• Title/Summary/Keyword: peptide synthesis

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Preparation of Natural Compounds-tripeptides Derivatives and Their Melanogensis Inhibitory Activity (천연유래물질 펩타이드 유도체의 제조와 멜라닌 생성 저해 효과 탐색)

  • Shin, Kyong-Hoon;Lee, Jae-Ho;Ryu, Geun-Seok;Jee, Kyung-Yup;Park, Soo-Nam;Kim, Jae-Il;Cho, In-Shik;Kim, Han-Young
    • Journal of the Society of Cosmetic Scientists of Korea
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    • v.36 no.3
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    • pp.233-240
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    • 2010
  • Derivatives of a novel natural compunds, melanostatin (PLG-$NH_2$) were prepared by solid phase synthesis[1,2] and assayed to evaluate their melanogensis inhibitory activity. Also, a small library (natural compound-XLG-$NH_2$, natural compound-X LG-OH) was prepared with same method for increasing synthetic yield and cost-reduction. PLG-$NH_2$ (Proline-Leucine-Glycine-$NH_2$) was well-known tripeptide as its $\alpha$-MSH release-inhibiting activity and tyrosinase inhibitory activity[3-5]. In order to choose best candidate for peptide derivatization, various natural compounds were screened by their tyrosinase inhibitory activity. As a result, caffeic acid and coumaric acid were selected. Most of these derivatives showed better activities than the parent natural compound, melanostatin.

Immunohistochemical studies on the relationship between pineal body and superior cervical ganglia of the Korean native goat (한국재래산양 송과체와 앞쪽목신경절의 관계규명을 위한 면역조직화학적 연구)

  • Lee, Heungshik S.;Lee, In-Se;Song, Seung-hoon;Yoon, Sung-tae;Hwang, In-koo;Lee, Choong-hyun
    • Korean Journal of Veterinary Research
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    • v.40 no.2
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    • pp.197-211
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    • 2000
  • The pineal body have been known to be affected by superior cervical ganglia, and most of its nerve fibers containing peptidergic neurotransmitters have been considered to be originated from this ganglia. To confirm this relationships, some peptidergic neurotransmitters were identified in both of pineal body and superior cervical ganglia of the Korean native goat, which were divided into two group; breeding season and non-breeding season. The localizations of two catecholamine-synthesizing enzymes; tyrosine hydroxylase (TH) and dopamine beta-hydroxylase (DBH), were investigated by immunohistochemistry in the superior cervical ganglia and the pineal body of adult Korean native goats. Substance P (SP), calcitonin gene-related peptide (CGRP), vasoactive intestinal polypeptide (VIP), neuropeptide Y (NPY) and galanin (GAL) were also identified in these organs by immunohistochemical and double immunofluorescent methods. In superior cervical ganglia, immunoreactivities for TH and DBH were confirmed in the same ganglion cells. The immunoreactivites for SP, VIP(only in male), NPY and GAL were identified in both of ganglion cell bodies and nerve fibers in the ganglia. CGRP immunoreactivity, however, was observed only in nerve fibers. Most NPY- and VIP-immunoreactive(IR) ganglion cells also contained TH. SP and TH were colocalized in the cell bodies, but not in the nerve fibers. TH immunoreactivity was shown in almost all of ganglion cells in the superior cervical ganglia. The immunoreactivity for NPY had some seasonal variation and was stronger in breeding season than in non-breeding season. In pineal body, lots of TH-IR fibers were observed throughout the parenchyma including the pineal stalk and most of them also contained DBH. SP- and NPY-IR fibers were also immunostained with TH or DBH. But a few SP- and NPY-IR fibers were not colocalized with TH or DBH. Exceptionally, a bipolar neuron-like cell was observed to be immunostained with NPY in the pineal body. A few CGRP and GAL-IR fibers were observed, while VIP-IR fibers were not present. It is concluded that most TH- and DBH-IR fibers as well as the peptidergic immunoreactive fibers of the pineal body might be originated from the superior cervical ganglia. Some peptidergic immunoreactive fibers, however, might be come from other regions of brain. We also suggest that NPY in pineal body plays a important role for pineal function. The seasonal variation of NPY immunoreactivity indicates that the synthesis and use of NPY may be different between in breeding and non-breeding seasons.

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Development of Peptides from the Germinated Black Rice and Applications as Cosmetics Ingredients (발아 흑미 유래 펩타이드의 개발과 화장품 응용에 대한 연구)

  • Dong-hwan, Lee;Jin-hwa , Kim;Jun-tae, Bae;Sung-min, Park;Hyeong-bae, Pyo;Tae-boo, Choe;Bum-chun, Lee
    • Journal of the Society of Cosmetic Scientists of Korea
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    • v.30 no.2
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    • pp.241-246
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    • 2004
  • To develop novel anti-aging peptides from the germinated black rice, we treated with bromelain, papain and Pronase E. And we investigated the effects of the germinated black rice peptide (GBRP) as anti-aging cosmetic ingredients, and compared with the non-germinated black rice protein (NBRP). We investigated the effects on in vitro inhibition of matrix-metalloprotease (MMP), proliferation of human skin fibroblasts, stimulation of collagen synthesis and expression of UVA-induced MMPs in human skin fibroblasts, UVA induced MMP-1 expression and collagen contents in human skin fibroblasts were analyzed by enzyme-linked immunosorbent assay (ELISA). As a result, the molecular weight distributions of GBRP and NBRP were determined by gel permeation chromatography to be approximately 900 and 10,000 daltons. GBRP increased skin cell proliferation about 40% and reduced UVA-induced MMP-1 expression about 50%. Also the collagen protein level of cells, which were cultured with GBRP, was increased about 25%. These results suggest that the geminated plant seed peptides can be novel anti-aging ingredients for cosmetics.

Analysis of Pine Nut Oil Composition and Its Effects on Obesity (잣기름 성분분석 및 비만 예방효과 연구)

  • Kim, Kyoung Kon;Kang, Yun Hwan;Kim, Dae Jung;Kim, Tae Woo;Choe, Myeon
    • Korean Journal of Food Science and Technology
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    • v.46 no.5
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    • pp.630-635
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    • 2014
  • Pine nut oil (PNO) is well known to impart beneficial effects in overweight individuals, but the mechanisms underlying PNO-mediated weight loss remain unclear. To investigate how PNO promotes weight loss, its composition was determined by gas chromatography coupled with mass spectrometry (GC-MS). In addition, the effects of PNO on cytotoxicity, lipid accumulation, expression of lipid metabolism-related biomarkers, and leptin secretion were assessed in 3T3-L1 cells. GC-MS analyses revealed that PNO contains several components, including linoleic acid, oleic acid, palmitic acid, and stearic acid. Moreover, PNO did not have a cytotoxic effect on 3T3-L1 cells. However, it inhibited the expression of peroxisome proliferator-activated receptor (PPAR) and adipocyte protein 2 (aP2). Finally, PNO significantly increased leptin secretion in a dose-dependent manner. Taken together, these results support the notion that PNO is useful for weight management in overweight individuals.

Effects of Provitamin D on Skin Pigmentation and Immunity (프로 비타민 D 의 피부색 조절 및 면역 효능)

  • Hyunjung Choi;Daejin Min;Eun-Jeong Choi;Seung-Han Park;Hyoung-June Kim;Won-Seok Park
    • Journal of the Society of Cosmetic Scientists of Korea
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    • v.50 no.2
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    • pp.153-161
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    • 2024
  • Vitamin D is a fat-soluble vitamin that is mainly produced in the skin by UV rays. Along with melatonin, it is a representative chronobiotic substance, and the skin plays an important role in distinguishing between day and night. However, vitamin D cannot be used directly in cosmetics because it is a vitamin that acts as a coenzyme and plays a hormonal role in regulating the expression of various types of genes. Therefore, it was to investigate the skin efficacy of provitamin D (7-dehydrocholesterol), a vitamin D precursor that can be used in cosmetics. Our findings reveal that pro vitamin D can effectively inhibit the expression of tyrosinase, the melanin-producing enzyme, thereby attenuating melanin synthesis. This skin tone regulatory effect has been corroborated in vitro using artificial skin models. Additionally, pro vitamin D demonstrated anti-inflammatory properties by suppressing the expression of TNFa and, upon conversion to vitamin D through UV exposure, it was observed to induce the production of the antimicrobial peptide CAMP (LL-37). The inhibitory effect of pro vitamin D on melanin production appears to be a result of it reducing the UV absorption capacity of melanin, thereby inducing the conversion of pro D to vitamin D. Utilizing pro vitamin D in cosmetic formulations could not only modulate skin tone and enhance skin immunity but also expect to contribute to other cutaneous benefits as anti-aging and barrier function improvement with everyday UV exposure. This multifaceted efficacy positions pro vitamin D as a promising ingredient in advancing the formulation of skin care products.

Disturbance of $\alpha$-Amylase Secretion from Bacillus amyloliquefaciens Cells by the Treatment of Puromycin and Magnesium (Bacillus amyloliquefaciens에서 Puromycin 과 Magnesium에 의한 $\alpha$-Amylase 의 분비저해)

  • 안순자;김순옥;이동희;송방호
    • Microbiology and Biotechnology Letters
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    • v.17 no.5
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    • pp.412-420
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    • 1989
  • To know how the ribosomes involved in secretory protein synthesis were attached to the cytoplasmic membrane in Bacillus amyloliquefaciens, the cells were treated with puromycin combinated with magnesium at the logarithmic phase, and the variation of cell-bound and extracellular $\alpha$-amylase activity was assayed for determining the $\alpha$-amylase translocation blocking through the cytoplasmic membrane. In the abnormal $\alpha$-amylase producing mutant in which the C-terminal of the $\alpha$-amylase structure was deleted, B. umytotiquefaciens CH10-2, the $\alpha$-amylase was translocated normally through the cytoplasmic membranes, and the translocation blocking by puromycin was revealed to have a similar pattern as that in the wild type. This means that the C-terminal part of the enzyme structure may not have a signal for secretion. The cell death of the logarithmic phase cells in both strains was not affected much under 20$\mu\textrm{g}$/$m\ell$ of puromycin, however, the $\alpha$-amylase translocation was blocked markedly under less than 10$\mu\textrm{g}$/$m\ell$ of the puromycin concentration. The blocking of the enzyme secretion by puromycin may be due to the detachment of the ribosomes from cytoplasmic membranes by disturbing the nascent polypeptide synthesis. Further evidence for confirming this was that the detachment was increased in 50 mM of magnesium ion because the extracellular $\alpha$-amylase activity was decreased more under this condition. If the cells were treated with trypsin combinated with Iysozyme, the extracellular $\alpha$-amylase activity from the cultured medium was reduced markedly, however, the activity from the cells treated with trypsin only was not reduced. This means that the nascent polypeptides protruding from the cytoplasmic membrane were sensitive to the trypsin digestion, whereas the matured ones were not. Therefore, the protruding polypeptides from the cytoplasmic membranes may be truncated by trypsin before forming their final tertiary structures by folding in the cell wall layer.

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Synthesis and Biological Activities of Myomodulin E and its Analogs (Myomodulin E 및 유도체들의 합성 및 생리활성)

  • Go, Hye-Jin;Seo, Jung-Kil;Seo, Hae-Jeom;Lee, Min-Jeong;Park, Tae-Hyun;Kim, Gun-Do;Park, Nam-Gyu
    • Journal of Life Science
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    • v.22 no.4
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    • pp.499-507
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    • 2012
  • Previous work has characterized myomodulin A (MMA, PMSMLRLamide) and myomodulin E (MME, GLQMLRLamide) purified from the central nervous systems of the sea hare, $Aplysia$ $Kurodai$, using the anterior byssus retractor muscle (ABRM) of the mussel, $Mytilus$ $edulis$. The amino acid sequences of MMA and MME were the same as those of the myomodulin family peptide found in other mollusks. In this study, we synthesized MME, its derivatives, and other neuropeptides to investigate the relationship between the structure and biological activity of MME. The primary structures of MME's derivatives, Des[$Gly^1$]-MME, Des[$Gly^1,Leu^2$]-MME, and Des[$Gly^1,Leu^2,Gln^3$]-MME, were LQMLRLamide, QMLRLamide, and MLRLamide, respectively. MMA and synthetic peptides were tested on ABRM in $M.$ $edulis$ as well as muscle preparations in $Achatina$ $fulica$. MME displayed an inhibitory effect on phasic contraction of the ABRM at $1{\times}10^{-9}$ M or higher. MME also had a relaxing effect on the catch-tension of AMRM at $1{\times}10^{-8}$ M. Both MMA and its analogs stimulated a contractile response on the crop and relaxed the catch-relaxing response on the penial retractor muscle of $A.$ $fulica$. These results suggest that MME and its analogs have modulatory effects on various muscles of mollusks. This study has also laid the groundwork for future neural and circuit modulation studies during animal behavioral changes.

Insulin-like growth factor가 소장 점막 세포 증식에 미치는 영향

  • 윤정한
    • Proceedings of the Korean Nutrition Society Conference
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    • 1995.11b
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    • pp.11-34
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    • 1995
  • Growth hormone (GH) plays a key role in regulating postnatal growth and can stimulate growth of animals by acting directly on specific receptors on the plasma membrane of tissues or indirectly through stimulating insulin-like growth factor (IGF)-I synthesis and secretion by the liver and other tissues. IGF-I and IGF-Ⅱ are polypeptides with structural similarity with proinsulin that stimulate cell proliferation by endocrine, paracrine and autocrine mechanisms. The initial event in the metabolic action of IGFs on target cells appears to be their binding to specific receptors on the plasma membrane. Current evidence indicates that the mitogenic actions of both IGFs are mediated primarily by binding to the type I IGF receptors, and that IGF action is also mediated by interactions with IGF-binding proteins (IGFBPs). Six distinct IGFBPs have been identified that are characterized by cell-specific interaction, transcriptional and post-translational regulation by many different effectors, and the ability to either potentiate or inhibit IGF actions. Nutritional deficiencies can have their devastating consequence during growth. Although IGF-I is the major mediator of GH's action on somatic growth, nutritional status of an organism is a critical regulator of IGF-I and IGFBPs. Various nutrient deficiencies result in decreased serum IGF-I levels and altered IGFBP levels, but the blood levels of GH are generally unchanged or elevated in malnutrition. Effects of protein, energy, vitamin C and D, and zinc on serum IGF and IGFBP levels and tissue mRNA levels were reviewed in the text. Multiple factors are involved in the regulation of intestinal epithelial cell growth and differentiation. Among these factors the nutritional status of individuals is the most important. The intestinal epithelium is an important site for mitogenic action of the IGFs in vivo, with exogenous IGF-I stimulating mucosal hyperplasia. Therefore, the IGF system appears to provide and important mechanism linking nutrition and the proliferation of intestinal epithelial cells. In order to study the detailed mechanisms by which intestinal mucosa is regulated, we have utilized IEC-6 cells, an intestinal epithelial cell line and Caco-2 cells, a human colon adenocarcinoma cell line. Like intestinal crypt cells analyzed in vivo or freshly isolated intestinal epithelial cells, IEC-6 cells and Caco-2 cells possess abundant quatities of both type Ⅰ and type Ⅱ IGF receptors. Exogenous IGFs stimulate, whereas addition of IGFBP-2 inhibits IEC-6 cell proliferation. To investigate whether endogenously secreted IGFBP-2 inhibit proliferation, IEC-6 cells were transfected with a full-length rat IGFBP-2 cDNA anti-sense expression construct. IEC-6 cells transfected with anti-sense IGFBP-2 protein in medium. These cells grew at a rate faster than the control cells indicating that endogenous IGFBP-2 inhibits proliferation of IEC-6 cells, probably by sequestering IGFs. IEC-6 cells express many characteristics of enterocyte, but do not undergo differentiation. On the other hand, Caco-2 cells undergo a spontaneous enterocyte differentiation. On the other hand, Caco-2 cells undergo a spontaneous enterocyte differentiation after reaching confluency. We have demonstrated that Caco-2 cells produce IGF-Ⅱ, IGFBP-2, IGFBP-3, and an as yet unidentified 31,000 Mr IGFBP, and that both mRNA and peptide secretion of IGFBP-2 and IGFBP-3 increased, but IGFBP-4 mRNA and protein secretion decreased after the cells reached confluency. These changes occurred in parallel to and were coincident with differentiation of the cells, as measured by expression of sucrase-isomaltase. In addition, Caco-2 cell clones forced to overexpress IGFBP-4 by transfection with a rat IGFBP-4 cDNA construct exhibited a significantly slower growth rate under serum-free conditions and had increased expression of sucrase-isomaltase compared with vector control cells. These results indicate that IGFBP-4 inhibits proliferation and stimulates differentiation of Caco-2 cells, probably by inhibiting the mitogenic actions of IGFs.

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Anti-wrinkle and Whitening Effects of Essential Oil from Abies koreana (Abies koreana 유래 정유의 항주름 및 미백 효과)

  • Song, Byeong-Wook;Song, Min-Jeong;Park, Mi-Jin;Choi, Don-Ha;Lee, Sung-Suk;Kim, Myungkil;Hwang, Ki-Chul;Kim, Il-Kwon
    • Journal of Life Science
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    • v.28 no.5
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    • pp.524-531
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    • 2018
  • The essential oil from Abies koreana E.H. Wilson had been developed, however, its efficacy has not yet been studied especially in terms of skin care research. The aim of this study is to investigate the effects of Abies koreana extracts (AKE) on melanogenesis and wrinkle formation in B16F10 melanoma cells (B16F10) and human dermal fibroblast cell line (HDF). The essential oil was extracted by hydrodistillation method and purified by anhydrous sodium sulfate. At a concentration of $10^{-5}$-fold, viability in these cells had been defined by cytotoxicity assays. Anti-melanogenic effects on B16F10 were evaluated using tyrosinase inhibition assay, and real-time PCR for verifying gene expression of tyrosinase, tyrosinase related protein-1 and -2 (TRP-1 and -2). AKEs reduced about 5-fold of tyrosinase inhibitory activity compared to ${\alpha}$-melanocyte-stimulating hormone (${\alpha}$-MSH)-induced group and about 30% reduction compared to Arbutin induced group. The mRNA levels of three melanin-related factors were increased, separately. To investigate the effects of anti-wrinkle, procollagen type I c peptide synthesis assay (PIP) and Western blot were performed. At AKE-treated group, PIP was up-regulated and the expression of collagen type 1 and matrix metalloproteinase (MMP)-1 were improved. Furthermore, AKE presented anti-wrinkle effects by increasing UVB-inhibited collagen type 1 expression, and reducing UVB-induced MMP-1 production at $60mJ/cm^2$ of UVB radiation. Therefore, Abies koreana extracts has potentials as a safe and an effective skin ingredient for whitening and anti-wrinkle.

Roles of the Insulin-like Growth Factor System in the Reproductive Function;Uterine Connection (Insulin-like Growth Factor Systems의 생식기능에서의 역할;자궁편)

  • Lee, Chul-Young
    • Clinical and Experimental Reproductive Medicine
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    • v.23 no.3
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    • pp.247-268
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    • 1996
  • It has been known for a long time that gonadotropins and steroid hormones play a pivotal role in a series of reproductive biological phenomena including the maturation of ovarian follicles and oocytes, ovulation and implantation, maintenance of pregnancy and fetal growth & development, parturition and mammary development and lactation. Recent investigations, however, have elucidated that in addition to these classic hormones, multiple growth factors also are involved in these phenomena. Most growth factors in reproductive organs mediate the actions of gonadotropins and steroid hormones or synergize with them in an autocrine/paracrine manner. The insulin-like growth factor(IGF) system, which is one of the most actively investigated areas lately in the reproductive organs, has been found to have important roles in a wide gamut of reproductive phenomena. In the present communication, published literature pertaining to the intrauterine IGF system will be reviewed preceded by general information of the IGF system. The IGF family comprises of IGF-I & IGF-II ligands, two types of IGF receptors and six classes of IGF-binding proteins(IGFBPs) that are known to date. IGF-I and IGF-II peptides, which are structurally homologous to proinsulin, possess the insulin-like activity including the stimulatory effect of glucose and amino acid transport. Besides, IGFs as mitogens stimulate cell division, and also play a role in cellular differentiation and functions in a variety of cell lines. IGFs are expressed mainly in the liver and messenchymal cells, and act on almost all types of tissues in an autocrine/paracrine as well as endocrine mode. There are two types of IGF receptors. Type I IGF receptors, which are tyrosine kinase receptors having high-affinity for IGF-I and IGF-II, mediate almost all the IGF actions that are described above. Type II IGF receptors or IGF-II/mannose-6-phosphate receptors have two distinct binding sites; the IGF-II binding site exhibits a high affinity only for IGF-II. The principal role of the type II IGF receptor is to destroy IGF-II by targeting the ligand to the lysosome. IGFs in biological fluids are mostly bound to IGFBP. IGFBPs, in general, are IGF storage/carrier proteins or modulators of IGF actions; however, as for distinct roles for individual IGFBPs, only limited information is available. IGFBPs inhibit IGF actions under most in vitro situations, seemingly because affinities of IGFBPs for IGFs are greater than those of IGF receptors. How IGF is released from IGFBP to reach IGF receptors is not known; however, various IGFBP protease activities that are present in blood and interstitial fluids are believed to play an important role in the process of IGF release from the IGFBP. According to latest reports, there is evidence that under certain in vitro circumstances, IGFBP-1, -3, -5 have their own biological activities independent of the IGF. This may add another dimension of complexity of the already complicated IGF system. Messenger ribonucleic acids and proteins of the IGF family members are expressed in the uterine tissue and conceptus of the primates, rodents and farm animals to play important roles in growth and development of the uterus and fetus. Expression of the uterine IGF system is regulated by gonadal hormones and local regulatory substances with temporal and spatial specificities. Locally expressed IGFs and IGFBPs act on the uterine tissue in an autocrine/paracrine manner, or are secreted into the uterine lumen to participate in conceptus growth and development. Conceptus also expresses the IGF system beginning from the peri-implantation period. When an IGF family member is expressed in the conceptus, however, is determined by the presence or absence of maternally inherited mRNAs, genetic programming of the conceptus itself and an interaction with the maternal tissue. The site of IGF action also follows temporal (physiological status) and spatial specificities. These facts that expression of the IGF system is temporally and spatially regulated support indirectly a hypothesis that IGFs play a role in conceptus growth and development. Uterine and conceptus-derived IGFs stimulate cell division and differentiation, glucose and amino acid transport, general protein synthesis and the biosynthesis of mammotropic hormones including placental lactogen and prolactin, and also play a role in steroidogenesis. The suggested role for IGFs in conceptus growth and development has been proven by the result of IGF-I, IGF-II or IGF receptor gene disruption(targeting) of murine embryos by the homologous recombination technique. Mice carrying a null mutation for IGF-I and/or IGF-II or type I IGF receptor undergo delayed prenatal and postnatal growth and development with 30-60% normal weights at birth. Moreover, mice lacking the type I IGF receptor or IGF-I plus IGF-II die soon after birth. Intrauterine IGFBPs generally are believed to sequester IGF ligands within the uterus or to play a role of negative regulators of IGF actions by inhibiting IGF binding to cognate receptors. However, when it is taken into account that IGFBP-1 is expressed and secreted in primate uteri in amounts assessedly far exceeding those of local IGFs and that IGFBP-1 is one of the major secretory proteins of the primate decidua, the possibility that this IGFBP may have its own biological activity independent of IGF cannot be excluded. Evidently, elucidating the exact role of each IGFBP is an essential step into understanding the whole IGF system. As such, further research in this area is awaited with a lot of anticipation and attention.

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