Results 1 to 10 of about 1,238 (123)

Using a NanoBRET‐Based Ligand‐Binding Assay at the β2‐Adrenoceptor for Undergraduate Pharmacology Education [PDF]

Pharmacology Research & Perspectives
The teaching of pharmacology includes a fundamental understanding of ligand binding; how it is measured and how it is calculated. We sought to modernize the techniques by which ligand affinity is determined by undergraduate students and introduce them to
Abigail Pearce, Xianglin Huang, Theo Redfern‐Nichols, Claudia M. Sisk, Dewi Safitri, Michael Collins, Milena A. Malcharek, Sergio Tomey García, Chiharu Nakamura, Andrzej Harris, Graham Ladds   +10 more
doaj   +3 more sources

An Integrated Approach toward NanoBRET Tracers for Analysis of GPCR Ligand Engagement

Molecules, 2021
Gaining insight into the pharmacology of ligand engagement with G-protein coupled receptors (GPCRs) under biologically relevant conditions is vital to both drug discovery and basic research.
Michael P Killoran, Sergiy Levin, Michelle E Boursier   +2 more
exaly   +3 more sources

Development of a novel NanoBRET high-throughput drug screening assay for human GnRH receptor using sulfo-cyanine 5 fluorophore [PDF]

Journal of Pharmaceutical Analysis
G protein-coupled receptors (GPCRs), the largest superfamily of cell surface receptors and targets for over 30% of current clinical drugs, remain crucial for future therapeutic development.
Li Shen, Xiaozhe Du, Yakai Yang, Ming Su, Rong Rong, Jia Meng, Lee Wei Lim, David G. Fernig, Zhi-Liang Lu   +8 more
doaj   +2 more sources

Development of a NanoBRET assay for evaluation of 14-3-3σ molecular glues

SLAS Discovery
We report the development of a 384-well formatted NanoBRET assay to characterize molecular glues of 14-3-3/client interactions in living cells. The seven isoforms of 14-3-3 are dimeric hub proteins with diverse roles including transcription factor ...
Holly R Vickery, Johanna M Virta, Markella Konstantinidou   +2 more
exaly   +3 more sources

REGA-SIGN: Development of a Novel Set of NanoBRET-Based G Protein Biosensors

Biosensors, 2023
Despite G protein-coupled receptors (GPCRs) being important theapeutic targets, the signaling properties of many GPCRs remain poorly characterized. GPCR activation primarily initiates heterotrimeric G protein signaling. To detect ligand-induced G protein
Katrijn Boon, Nathan Vanalken, Eef Meyen   +2 more
exaly   +3 more sources

Development of SYK NanoBRET cellular target engagement assays for gain–of–function variants

Frontiers in Chemical Biology
Spleen tyrosine kinase (SYK) is a non-receptor tyrosine kinase that is activated by phosphorylation events downstream of FcR, B-cell and T-cell receptors, integrins, and C-type lectin receptors. When the tandem Src homology 2 (SH2) domains of SYK bind to
Jacob L Capener, Vittorio L Katis, Sabrina C D Daglish   +2 more
exaly   +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

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

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

Agonist-specific FPR1 conformational change prevents receptor recycling and promotes targeted protein degradation [PDF]

Acta Pharmaceutica Sinica B
Recycling of internalized cell surface receptors is critical for membrane transport and receptor-mediated signaling. Formyl peptide receptor 1 (FPR1) plays important roles in host defense and inflammatory tissue injury.
Junlin Wang, Qiwen Liao, Geng Chen, Yixin Chang, Hong Nie, Jiahong Lu, Richard D. Ye   +6 more
doaj   +2 more sources