Results 21 to 30 of about 1,298 (145)

Live-Cell NanoBRET Assay to Measure AKT Inhibitor Binding to Conformational States of AKT. [PDF]

ACS Chem Biol
ABSTRACT AKT is the main protein kinase of the PI3K-AKT pathway, interacting with over one hundred protein partners to facilitate cellular processes that allow cancer cells to survive and proliferate. It is an attractive target due to its control over many cellular outputs.
Harris JW, de Oliveira Simões FA, Ryerson EN, Marsiglia WM.   +3 more
europepmc   +3 more sources

Discovery of a novel and potent KRASG12V-targeting peptide with antiproliferative activity against colorectal cancer cells [PDF]

Journal of Enzyme Inhibition and Medicinal Chemistry
Despite the clinical relevance of KRASG12V in colorectal cancer, KRASG12V-specific inhibitors remain limited. Through structure-based virtual screening of a 59,319-member peptide library, we identified four KRASG12V-targeting peptides, among which ...
Hai Zhang, Shudan Yang, Yuting Wang, Miao-Miao Niu, Jingjiang She   +4 more
doaj   +2 more sources

Using nanoBRET and CRISPR/Cas9 to monitor proximity to a genome-edited protein in real-time [PDF]

Scientific Reports, 2017
Bioluminescence resonance energy transfer (BRET) has been a vital tool for understanding G protein-coupled receptor (GPCR) function. It has been used to investigate GPCR-protein and/or -ligand interactions as well as GPCR oligomerisation.
Carl W. White, Hannah K. Vanyai, Heng B. See, Elizabeth K. M. Johnstone, Kevin D. G. Pfleger   +4 more
doaj   +3 more sources

Identification of low-molecular compounds that inhibit envelope formation of hepatitis B virus [PDF]

Scientific Reports
Agents with novel mechanisms are clinically needed for the functional cure of chronic hepatitis B virus (HBV) infection. This study aimed to identify compounds that inhibit an interaction between large hepatitis B surface (LHBs) and hepatitis B core (HBc)
Kosuke Sato, Jun Inoue, Masashi Ninomiya, Akitoshi Sano, Mio Tsuruoka, Masazumi Onuki, Satoko Sawahashi, Keishi Ouchi, Kotaro Doi, Kengo Watanabe, Atsushi Masamune   +10 more
doaj   +2 more sources

Development of a HiBiT Peptide-Based NanoBRET Ligand Binding Assay for Galanin Receptor 1 in Live Cells. [PDF]

ACS Chem Biol
Galanin is a neuroendocrine peptide that regulates a wide range of physiological functions, including feeding and energy homeostasis, mood and anxiety, and modulation of pain. The function of the galanin peptide is mediated through its three galanin receptors, namely, GALR1, GALR2, and GALR3, which belong to the G protein-coupled receptor family.
Zhu H, Daly HC, Yang TG, Born J, Camacho-Hernandez GA, Yuan M, Inglese M, Chenniappan VK, Zimmerman K, Hurst R, Hu X, Newman AH, Ferré S, Ohana RF, Hall MD, Patnaik S.   +15 more
europepmc   +3 more sources

USP45-mediated deubiquitination of HIV-1 Tat regulates viral transcription and latency [PDF]

Frontiers in Microbiology
The HIV-1 Tat protein is regulated by post-translational modifications, particularly ubiquitination, but the full spectrum of deubiquitinating enzymes (DUBs) controlling HIV-1 transcription remains incompletely understood.
Kei Miyakawa, Kei Miyakawa, Kei Miyakawa, Kei Miyakawa, Hiyori Okura, Yasuyoshi Hatayama, Yasuyoshi Hatayama, Mayuko Nishi, Mayuko Nishi, Hirokazu Kimura, Hiroyuki Yamamoto, Hideki Hasegawa, Hideki Hasegawa, Tetsuro Matano, Tetsuro Matano, Akihide Ryo, Akihide Ryo   +16 more
doaj   +2 more sources

A kinetic intra-cellular assay (KICA) to measure quantitative compound binding kinetics within living cells

STAR Protocols, 2022
Summary: The Kinetic Intra-Cellular Assay (KICA) is a recombinant cell-based technique that utilizes NanoBRET technology. KICA enables the measurement of intracellular binding kinetics.
Charles S. Lay, Daniel A. Thomas, John P. Evans, Emma J. Jones, Kelly M. Gatfield, Peter D. Craggs   +5 more
doaj   +1 more source

Agonist dependency of the second phase access of β-arrestin 2 to the heteromeric µ-V1b receptor

Scientific Reports, 2021
During the development of analgesic tolerance to morphine, the V1b vasopressin receptor has been proposed to bind to β-arrestin 2 and the µ-opioid receptor to enable their interaction.
Nuttawadee Ngamlertwong, Hiroyoshi Tsuchiya, Yuta Mochimaru, Morio Azuma, Takahiro Kuchimaru, Taka-aki Koshimizu   +5 more
doaj   +1 more source

Development of a High-throughput NanoBRET Screening Platform to Identify Modulators of the RAS/RAF Interaction [PDF]

Molecular Cancer Therapeutics, 2021
Abstract Activating mutations in RAS are found in approximately 30% of human cancers, resulting in the delivery of a persistent signal to critical downstream effectors that drive tumorigenesis. RAS-driven malignancies respond poorly to conventional cancer treatments and inhibitors that target RAS directly are limited; therefore, the ...
David E. Durrant, Emily A. Smith, Ekaterina I. Goncharova, Nirmala Sharma, Patrick A. Alexander, Andrew G. Stephen, Curtis J. Henrich, Deborah K. Morrison   +7 more
openaire   +2 more sources

A Toolbox for the Generation of Chemical Probes for Baculovirus IAP Repeat Containing Proteins

Frontiers in Cell and Developmental Biology, 2022
E3 ligases constitute a large and diverse family of proteins that play a central role in regulating protein homeostasis by recruiting substrate proteins via recruitment domains to the proteasomal degradation machinery. Small molecules can either inhibit,
Martin P. Schwalm, Martin P. Schwalm, Lena M. Berger, Lena M. Berger, Maximilian N. Meuter, James D. Vasta, Cesear R. Corona, Sandra Röhm, Sandra Röhm, Benedict-Tilman Berger, Benedict-Tilman Berger, Frederic Farges, Sebastian M. Beinert, Franziska Preuss, Franziska Preuss, Viktoria Morasch, Viktoria Morasch, Vladimir V. Rogov, Vladimir V. Rogov, Sebastian Mathea, Sebastian Mathea, Krishna Saxena, Krishna Saxena, Matthew B. Robers, Susanne Müller, Susanne Müller, Stefan Knapp, Stefan Knapp, Stefan Knapp   +28 more
doaj   +1 more source