Constraints on GPCR Heterodimerization Revealed by the Type-4 Induced-Association BRET Assay
Sign Up to like & getrecommendations! Published in 2019 at "Biophysical Journal"
DOI: 10.1016/j.bpj.2018.09.034
Abstract: G-protein-coupled receptors (GPCRs) comprise the largest and most pharmacologically important family of cell-surface receptors encoded by the human genome. In many instances, the distinct signaling behavior of certain GPCRs has been explained in terms of… read more here.
Keywords: heterodimerization revealed; constraints gpcr; gpcr heterodimerization; heterodimerization ... See more keywords
Examining Heterodimerization by Aryl C-N Coupling in Dynemicin Biosynthesis.
Sign Up to like & getrecommendations! Published in 2023 at "ACS chemical biology"
DOI: 10.1021/acschembio.2c00709
Abstract: Distinct among the enediyne antitumor antibiotics, the dynemicin subgroup is comprised of two discrete halves, an enediyne and an anthraquinone, but each is ultimately derived from the same linear β-hydroxyhexaene precursor. The linkage of these… read more here.
Keywords: aryl coupling; heterodimerization; examining heterodimerization; heterodimerization aryl ... See more keywords
Oxidation of Dueling Cysteine Promotes Subunit Exchange in SOD1.
Sign Up to like & getrecommendations! Published in 2023 at "ACS chemical neuroscience"
DOI: 10.1021/acschemneuro.3c00174
Abstract: The heterodimerization of wild-type (WT) Cu, Zn superoxide dismutase-1 (SOD1) and mutant SOD1 might be a critical step in the pathogenesis of SOD1-linked amyotrophic lateral sclerosis (ALS). Post-translational modifications that accelerate SOD1 heterodimerization remain unidentified.… read more here.
Keywords: oxidation; heterodimerization; sod1; promotes subunit ... See more keywords
Development of a Novel σ1 Receptor Biosensor Based on Its Heterodimerization with Binding Immunoglobulin Protein in Living Cells.
Sign Up to like & getrecommendations! Published in 2023 at "ACS chemical neuroscience"
DOI: 10.1021/acschemneuro.3c00206
Abstract: The σ1 receptor (S1R) is a ligand-regulated non-opioid intracellular receptor involved in several pathological conditions. The development of S1R-based drugs as therapeutic agents is a challenge due to the lack of simple functional assays to… read more here.
Keywords: s1r; heterodimerization; binding immunoglobulin; s1r bip ... See more keywords
On-Resin Recognition of Aromatic Oligopeptides and Proteins through Host-Enhanced Heterodimerization
Sign Up to like & getrecommendations! Published in 2022 at "Journal of the American Chemical Society"
DOI: 10.1021/jacs.2c02287
Abstract: Peptide dimerization is ubiquitous in natural protein conjugates and artificial self-assemblies. A major challenge in artificial systems remains achieving quantitative peptide heterodimerization, critical for next-generation biomolecular purification and formulation of therapeutics. Here, we employ a… read more here.
Keywords: host; heterodimerization; recognition aromatic; resin recognition ... See more keywords
Prevention of EloR/KhpA heterodimerization by introduction of site-specific amino acid substitutions renders the essential elongasome protein PBP2b redundant in Streptococcus pneumoniae
Sign Up to like & getrecommendations! Published in 2018 at "Scientific Reports"
DOI: 10.1038/s41598-018-38386-6
Abstract: The RNA binding proteins EloR and KhpA are important components of the regulatory network that controls and coordinates cell elongation and division in S. pneumoniae. Loss of either protein reduces cell length, and makes the… read more here.
Keywords: khpa; pneumoniae; site; heterodimerization ... See more keywords
10D1F, an Anti-HER3 Antibody That Uniquely Blocks the Receptor Heterodimerization Interface, Potently Inhibits Tumor Growth Across a Broad Panel of Tumor Models
Sign Up to like & getrecommendations! Published in 2020 at "Molecular Cancer Therapeutics"
DOI: 10.1158/1535-7163.mct-19-0515
Abstract: In recent years, HER3 has increasingly been implicated in the progression of a variety of tumor types and in acquired resistance to EGFR and HER2 therapies. Whereas EGFR and HER2 primarily signal through the MAPK… read more here.
Keywords: potently inhibits; anti her3; heterodimerization; tumor growth ... See more keywords
Abstract 3439: Evaluating nuclear receptor heterodimerization using live cell proximity assays: Implications for novel therapeutic approaches for hormone driven cancers
Sign Up to like & getrecommendations! Published in 2023 at "Cancer Research"
DOI: 10.1158/1538-7445.am2023-3439
Abstract: Breast and prostate cancer are the leading cancer diagnoses for women and men, respectively, second only to cutaneous cancers. Breast and prostate cancer arise from aberrant estrogen/estrogen receptor (ER) and testosterone/androgen receptor signaling (AR), respectively.… read more here.
Keywords: proximity; heterodimerization; live cell; receptor ... See more keywords
Agonist-induced CXCR4 and CB2 Heterodimerization Inhibits Gα13/RhoA-mediated Migration
Sign Up to like & getrecommendations! Published in 2018 at "Molecular Cancer Research"
DOI: 10.1158/1541-7786.mcr-16-0481
Abstract: G-protein–coupled receptor (GPCR) heterodimerization has emerged as a means by which alternative signaling entities can be created; yet, how receptor heterodimers affect receptor pharmacology remains unknown. Previous observations suggested a biochemical antagonism between GPCRs, CXCR4… read more here.
Keywords: migration; heterodimerization; cb2; cancer ... See more keywords
Modulation of ERCC1-XPF Heterodimerization Inhibition via Structural Modification of Small Molecule Inhibitor Side-Chains
Sign Up to like & getrecommendations! Published in 2022 at "Frontiers in Oncology"
DOI: 10.3389/fonc.2022.819172
Abstract: Inhibition of DNA repair enzymes is an attractive target for increasing the efficacy of DNA damaging chemotherapies. The ERCC1-XPF heterodimer is a key endonuclease in numerous single and double strand break repair processes, and inhibition… read more here.
Keywords: inhibition; ercc1 xpf; inhibitor; side ... See more keywords