Potent PDZ-domain PICK1 inhibitors that modulate amyloid beta-mediated synaptic dysfunction
EYS Lin, LF Silvian, DJ Marcotte, CC Banos, F Jow… - Scientific reports, 2018 - nature.com
… the discovery of PICK1 small molecule inhibitors using a … in hippocampal neurons cultured
from wild-type and PICK1 … with the PICK1 PDZ domain by crystal structure determination of …
from wild-type and PICK1 … with the PICK1 PDZ domain by crystal structure determination of …
A high‐affinity, bivalent PDZ domain inhibitor complexes PICK 1 to alleviate neuropathic pain
NR Christensen, M De Luca, MB Lever… - EMBO molecular …, 2020 - embopress.org
… = 1 μM) (Madsen et al, 2005), we sought to identify the … down PICK1 expression (without
replacement) in the hippocampal … it administration (20 μM) of the small‐molecule PICK1 inhibitor …
replacement) in the hippocampal … it administration (20 μM) of the small‐molecule PICK1 inhibitor …
AMPA GluA2 subunit competitive inhibitors for PICK1 PDZ domain: Pharmacophore-based virtual screening, molecular docking, molecular dynamics simulation, and …
… compared to the availability of small molecule databases. … study to identify the best hits
against the PICK1 PDZ domain. … domain that inhibits hippocampal LTP and LTD. Proceedings …
against the PICK1 PDZ domain. … domain that inhibits hippocampal LTP and LTD. Proceedings …
Unconventional PDZ Recognition Revealed in α7 nAChR-PICK1 Complexes
… on hippocampal interneurons through its PDZ coupling with … nAChR binding to the PICK1
PDZ domain by carrying out NMR… To identify residues of α7 nAChR involved in binding PICK1, …
PDZ domain by carrying out NMR… To identify residues of α7 nAChR involved in binding PICK1, …
The electrostatic allostery could be the trigger for the changes in dynamics for the PDZ domain of PICK1
AO Stevens, Y He - bioRxiv, 2020 - biorxiv.org
… low sequence identity, making each PDZ domain unique. … -GluR2 interactions abolishes
cerebellar and hippocampal … , successfully developing a PICK1 small-molecule inhibitor with the …
cerebellar and hippocampal … , successfully developing a PICK1 small-molecule inhibitor with the …
Administration of a novel high affinity PICK1 PDZ domain inhibitor attenuates cocaine seeking in rats
C Turner, M De Luca, J Wolfheimer, N Hernandez… - …, 2020 - Elsevier
… of the small molecule PICK1 inhibitor FSC231 directly into the … Our findings support the
hypothesis that inhibition of PICK1 … Moreover, we identified systemic doses of the PICK1 inhibitor …
hypothesis that inhibition of PICK1 … Moreover, we identified systemic doses of the PICK1 inhibitor …
Rational design of PDZ domain inhibitors: discovery of small organic compounds targeting PDZ domains
… of small molecule inhibitors to modulate PDZ domains. … used to discover potent small molecule
PICK1-PDZ inhibitors. This … the detection of weakly binding inhibitors for the PDZ domain …
PICK1-PDZ inhibitors. This … the detection of weakly binding inhibitors for the PDZ domain …
PDZ domains as drug targets
NR Christensen, J Čalyševa… - Advanced …, 2019 - Wiley Online Library
… of small-molecule and peptide modulators of PDZ domains. … The first small-molecule inhibitor
of the PDZ domain in PICK1… long-term potentiation in hippocampal cornu ammonis 1 (CA1) …
of the PDZ domain in PICK1… long-term potentiation in hippocampal cornu ammonis 1 (CA1) …
Three Binding Conformations of BIO124 in the Pocket of the PICK1 PDZ Domain
AO Stevens, S Luo, Y He - Cells, 2022 - mdpi.com
… was the first-identified small-molecule inhibitor of PICK1 [44]. … long-term potentiation in
hippocampal cornu ammonis 1 (CA1) … , here we will focus on the small-molecule inhibitor BIO124 (…
hippocampal cornu ammonis 1 (CA1) … , here we will focus on the small-molecule inhibitor BIO124 (…
Emerging themes in PDZ domain signaling: structure, function, and inhibition
X Liu, EJ Fuentes - International review of cell and molecular biology, 2019 - Elsevier
… Effective small molecule inhibitors that target unique PDZ domains might be useful for the …
recognized by PDZ domains. For instance, mGluR7 interacts with the PICK-1 PDZ domain to …
recognized by PDZ domains. For instance, mGluR7 interacts with the PICK-1 PDZ domain to …