scholarly journals Characterization of a new duplicate δ-opioid receptor from zebrafish

2006 ◽  
Vol 37 (3) ◽  
pp. 391-403 ◽  
Author(s):  
Noelia Pinal-Seoane ◽  
Ivan Rodríguez Martin ◽  
Veronica Gonzalez-Nuñez ◽  
Ezequiel Marron Fernandez de Velasco ◽  
Francisco Alvar Alvarez ◽  
...  
Keyword(s):  
Opioid Receptor ◽  
Sequence Similarity ◽  
Duplicate Genes ◽  
Receptor Density ◽  
Brain Areas ◽  
High Sequence Similarity ◽  
Competition Binding ◽  
Δ Opioid Receptor

A new full-length cDNA (ZFOR4) that encodes an opioid receptor has been isolated from the teleost zebrafish. The encoded polypeptide is 375 amino acids long and shows high sequence similarity to other δ-opioid receptors, including ZFOR1, the other δ-opioid receptor from zebrafish previously characterized by us. In situ hybridization studies have revealed that ZFOR4 mRNA is highly expressed in particular brain areas that coincide with the expression of the δ-opioid receptor in other species. Pharmacological analysis of ZFOR4 shows specific and saturable binding with [3H] diprenorphine, displaying one binding site with KD = 3.42 ± 0.38 nM and a receptor density of 6231 ± 335 fmol/mg protein. Competition-binding experiments were performed using [3H]diprenorphine and several unlabelled ligands (peptidic and non-peptidic). The order of affinity obtained is Met-enkephalin>Naloxone>Leu-enkephalin>Dynorphin A≫BW373U86>Morphine≫≫ [D-Pen2,D-Pen5]-Enkephalin, U69,593. [35S]GTPγS stimulation studies show that the endogenous ligands Met- and Leu-enkephalin and the non-peptidic δ agonist BW373U86 were able to fully activate ZFOR4. Our results prove the existence of two functional duplicate genes of the δ-opioid receptor in the teleost zebrafish.

scholarly journals Identification of a Novel Delta Opioid Receptor Agonist Chemotype with Potential Negative Allosteric Modulator Capabilities

Molecules ◽  
2021 ◽  
Vol 26 (23) ◽  
pp. 7236
Author(s):  
Yazan J. Meqbil ◽  
Hongyu Su ◽  
Robert J. Cassell ◽  
Kendall L. Mores ◽  
Anna M. Gutridge ◽  
...  
Keyword(s):  
Opioid Receptor ◽  
Clinical Drug Development ◽  
In Vitro Characterization ◽  
Opioid Receptor Agonist ◽  
Negative Allosteric Modulator ◽  
Δ Opioid Receptor ◽  
Clinical Drug

The δ-opioid receptor (δOR) holds great potential as a therapeutic target. Yet, clinical drug development, which has focused on δOR agonists that mimic the potent and selective tool compound SNC80 have largely failed. It has increasingly become apparent that the SNC80 scaffold carries with it potent and efficacious β-arrestin recruitment. Here, we screened a relatively small (5120 molecules) physical drug library to identify δOR agonists that underrecruit β-arrestin, as it has been suggested that compounds that efficaciously recruit β-arrestin are proconvulsant. The screen identified a hit compound and further characterization using cellular binding and signaling assays revealed that this molecule (R995045, compound 1) exhibited ten-fold selectivity over µ- and κ-opioid receptors. Compound 1 represents a novel chemotype at the δOR. A subsequent characterization of fourteen analogs of compound 1, however did not identify a more potent δOR agonist. Computational modeling and in vitro characterization of compound 1 in the presence of the endogenous agonist leu-enkephalin suggest compound 1 may also bind allosterically and negatively modulate the potency of Leu-enkephalin to inhibit cAMP, acting as a ‘NAM-agonist’ in this assay. The potential physiological utility of such a class of compounds will need to be assessed in future in vivo assays.

Decrease in δ-opioid receptor density in rat brain after chronic [d-Ala2,d-Leu5]enkephalin treatment

1988 ◽  
Vol 462 (2) ◽  
pp. 313-320 ◽  
Author(s):  
Pao-Luh Tao ◽  
Li-Ren Chang ◽  
P.Y. Law ◽  
Horace H. Loh
Keyword(s):  
Rat Brain ◽  
Opioid Receptor ◽  
Receptor Density ◽  
Δ Opioid Receptor

scholarly journals Tuning the ion selectivity of two-pore channels

2017 ◽  
Vol 114 (5) ◽  
pp. 1009-1014 ◽  
Author(s):  
Jiangtao Guo ◽  
Weizhong Zeng ◽  
Youxing Jiang
Keyword(s):  
Sequence Similarity ◽  
Ion Selectivity ◽  
Structural Basis ◽  
Monovalent Cations ◽  
Nonselective Cation Channel ◽  
High Sequence Similarity ◽  
Selective Channel ◽  
Tm Domain ◽  
Key Residues

Organellar two-pore channels (TPCs) contain two copies of aShaker-like six-transmembrane (6-TM) domain in each subunit and are ubiquitously expressed in plants and animals. Interestingly, plant and animal TPCs share high sequence similarity in the filter region, yet exhibit drastically different ion selectivity. Plant TPC1 functions as a nonselective cation channel on the vacuole membrane, whereas mammalian TPC channels have been shown to be endo/lysosomal Na+-selective or Ca2+-release channels. In this study, we performed systematic characterization of the ion selectivity of TPC1 fromArabidopsis thaliana(AtTPC1) and compared its selectivity with the selectivity of human TPC2 (HsTPC2). We demonstrate that AtTPC1 is selective for Ca2+over Na+, but nonselective among monovalent cations (Li+, Na+, and K+). Our results also confirm that HsTPC2 is a Na+-selective channel activated by phosphatidylinositol 3,5-bisphosphate. Guided by our recent structure of AtTPC1, we converted AtTPC1 to a Na+-selective channel by mimicking the selectivity filter of HsTPC2 and identified key residues in the TPC filters that differentiate the selectivity between AtTPC1 and HsTPC2. Furthermore, the structure of the Na+-selective AtTPC1 mutant elucidates the structural basis for Na+selectivity in mammalian TPCs.

scholarly journals Inheritance of seedlessness and the molecular characterization of the INO gene in Annonaceae

2023 ◽  
Vol 83 ◽  
Author(s):  
B. R. R. M. Nassau ◽  
P. S. C. Mascarenhas ◽  
A. G. Guimarães ◽  
F. M. Feitosa ◽  
H. M. Ferreira ◽  
...  
Keyword(s):  
Sequence Similarity ◽  
Type A ◽  
Molecular Techniques ◽  
Wild Type ◽  
Annona Squamosa ◽  
High Sequence Similarity ◽  
Breeding Programs ◽  
Complete Dominance ◽  
Young Leaves

Abstract The inheritance of the seedless fruit characteristic of Annona squamosa has not yet been explained. Molecular techniques may aid breeding programs, mainly in the assisted selection of the target gene. The INO gene may be related to seed development in these fruits. The objective of the present paper was to investigate the inheritance of seedlessness in the 'Brazilian seedless' sugar apple and INO gene conservation in Annona squamosa and Annona cherimola x Annona squamosa genotypes by assessing their homology with the INO database genes. The F1 generation was obtained by crossing the mutant 'Brazilian seedless' (male genitor) (P1) with the wild-type A. squamosa with seeds (M1 and M2, female genitors). The INO gene was studied in mutant and wild-type A. squamosa (P1, M1, M2 and M3) and in the Gefner atemoya (A. cherimola x A. squamosa) (M4) cultivar. The DNA was extracted from young leaves, and four sets of specific primers flanking the INO gene were amplified. The seedless characteristic was identified as stenospermatic in the fruits of parental P1, suggesting monogenic inheritance with complete dominance. High sequence similarity of the INO gene amplifications in the sugar apple accessions (M1, M2, M3) and the atemoya cultivar Gefner (M4) reinforces the hypothesis of their conservation.

scholarly journals Identification of a novel receptor for an invertebrate oxytocin/vasopressin superfamily peptide: molecular and functional evolution of the oxytocin/vasopressin superfamily

2004 ◽  
Vol 382 (1) ◽  
pp. 231-237 ◽  
Author(s):  
Tsuyoshi KAWADA ◽  
Atsuhiro KANDA ◽  
Hiroyuki MINAKATA ◽  
Osamu MATSUSHIMA ◽  
Honoo SATAKE
Keyword(s):  
Sequence Similarity ◽  
Genomic Analysis ◽  
Egg Laying ◽  
Pcr Analysis ◽  
High Sequence Similarity ◽  
Calcium Dependent ◽  
Functional Correlation ◽  
Dependent Signal ◽  
Egg Laying Behaviour

Annetocin is structurally related to an OT (oxytocin)/VP (vasopressin) family peptide, which has been isolated from the earthworm Eisenia foetida and has been shown to induce OT-like egg-laying behaviour. We now report the identification of an endogenous AnR (annetocin receptor). The deduced AnR precursor displays high sequence similarity with OT/VP receptors. Genomic analysis of the AnR gene revealed that the intron-inserted position is conserved between the AnR gene and the mammalian OT/VP receptor genes. These results indicate that AnR and mammalian OT/VP receptors share a common ancestor gene. Administration of annetocin to the AnR expressed in Xenopus oocytes induced a calcium-dependent signal transduction. Reverse transcriptase–PCR analysis and in situ hybridization showed that the AnR gene is expressed specifically in the nephridia located in the clitellum region, although the nephridia are distributed throughout the worm body. This result suggests that annetocin induces egg-laying behaviour through its action on the nephridia. This is the first description concerning the functional correlation between an invertebrate OT/VP-related peptide and egg-laying behaviour.

scholarly journals In vitro and in vivo characterization of the bifunctional μ and δ opioid receptor ligand UFP‐505

2018 ◽  
Vol 175 (14) ◽  
pp. 2881-2896 ◽  
Author(s):  
N Dietis ◽  
H Niwa ◽  
R Tose ◽  
J McDonald ◽  
V Ruggieri ◽  
...  
Keyword(s):  
Opioid Receptor ◽  
Receptor Ligand ◽  
Δ Opioid Receptor ◽  
In Vivo Characterization

scholarly journals Isolation and Characterization of Insecticidal Toxins from the Venom of the North African Scorpion, Buthacus leptochelys

Toxins ◽  
2019 ◽  
Vol 11 (4) ◽  
pp. 236 ◽  
Author(s):  
Yusuke Yoshimoto ◽  
Masahiro Miyashita ◽  
Mohammed Abdel-Wahab ◽  
Moustafa Sarhan ◽  
Yoshiaki Nakagawa ◽  
...  
Keyword(s):  
Sequence Similarity ◽  
Scorpion Venom ◽  
Spectrometric Analysis ◽  
North African ◽  
High Sequence Similarity ◽  
The North ◽  
Isolation And Characterization ◽  
Ms Analysis ◽  
Insect Toxicity

Various bioactive peptides have been identified in scorpion venom, but there are many scorpion species whose venom has not been investigated. In this study, we characterized venom components of the North African scorpion, Buthacus leptochelys, by mass spectrometric analysis and evaluated their insect toxicity. This is the first report of chemical and biological characterization of the B. leptochelys venom. LC/MS analysis detected at least 148 components in the venom. We isolated four peptides that show insect toxicity (Bl-1, Bl-2, Bl-3, and Bl-4) through bioassay-guided HPLC fractionation. These toxins were found to be similar to scorpion α- and β-toxins based on their N-terminal sequences. Among them, the complete primary structure of Bl-1 was determined by combination of Edman degradation and MS/MS analysis. Bl-1 is composed of 67 amino acid residues and crosslinked with four disulfide bonds. Since Bl-1 shares high sequence similarity with α-like toxins, it is likely that it acts on Na+ channels of both insects and mammals.

Weaning-induced changes in δ-opioid receptor subtypes: Evidence from autoradiography and in situ hybridisation

1994 ◽  
Vol 54 (1) ◽  
pp. 153-154 ◽  
Author(s):  
I. Kitchen ◽  
F.M. Leslie ◽  
A. Borsodi ◽  
G. Toth ◽  
P. Melchiorri ◽  
...  
Keyword(s):  
Opioid Receptor ◽  
In Situ Hybridisation ◽  
Receptor Subtypes ◽  
Opioid Receptor Subtypes ◽  
Δ Opioid Receptor ◽  
Induced Changes

Characterization of the δ-opioid receptor found in SH-SY5Y neuroblastoma cells

1997 ◽  
Vol 323 (2-3) ◽  
pp. 261-267 ◽  
Author(s):  
Lawrence Toll ◽  
Willma E Polgar ◽  
Jane S Auh
Keyword(s):  
Opioid Receptor ◽  
Neuroblastoma Cells ◽  
Δ Opioid Receptor
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