs, particularly to inhibit protein-protein interactions (PPI) with large interaction surface area.
Suman, Chakrabarty, Zacharia , Shah, Salim , Shah, Krishnendu , Sinha, Ipsita, Basu   +4 more
core   +2 more sources

A Structure-Based Allosteric Modulator Design Paradigm

Health Data Science, 2023
Importance: Allosteric drugs bound to topologically distal allosteric sites hold a substantial promise in modulating therapeutic targets deemed undruggable at their orthosteric sites. Traditionally, allosteric modulator discovery has predominantly relied
Mingyu Li, Xiaobin Lan, Xun Lu, Jian Zhang   +3 more
doaj   +1 more source

Structurally similar allosteric modulators of α7 nicotinic acetylcholine receptors exhibit five distinct pharmacological effects. [PDF]

, 2015
Activation of nicotinic acetylcholine receptors (nAChRs) is associated with the binding of agonists such as acetylcholine to an extracellular site that is located at the interface between two adjacent receptor subunits.
Dhankher, P, Gill-Thind, JK, D'Oyley, JM, Sheppard, TD, Millar, NS   +4 more
core  

Engineering peptides into antibodies—opportunities and strategies for therapeutic innovation

FEBS Letters, EarlyView.
Peptides and antibodies occupy complementary therapeutic niches. Peptides recognize difficult targets in a compact format, while antibodies add specificity, long half‐life, and effector functions. This review examines strategies that merge both modalities—peptide grafting into loops, terminal and Fc fusions, and bioconjugation—highlighting how ...
Jinling Wang, Ruslana Romaniuk, Hristo L. Svilenov   +2 more
wiley   +1 more source

Sterically stabilized recombined HDL composed of modified apolipoprotein A-I for efficient targeting toward glioma cells

Drug Delivery, 2020
Reconstituted high density lipoprotein (rHDL) has been regarded as a promising brain-targeting vehicle for anti-glioma drugs under the mediation of apolipoprotein A-I (apoA-I).
Jin Li, Mengmeng Han, Jianfei Li, Zhiming Ge, Qianqian Wang, Kai Zhou, Xiaoxing Yin   +6 more
doaj   +1 more source

Cooperativity of Allosteric Receptors

Journal of Molecular Biology, 2013
Cooperativity of ligand binding to allosteric receptors can be quantified using the Hill coefficient (nH) to measure the sigmoidal character of the binding curve. However, for measurements of the transition between conformational states, nH values can be misleading due to ambiguity of the reference state.
Edelstein, Stuart J., Le Novère, Nicolas   +1 more
openaire   +2 more sources