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At least 253 records · Page 14Linked to original sources

PubMed1991

Bioactive glass ceramics: properties and applications.

Heat treatment of an MgO-CaO-SiO2-P2O5 glass gave a glass ceramic containing crystalline apatite (Ca10(PO4)6O,F2] and beta-wollastonite (CaO,SiO2) in an MgO-CaO-SiO2 glassy matrix. It showed bioactivity and a fairly high mechanical strength which decreased only slowly, even under load-bearing conditions in the body. It is used clinically as artificial vertebrae, iliac bones, etc. The bioactivity of this glass ceramic was attributed to apatite formation on its surface in the body. Dissolution of calcium and silicate ions from the glass ceramic was considered to play an important role in forming the surface apatite layer. It was shown that some new kinds of bioactive materials can be developed from CaO,SiO2-based glasses. Ceramics, metals and organic polymers coated with bone-like apatite were obtained when such materials were placed in the vicinity of a CaO,SiO2-based glass in a simulated body fluid. A bioactive bone cement which was hardened within 4 min and bonded to living bone, forming an apatite, was obtained by mixing a CaO,SiO2-based glass powder with a neutral ammonium phosphate solution. Its compressive strength reached 80 MPa comparable to that of poly(methyl methacrylate) within 3 d. A bioactive and ferromagnetic glass ceramic containing crystalline magnetite (Fe3O4) in a matrix of CaO,SiO2-based glassy and crystalline phases was obtained by a heat treatment of a Fe2O3-CaO.SiO2-B2O3-P2O5 glass. This glass ceramic was shown to be useful as thermoseeds for hyperthermia treatment of cancer.

Animals↗

PubMed2006

Effect of ZnO addition on bioactive CaO-SiO2-P2O5-CaF2 glass-ceramics containing apatite and wollastonite.

Some ceramics show bone-bonding ability, i.e. bioactivity. Apatite formation on ceramics is an essential condition to bring about direct bonding to living bone when implanted into bony defects. A controlled surface reaction of the ceramic is an important factor governing the bioactivity and biodegradation of the implanted ceramic. Among bioactive ceramics, glass-ceramic A-W containing apatite and wollastonite shows high bioactivity, as well as high mechanical strength. In this study, glass-ceramics containing zinc oxide were prepared by modification of the composition of the glass-ceramic A-W. Zinc oxide was selected to control the reactivity of the glass-ceramics since zinc is a trace element that shows stimulatory effects on bone formation. Glass-ceramics were prepared by heat treatment of glasses with the general composition: xZnOx(57.0-x)CaOx35.4SiO(2)x7.2P(2)O(5)x0.4CaF(2) (where x=0-14.2mol.%). Addition of ZnO increased the chemical durability of the glass-ceramics, resulting in a decrease in the rate of apatite formation in a simulated body fluid. On the other hand, the release of zinc from the glass-ceramics increased with increasing ZnO content. Addition of ZnO may provide bioactive CaO-SiO(2)-P(2)O(5)-CaF(2) glass-ceramics with the capacity for appropriate biodegradation, as well as enhancement of bone formation.

Apatites↗

PubMed2005

The effect of the topical administration of bioactive glass on inflammatory markers of human experimental gingivitis.

Recent studies demonstrated that bioactive glass attenuated inflammatory reactions and bacterial growth in vitro. The aim of the present clinical study was to evaluate the effects of local bioactive glass-administration in vivo in subjects with experimental gingivitis. In each individual, contralateral teeth served as test and control over a 21-day non-hygiene (preventive phase) and a 7-day therapeutic phase. A 45S5 bioactive glass (10% solution) was applied daily (2 x 1 h) on the test teeth during the preventive and therapeutic phase of the study. Inflammation assessment was based on the plaque index record (PI), on the bleeding frequency (BOP) and the gingival crevicular fluid volume (GCF). Interleukin-1beta levels (IL-1beta) in the GCF were measured by ELISA. Bacterial deposits on teeth increased during the 21-days non-brushing period, with no difference in plaque accumulation between test and control sides. BOP levels were significantly reduced during the therapeutic phase by the application of bioactive glass. GCF-values showed a significant reduction on the test compared to control side during the preventive and therapeutic phase. IL-1beta counts decreased during the last 7 days of the study on the test side, but no significance was given. The topical application of 45S5 bioactive glass in humans with experimental gingivitis attenuated the clinical signs of inflammation, although the bacterial accumulation was not inhibited in this clinical trial.

Administration, Topical↗

PubMed2006

Extracellular matrix formation and mineralization on a phosphate-free porous bioactive glass scaffold using primary human osteoblast (HOB) cells.

Sol-gel derived bioactive glasses of the 70S30C (70mol% SiO2, 30mol% CaO) composition have been foamed to produce 3D bioactive scaffolds with hierarchical interconnected pore morphologies similar to trabecular bone. The aim of this study was to investigate primary human osteoblast response to porous bioactive glass scaffolds. The scaffolds supported osteoblast growth and induced differentiation, within the 3-week culture period, as depicted by enhanced ALPase enzymatic activity, without the addition of supplementary factors such as ascorbic acid, beta-glycerophosphate and dexamethasone. This is the first time this has been observed on a bioactive glass that does not contain phosphate. Deposition of extracellular matrix was also confirmed by enhanced production of the extracellular matrix protein collagen type I. SEM showed indications of mineralized bone nodule formation without the addition of growth factors. The 70S30C bioactive glass scaffolds therefore fulfil many of the criteria for an ideal scaffold for bone tissue engineering applications.

Calcification, Physiologic↗

PubMed2006

Long-acting interferon-alpha 2a modified with a trimer-structured polyethylene glycol: preparation, in vitro bioactivity, in vivo stability and pharmacokinetics.

The proper selection of size and shape for polyethylene glycol (PEG) is one of the most important points in PEGylation technology. Therefore, PEGs of various sizes and shapes have been widely developed to endow specific properties. In this study, a unique, trimer-structured, 43 kDa PEG was conjugated to interferon-alpha 2a (IFN) by forming an amide bond to improve the pharmacokinetic properties and minimize the loss of IFN bioactivity. Mono-PEGylated IFN (PEG(3)-IFN) prepared by utilizing this unique PEG was purified and characterized by cation-exchange chromatography and MALDI-TOF mass spectrometry. The in vitro bioactivity, in vivo stability, and pharmacokinetics of PEG(3)-IFN were examined and compared to those of native IFN. PEG(3)-IFN exhibited comparable in vitro bioactivities to native IFN and an excellent stability of the conjugation linkage in rat serum and various organs following subcutaneous injection. Furthermore, it showed slow absorption and markedly reduced clearance in rats, thereby increasing the biological half-life by about 40-fold compared to that of native IFN. This is the first report on the application of unique, trimer-structured PEG to bioactive proteins. The results suggest that unique, trimer-structured 43 kDa PEG can provide some advantages to improve the pharmacokinetic properties and to maintain the bioactivity of therapeutic proteins in clinical use.

Animals↗

PubMed2004

Strategy for analysis and screening of bioactive compounds in traditional Chinese medicines.

Traditional Chinese medicines (TCMs), due to their long time clinic test and reliable therapeutic efficacy, are attracting increased global attention served as excellent pools of bioactive compounds for the discovery of new drugs. However, hundreds or even thousands of components are usually contained in traditional Chinese medicines and only a few compounds are responsible for the pharmaceutical and/or toxic effects. The large numbers of other components in traditional Chinese medicines make the screening and analysis of the bioactive components extremely difficult. By the way, the combination effect of bioactive components on the pharmacological activity makes it very difficult to clear the therapeutic mechanism of TCMs. Therefore, some strategies have to design for screening of bioactive compounds in traditional Chinese medicines, which further leads to disclose the therapeutic mechanism of TCMs in molecular level. The review will summarize the present state of the art of screening strategy for active compounds in traditional Chinese medicines, and the chromatography methods for screening and analysis of bioactive compounds in traditional Chinese medicines will be emphasized.

Animals↗

PubMed2006

Sustained release of bioactive therapeutic proteins from a biodegradable elastomeric device.

Effective localized delivery of a therapeutic protein requires a biodegradable device capable of delivering active protein at a sustained rate, and at a concentration within its therapeutic window. The objective of this study was to demonstrate that a biodegradable elastomeric device can be made in a cylindrical geometry, and still retain the ability to release a variety of therapeutic proteins at a nearly constant rate in nanomolar concentration with high bioactivity. The elastomers were prepared with cylindrical geometry by photo-cross-linking an acrylated star-poly(epsilon-caprolactone-co-d,l-lactide) macromer. Vascular endothelial growth factor (VEGF), interferon-gamma (IFN-gamma), and interleukin-2 (IL-2) were co-lyophilized with excipients, then entrapped within the elastomer matrix by photo-polymerization. Under identical formulation conditions, these proteins were released at the same, nearly constant rate for a significant part of the release profile (until 70%-80% release depending on formulation characteristics). Decreasing the molecular weight of the acrylated macromer increased the rate of protein release, but did not alter the zero order nature of the release kinetics. Cell based bioactivity assays showed only that 57% of the VEGF released was bioactive. By contrast, both IL-2 and IFN-gamma showed relatively high bioactivity and over 80% of the released proteins were bioactive. The elastomer formulation has potential as a regio-specific protein delivery device.

Cells, Cultured↗

PubMed2005

The bioactivity of transforming growth factor-beta1 can be regulated via binding to dermal collagens in mink lung epithelial cells.

BACKGROUND: The bioactivity of transforming growth factor-beta1 (TGF-beta1) is known to be regulated by some components of the extracellular matrix (ECM), but the possibility that it might be regulated by collagen, the richest ECM component, has never been previously reported. OBJECTIVE: This study was designed to investigate the possible role that different types of collagens might play on the bioactivity of TGF-beta1. METHODS: The interaction of 125I-TGF-beta1 and various types of collagen was examined by a solid-phase assay and by a co-precipitation assay. The bioactivity of TGF-beta1 was assessed by a proliferation assay in which mink lung epithelial cells were examined in the presence and absence of collagens. RESULTS: Activated native dimeric TGF-beta1 bound to type I collagen in a dose-dependent manner, while monomeric TGF-beta1 bound poorly to the collagen. Type III collagen, and type I gelatin, a heat-denatured type I collagen, also showed a similar interaction with TGF-beta1, however, type IV collagen showed a weak interaction. In the presence of types I and III collagens, the inhibitory effect of TGF-beta1 on the proliferation of mink lung epithelial cells was sustained, thus suggesting that the bioactivity of TGF-beta1 had been enhanced. Type I gelatin also enhanced the inhibition of cell growth, but its effect was weak in comparison with that of type I collagen. The amount of TGF-beta1 which remained intact in the conditioned medium after incubation with MLEC in the presence of types I and III collagens was more than that incubated without collagen. CONCLUSIONS: Our results suggest that types I and III collagens, the two most abundant components of the interstitial collagens, can potentially bind to activated TGF-beta1 and regulate the bioactivity of this growth factor, thereby possibly maintaining the biologically available TGF-beta1 level.

Animals↗

PubMed2006

Live cell extraction and HPLC-MS analysis for predicting bioactive components of traditional Chinese medicines.

A novel strategy for predicting bioactive components in traditional Chinese medicines (TCM) using live cell extraction and high performance liquid chromatography-diode array detection-mass spectrometry (HPLC-DAD-MS) analysis was proposed. The hypothesis is that when cells are incubated together with the extract of TCM, the potential bioactive components in the TCM should selectively combine with the cells, and the relative concentrations of the cell-combining components in the suspension medium should decrease, while the cell-combining components would be detectable in the extract of denatured cells. The identities of the cell-combining components could be determined by HPLC-DAD-MS analysis. Using the proposed approach, the potential bioactive components of Danggui Buxue decoction, a commonly used TCM for anaemia, and its compositions, Radix Angelica Sinensis and Radix Astragli for endothelial cells, were investigated. Six compounds in the extract of Danggui Buxue decoction were detected as the components selectively combined with endothelial cells, among them two were contributed by Radix Angelica Sinensis, and four by Radix Astragli. The identities of four of the six potential bioactive compounds were elucidated as ononoside, calycosin, 3-butylphthalide and ligustilide by HPLC-DAD-MS analysis. The results indicate that the proposed approach may be applied to predict the bioactive candidates in TCM.

4-Butyrolactone↗

PubMed2004

In depth analysis of the N-terminal bioactive domain of gastric inhibitory polypeptide.

Gastric inhibitory polypeptide/glucose-dependent insulinotropic polypeptide (GIP) is an important gastrointestinal regulator of insulin release and glucose homeostasis following a meal. Strategies have been undertaken to delineate the bioactive domains of GIP with the intention of developing small molecular weight GIP mimetics. The molecular cloning of receptors for GIP and the related hormone GLP-1 (glucagon-like peptide-1) has allowed examination of the characteristics of incretin analogs in transfected cell models. The current report examines the N-terminal bioactive domain of GIP residing in residues 1-14 by alanine scanning mutagenesis and N-terminal substitution/modification. Further studies examined peptide chimeras of GIP and GLP-1 designed to localize bioactive determinants of the two hormones. The alanine scan of the GIP(1-14) sequence established that the peptide was extremely sensitive to structural perturbations. Only replacement of amino acids 2 and 13 with those found in glucagon failed to dramatically reduce receptor binding and activation. Of four GIP(1-14) peptides modified by the introduction of DP IV-resistant groups, a peptide with a reduced bond between Ala2 and Glu3 demonstrated improved receptor potency compared to native GIP(1-14). The peptide chimera studies supported recent results on the importance of a mid-region helix for bioactivity of GIP, and confirmed existence of two separable regions with independent intrinsic receptor binding and activation properties. Furthermore, peptide chimeras showed that binding of GLP-1 also involves both N- and C-terminal domains, but that it apparently contains only a single bioactive domain in its N-terminus. Together, these results should facilitate development of incretin based therapies using rational drug design for potential treatment of diabetes.

Animals↗

PubMed2004

Development of a robust microtiter plate-based assay method for assessment of bioactivity.

A microtiter plate-based assay was developed for the quantitative monitoring of bioactive compound production in Streptomyces hygroscopicus fermentation samples. The method reported demonstrates the successful application of the theories of disk diffusion based methods of bioactivity assessment, to a microtiter assay for high throughput analysis. The assay method facilitates the generation of the dose-response curve of test organisms (Escherichia coli, Bacillus subtilis and Saccharomyces cerevisiae) to a bioactive compound. Using this dose-response curve, the method facilitates definition of three distinct Minimum Inhibitory Concentration (MIC) values for use in the characterisation of the bioactive attributes of a sample. The assay uses established standard procedures to facilitate adaptation of the assay for use with a wider range of test microorganisms. Errors due to the assumption of a linear relationship between turbidity and biomass concentration are also reduced, due to incorporation of a step to convert turbidity to biomass concentration, for use in the calculation of bioactivity.

Anti-Bacterial Agents↗

PubMed1994

Circulating bioactive and immunoreactive recombinant human follicle stimulating hormone (Org 32489) after administration to gonadotropin-deficient subjects.

OBJECTIVE: To study the bioactivity of recombinant and urinary human FSH after single IM injection into gonadotropin-deficient subjects. DESIGN: Serum FSH levels were measured by immature rat granulosa cell bioassay and immuno-fluorometric assay. The isohormone distributions of injected FSH materials were analyzed by chromatofocusing. Serum samples were collected before, and 6, 24, and 72 hours after 300 IU of recombinant or urinary FSH. VOLUNTEERS: Fifteen gonadotropin-deficient subjects (8 women and 7 men) received recombinant FSH and 8 of them (4 women and 4 men) received an equal dose of urinary FSH. RESULTS: No significant differences were apparent between the bioactive FSH levels after recombinant and urinary FSH treatments (n = 8). The immunoreactive FSH levels at 72 hours after urinary FSH were significantly higher than after recombinant FSH injection with values (median and range) of 3.80 (2.76 to 5.75) IU/L (IRP 78/549) and 3.10 (1.78 to 4.95) IU/L, respectively. There were no significant changes in the bioactive to immunoreactive ratios of FSH within time and between sexes after either recombinant FSH (n = 15) or urinary FSH (n = 8). However, the bioactive to immunoreactive ratio of the FSH material injected and of the post-treatment serum samples were both higher after recombinant FSH than after urinary FSH injection. Chromatofocusing revealed that injected recombinant FSH contained more activity in the basic fractions than urinary FSH. CONCLUSION: Recombinant human FSH maintains its biological activity when injected into gonadotropin-deficient subjects. The bioactive to immunoreactive ratio of recombinant FSH was higher than that of urinary FSH indicating that recombinant FSH contains relatively more basic isohormones, and this finding was strengthened by chromatofocusing.

Adult↗

PubMed1998

Measurement and biological correlates of antibody bioactivity during antibody immunotherapies.

An important factor in the effectiveness of antibody immunotherapies is the antibody bioactivity, or the availability of free binding sites. Bioactivity may be decreased in settings where the target antigen exists in a soluble form capable of binding to circulating antibody. Because many antigens have soluble forms, we developed a method for determining if antibody is bound by soluble antigen in vivo. As a model system, we studied the interaction of soluble interleukin-2 receptor alpha (Tac; IL2R alpha; CD25) and anti-Tac antibody. We show first that HPLC readily separates free antibody from antibody which is monovalently or bivalently bound by soluble antigen. Further, we demonstrate that the distribution of the three forms of antibody accords with predictions of mass action and the binomial probability distribution. These methods were used to examine the bioactivity and concentration of free antibody in 14 patients undergoing therapeutic trial with Humanized anti-Tac antibody in leukemia and lymphoma. Results of two contrasting patients are highlighted. Low bioactivities correlated with reduced targeting of tumor cells and reduced therapeutic effectiveness. This report highlights the importance of soluble antigen in antibody therapies and demonstrates a simple method for evaluating in vivo bioactivity of antibody after therapeutic administration.

Adult↗

PubMed2001

Evaluation of hepatic cytochrome P4502E1 in the species-dependent bioactivation of 4-vinylcyclohexene.

4-Vinyl-1-cyclohexene (VCH), is converted by multiple forms of cytochrome P450 (CYP) to two monoepoxides (4-vinyl-1-cyclohexene 1,2-epoxide [VCH-1,2-epoxide], 4-vinyl-1-cyclohexene 7,8-epoxide [VCH-7,8-epoxide]), and 4-vinyl-1-cyclohexene diepoxide (VCD). A greater degree of formation of these epoxides by female B6C3F1 mice as compared to Fischer 344 rats correlates with the ovarian toxicity observed only in the mice. Understanding which isoforms of CYP are involved in VCH bioactivation will better explain the species-dependent ovotoxicity of VCH. Present studies focus on the role of CYP2E1, as this isoform is responsible for the bioactivation of several structurally related small molecular weight compounds, including 1,3-butadiene. Hepatic microsomes prepared from either mice or rats pretreated with the CYP inducer acetone demonstrated 2-fold increases in the formation of VCH-1,2-epoxide. However, incubations with microsomes from cyp2e1-deficient mice compared to those from wild type mice revealed no differences in the rates of bioactivation of VCH to the monoepoxides. Since repeated exposure to VCH is required for VCH-induced ovotoxicity, rodents were dosed with VCH for 5 or 10 d to observe effects on the hepatic concentration of CYP2E1 and/or associated activities. VCH pretreatment failed to increase the concentration of CYP2E1 or CYP2E1 activity in either species, as measured by immunoblotting analysis and p-nitrophenol hydroxylation. Based on these data, it is concluded that CYP2E1 does not play a role in the species differences between mice and rats in the bioactivation of VCH following repeated exposure to VCH. Other isoforms, such as those in CYP2A and CYP2B subfamilies, are likely involved in VCH bioactivation.

Animals↗

PubMed1991

Lung lining fluid modification of asbestos bioactivity for the alveolar macrophage.

It is likely that chrysotile fibers deposited in the lower respiratory tract become rapidly coated by components of lung lining fluid. Therefore, we have used lung lining fluid and its components as part of an in vitro model to study chrysotile stimulation of superoxide anion production by the alveolar macrophage. In terms of superoxide anion production, lung lining fluid-treated chrysotile was 50% as effective as the untreated fibers. Fractionated lung lining fluid components and pure phospholipids were tested individually for their effects on chrysotile bioactivity. Pretreatment of chrysotile with lung surfactant isolated from a 30,000g pellet of lung lining fluid decreased chrysotile-stimulated superoxide anion production by 90%. The inhibitory activity of lung surfactant was found to reside in a chloroform extract containing hydrophobic proteins and lipids. Total proteolysis of the proteins did not affect the inhibitory activity of the chloroform extract, but treatment with phospholipase C significantly decreased its inhibitory activity. The inhibitory effects of lung surfactant could be simulated with phosphatidylinositol, phosphatidylserine, and phosphatidylglycerol at concentrations equivalent to those found in lung lining fluid. These results strongly suggest that phosphatidylinositol, phosphatidylserine, and phosphatidylglycerol in lung lining fluid can modify chrysotile bioactivity for the alveolar macrophage. Together with previous results indicating that IgG enhances asbestos bioactivity, it would appear that lung lining fluid contains components that can either inhibit or enhance the bioactivity of asbestos and that it is the relative amounts of these components that determines the overall bioactivity of the fiber.

Animals↗

PubMed2002

Development and in vitro characterisation of novel bioresorbable and bioactive composite materials based on polylactide foams and Bioglass for tissue engineering applications.

Bioactive and bioresorbable composite materials were fabricated using macroporous poly(DL-lactide) (PDLLA) foams coated with and impregnated by bioactive glass (Bioglass) particles. Stable and homogeneous Bioglass coatings on the surface of PDLLA foams as well as infiltration of Bioglass particles throughout the porous network were achieved using a slurry-dipping technique in conjunction with pre-treatment of the foams in ethanol. The quality of the bioactive glass coatings was reproducible in terms of thickness and microstructure. Additionally, electrophoretic deposition was investigated as an alternative method for the fabrication of PDLLA foam/Bioglass composite materials. In vitro studies in simulated body fluid (SBF) were performed to study the formation of hydroxyapatite (HA) on the surface of PDLLA/Bioglass composites. SEM analysis showed that the HA layer thickness rapidly increased with increasing time in SBF. The high bioactivity of the PDLLA foam/Bioglass composites indicates the potential of the materials for use as bioactive, resorbable scaffolds in bone tissue engineering.

Biocompatible Materials↗

PubMed2003

New biomorphic SiC ceramics coated with bioactive glass for biomedical applications.

A new generation of light, tough and high-strength material for medical implants for bone substitutions with a good biological response is presented. The innovative product that fulfills all these requirements is based on biomorphic silicon carbide ceramics coated with a bioactive glass layer. The combination of the excellent mechanical properties and low density of the biomorphic SiC ceramics, used as a base material for implants, with the osteoconducting properties of the bioactive glass materials opens new possibilities for the development of alternative dental and orthopedic implants with enhanced mechanical and biochemical properties that ensures optimum fixation to living tissue. Biomorphic SiC is fabricated by molten-Si infiltration of carbon templates obtained by controlled pyrolysis of wood. Through this process, the microstructure of the final SiC product mimics that of the starting wood, which has been perfected by natural evolution. The basic features of such microstructure are its porosity (ranging from 30% to 70%) and its anisotropy, which resembles the cellular microstructure and the mechanical characteristics of the bone. The SiC ceramics have been successfully coated with a uniform and adherent bioactive glass film by pulsed laser ablation using an excimer ArF laser. The excellent coverage of the SiC rough surface without film spallation or detachment is demonstrated. In order to assess the coating bioactivity, in vitro tests by soaking the samples in simulated body fluid have been carried out. After 72 h, the formation of a dense apatite layer has been observed even in interconnecting pores by SEM and energy dispersive X-ray spectroscopy analysis demonstrating the bioactive response of this product.

Biomedical Engineering↗

PubMed1998

In vitro inhibition of the bioactivity of follicle-stimulating hormone by antisera against a peptide representing part of the FSH-receptor.

The aim of the present work was to define an FSH receptor (FSHR) peptide that can induce antibodies that will inhibit the bioactivity of FSH. Therefore, the hFSHR sequence was aligned with that of all other known G-protein coupled receptors. An area with increased sequence homology was identified between the FSH-, LH-, TSH receptors, the C5a receptor and the IL8 receptor. The similarity consists of a richness in acidic (D and E) and hydrophobic (Y and F) residues. In hFSHR the sequence is EDNESSYSRGFDMTYTEFDYDLCNEVVD (amino acid 299-326). Research on both the C5a- and IL8-receptor has indicated that this part is responsible for hormone binding but not for signal transduction. Protamine. an antagonist for both the C5a- and IL8 receptor also inhibited the bioactivities of FSH and LH when tested in a bioassay. This suggests that in the hFSHR this region might also be involved in hormone binding. Specificity of this region towards the diverse ligands all binding to the C5a or to the IL8 receptor might be attributed to differences in the profile of alternating basic and hydrophobic residues. Therefore, the hypothesis was tested as to whether antisera raised against peptides of this FSHR-domain would inhibit FSH-bioactivity but not LH-bioactivity. Indeed antisera were found (anti-hFSHR 309-322) that inhibited the biological activity of FSH in a bioassay. These antisera proved to be specific since they did not inhibit the bioactivity of LH. These data suggest that the core sequence (hFSHR 309-322) of the aligned domain of the hFSHR, in analogy to the IL8- and C5a receptors, is involved in hormone binding and ligand specificity. This domain therefore forms a valuable tool in FSH- and FSHR research for scientific and medical purposes.

Amino Acid Sequence↗