Neuropeptide and gut hormone that helps regulate GASTRIC ACID secretion and motor function. Once released from nerves in the antrum of the STOMACH, the neuropeptide stimulates release of GASTRIN from the GASTRIN-SECRETING CELLS.
Cell surface receptors that bind signalling molecules released by neurons and convert these signals into intracellular changes influencing the behavior of cells. Neurotransmitter is used here in its most general sense, including not only messengers that act to regulate ion channels, but also those which act on second messenger systems and those which may act at a distance from their release sites. Included are receptors for neuromodulators, neuroregulators, neuromediators, and neurohumors, whether or not located at synapses.
Members of the class of compounds composed of AMINO ACIDS joined together by peptide bonds between adjacent amino acids into linear, branched or cyclical structures. OLIGOPEPTIDES are composed of approximately 2-12 amino acids. Polypeptides are composed of approximately 13 or more amino acids. PROTEINS are linear polypeptides that are normally synthesized on RIBOSOMES.
A peptide, of about 33 amino acids, secreted by the upper INTESTINAL MUCOSA and also found in the central nervous system. It causes gallbladder contraction, release of pancreatic exocrine (or digestive) enzymes, and affects other gastrointestinal functions. Cholecystokinin may be the mediator of satiety.
A family of gastrointestinal peptide hormones that excite the secretion of GASTRIC JUICE. They may also occur in the central nervous system where they are presumed to be neurotransmitters.
Cell lines whose original growing procedure consisted being transferred (T) every 3 days and plated at 300,000 cells per plate (J Cell Biol 17:299-313, 1963). Lines have been developed using several different strains of mice. Tissues are usually fibroblasts derived from mouse embryos but other types and sources have been developed as well. The 3T3 lines are valuable in vitro host systems for oncogenic virus transformation studies, since 3T3 cells possess a high sensitivity to CONTACT INHIBITION.
An order of the class Amphibia, which includes several families of frogs and toads. They are characterized by well developed hind limbs adapted for jumping, fused head and trunk and webbed toes. The term "toad" is ambiguous and is properly applied only to the family Bufonidae.
A nodular organ in the ABDOMEN that contains a mixture of ENDOCRINE GLANDS and EXOCRINE GLANDS. The small endocrine portion consists of the ISLETS OF LANGERHANS secreting a number of hormones into the blood stream. The large exocrine portion (EXOCRINE PANCREAS) is a compound acinar gland that secretes several digestive enzymes into the pancreatic ductal system that empties into the DUODENUM.
A group of amylolytic enzymes that cleave starch, glycogen, and related alpha-1,4-glucans. (Stedman, 25th ed) EC 3.2.1.-.
Antidiuretic hormones released by the NEUROHYPOPHYSIS of all vertebrates (structure varies with species) to regulate water balance and OSMOLARITY. In general, vasopressin is a nonapeptide consisting of a six-amino-acid ring with a cysteine 1 to cysteine 6 disulfide bridge or an octapeptide containing a CYSTINE. All mammals have arginine vasopressin except the pig with a lysine at position 8. Vasopressin, a vasoconstrictor, acts on the KIDNEY COLLECTING DUCTS to increase water reabsorption, increase blood volume and blood pressure.
A peptide extracted from the posterior salivary glands of certain small octopi (Eledone spp., Mollusca), or obtained by synthesis. Its actions resemble those of SUBSTANCE P; it is a potent vasodilator and increases capillary permeability. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1364)
HORMONES secreted by the gastrointestinal mucosa that affect the timing or the quality of secretion of digestive enzymes, and regulate the motor activity of the digestive system organs.
A specific decapeptide obtained from the skin of Hila caerulea, an Australian amphibian. Caerulein is similar in action and composition to CHOLECYSTOKININ. It stimulates gastric, biliary, and pancreatic secretion; and certain smooth muscle. It is used in paralytic ileus and as diagnostic aid in pancreatic malfunction.
An octapeptide hormone present in the intestine and brain. When secreted from the gastric mucosa, it stimulates the release of bile from the gallbladder and digestive enzymes from the pancreas.
Abnormal passage communicating with the STOMACH.
A derivative of benzodiazepine that acts on the cholecystokinin A (CCKA) receptor to antagonize CCK-8's (SINCALIDE) physiological and behavioral effects, such as pancreatic stimulation and inhibition of feeding.
A phorbol ester found in CROTON OIL which, in addition to being a potent skin tumor promoter, is also an effective activator of calcium-activated, phospholipid-dependent protein kinase (protein kinase C). Due to its activation of this enzyme, phorbol 12,13-dibutyrate profoundly affects many different biological systems.
An eleven-amino acid neurotransmitter that appears in both the central and peripheral nervous systems. It is involved in transmission of PAIN, causes rapid contractions of the gastrointestinal smooth muscle, and modulates inflammatory and immune responses.
A 14-amino acid peptide named for its ability to inhibit pituitary GROWTH HORMONE release, also called somatotropin release-inhibiting factor. It is expressed in the central and peripheral nervous systems, the gut, and other organs. SRIF can also inhibit the release of THYROID-STIMULATING HORMONE; PROLACTIN; INSULIN; and GLUCAGON besides acting as a neurotransmitter and neuromodulator. In a number of species including humans, there is an additional form of somatostatin, SRIF-28 with a 14-amino acid extension at the N-terminal.
Rapidly decreasing response to a drug or physiologically active agent after administration of a few doses. In immunology, it is the rapid immunization against the effect of toxic doses of an extract or serum by previous injection of small doses. (Dorland, 28th ed)
A biologically active tridecapeptide isolated from the hypothalamus. It has been shown to induce hypotension in the rat, to stimulate contraction of guinea pig ileum and rat uterus, and to cause relaxation of rat duodenum. There is also evidence that it acts as both a peripheral and a central nervous system neurotransmitter.
Phosphoric acid esters of inositol. They include mono- and polyphosphoric acid esters, with the exception of inositol hexaphosphate which is PHYTIC ACID.
The rate dynamics in chemical or physical systems.
An anaplastic, highly malignant, and usually bronchogenic carcinoma composed of small ovoid cells with scanty neoplasm. It is characterized by a dominant, deeply basophilic nucleus, and absent or indistinct nucleoli. (From Stedman, 25th ed; Holland et al., Cancer Medicine, 3d ed, p1286-7)
An serine-threonine protein kinase that requires the presence of physiological concentrations of CALCIUM and membrane PHOSPHOLIPIDS. The additional presence of DIACYLGLYCEROLS markedly increases its sensitivity to both calcium and phospholipids. The sensitivity of the enzyme can also be increased by PHORBOL ESTERS and it is believed that protein kinase C is the receptor protein of tumor-promoting phorbol esters.
A basic element found in nearly all organized tissues. It is a member of the alkaline earth family of metals with the atomic symbol Ca, atomic number 20, and atomic weight 40. Calcium is the most abundant mineral in the body and combines with phosphorus to form calcium phosphate in the bones and teeth. It is essential for the normal functioning of nerves and muscles and plays a role in blood coagulation (as factor IV) and in many enzymatic processes.
A drug that exerts an inhibitory effect on gastric secretion and reduces gastrointestinal motility. It is used clinically in the drug therapy of gastrointestinal ulcers.
An oligopeptide isolated from the skin of Physalaemus fuscumaculatus, a South American frog. It is a typical kinin, resembling SUBSTANCE P in structure and action and has been proposed as a sialagogue, antihypertensive, and vasodilator.
A peptide hormone of about 27 amino acids from the duodenal mucosa that activates pancreatic secretion and lowers the blood sugar level. (USAN and the USP Dictionary of Drug Names, 1994, p597)
Mitogenic peptide growth hormone carried in the alpha-granules of platelets. It is released when platelets adhere to traumatized tissues. Connective tissue cells near the traumatized region respond by initiating the process of replication.
The region between the sharp indentation at the lower third of the STOMACH (incisura angularis) and the junction of the PYLORUS with the DUODENUM. Pyloric antral glands contain mucus-secreting cells and gastrin-secreting endocrine cells (G CELLS).
Substances that stimulate mitosis and lymphocyte transformation. They include not only substances associated with LECTINS, but also substances from streptococci (associated with streptolysin S) and from strains of alpha-toxin-producing staphylococci. (Stedman, 25th ed)
A serine proteinase inhibitor used therapeutically in the treatment of pancreatitis, disseminated intravascular coagulation (DIC), and as a regional anticoagulant for hemodialysis. The drug inhibits the hydrolytic effects of thrombin, plasmin, and kallikrein, but not of chymotrypsin and aprotinin.
A synthetic pentapeptide that has effects like gastrin when given parenterally. It stimulates the secretion of gastric acid, pepsin, and intrinsic factor, and has been used as a diagnostic aid.
The interaction of two or more substrates or ligands with the same binding site. The displacement of one by the other is used in quantitative and selective affinity measurements.
The fission of a CELL. It includes CYTOKINESIS, when the CYTOPLASM of a cell is divided, and CELL NUCLEUS DIVISION.
Hydrochloric acid present in GASTRIC JUICE.
A subclass of IMIDES with the general structure of pyrrolidinedione. They are prepared by the distillation of ammonium succinate. They are sweet-tasting compounds that are used as chemical intermediates and plant growth stimulants.
A non-receptor protein tyrosine kinase that is localized to FOCAL ADHESIONS and is a central component of integrin-mediated SIGNAL TRANSDUCTION PATHWAYS. Focal adhesion kinase 1 interacts with PAXILLIN and undergoes PHOSPHORYLATION in response to adhesion of cell surface integrins to the EXTRACELLULAR MATRIX. Phosphorylated p125FAK protein binds to a variety of SH2 DOMAIN and SH3 DOMAIN containing proteins and helps regulate CELL ADHESION and CELL MIGRATION.
Unstable isotopes of iodine that decay or disintegrate emitting radiation. I atoms with atomic weights 117-139, except I 127, are radioactive iodine isotopes.
Peptides composed of between two and twelve amino acids.
Cell surface proteins that bind cholecystokinin (CCK) with high affinity and trigger intracellular changes influencing the behavior of cells. Cholecystokinin receptors are activated by GASTRIN as well as by CCK-4; CCK-8; and CCK-33. Activation of these receptors evokes secretion of AMYLASE by pancreatic acinar cells, acid and PEPSIN by stomach mucosal cells, and contraction of the PYLORUS and GALLBLADDER. The role of the widespread CCK receptors in the central nervous system is not well understood.
Mutant mice homozygous for the recessive gene "nude" which fail to develop a thymus. They are useful in tumor studies and studies on immune responses.
The order of amino acids as they occur in a polypeptide chain. This is referred to as the primary structure of proteins. It is of fundamental importance in determining PROTEIN CONFORMATION.
Cells grown in vitro from neoplastic tissue. If they can be established as a TUMOR CELL LINE, they can be propagated in cell culture indefinitely.
Beta-Sulfoalanine. An amino acid with a C-terminal sulfonic acid group which has been isolated from human hair oxidized with permanganate. It occurs normally in the outer part of the sheep's fleece, where the wool is exposed to light and weather.
An alkaloid, originally from Atropa belladonna, but found in other plants, mainly SOLANACEAE. Hyoscyamine is the 3(S)-endo isomer of atropine.
Partial proteins formed by partial hydrolysis of complete proteins or generated through PROTEIN ENGINEERING techniques.
Preparations made from animal tissues or organs (ANIMAL STRUCTURES). They usually contain many components, any one of which may be pharmacologically or physiologically active. Tissue extracts may contain specific, but uncharacterized factors or proteins with specific actions.
Tumor-promoting compounds obtained from CROTON OIL (Croton tiglium). Some of these are used in cell biological experiments as activators of protein kinase C.
Unstable isotopes of copper that decay or disintegrate emitting radiation. Cu atoms with atomic weights 58-62, 64, and 66-68 are radioactive copper isotopes.
Established cell cultures that have the potential to propagate indefinitely.
Lutetium. An element of the rare earth family of metals. It has the atomic symbol Lu, atomic number 71, and atomic weight 175.
Techniques for labeling a substance with a stable or radioactive isotope. It is not used for articles involving labeled substances unless the methods of labeling are substantively discussed. Tracers that may be labeled include chemical substances, cells, or microorganisms.
A class of organic compounds containing a ring structure made up of more than one kind of atom, usually carbon plus another atom. The ring structure can be aromatic or nonaromatic.
A subclass of phospholipases that hydrolyze the phosphoester bond found in the third position of GLYCEROPHOSPHOLIPIDS. Although the singular term phospholipase C specifically refers to an enzyme that catalyzes the hydrolysis of PHOSPHATIDYLCHOLINE (EC 3.1.4.3), it is commonly used in the literature to refer to broad variety of enzymes that specifically catalyze the hydrolysis of PHOSPHATIDYLINOSITOLS.
Locomotor behavior not involving a steering reaction, but in which there may be a turning random in direction. It includes orthokinesis, the rate of movement and klinokinesis, the amount of turning, which are related to the intensity of stimulation.
A 36-amino acid pancreatic hormone that is secreted mainly by endocrine cells found at the periphery of the ISLETS OF LANGERHANS and adjacent to cells containing SOMATOSTATIN and GLUCAGON. Pancreatic polypeptide (PP), when administered peripherally, can suppress gastric secretion, gastric emptying, pancreatic enzyme secretion, and appetite. A lack of pancreatic polypeptide (PP) has been associated with OBESITY in rats and mice.
A family of non-receptor, PROLINE-rich protein-tyrosine kinases.
A fungal metabolite that blocks cytoplasmic cleavage by blocking formation of contractile microfilament structures resulting in multinucleated cell formation, reversible inhibition of cell movement, and the induction of cellular extrusion. Additional reported effects include the inhibition of actin polymerization, DNA synthesis, sperm motility, glucose transport, thyroid secretion, and growth hormone release.
Descriptions of specific amino acid, carbohydrate, or nucleotide sequences which have appeared in the published literature and/or are deposited in and maintained by databanks such as GENBANK, European Molecular Biology Laboratory (EMBL), National Biomedical Research Foundation (NBRF), or other sequence repositories.
Protein kinases that catalyze the PHOSPHORYLATION of TYROSINE residues in proteins with ATP or other nucleotides as phosphate donors.
A phorbol ester found in CROTON OIL with very effective tumor promoting activity. It stimulates the synthesis of both DNA and RNA.
Cell lines developed from disaggregated BALB/c mouse embryos. They are extremely sensitive to CONTACT INHIBITION, and highly susceptible to transformation by SV40 VIRUS and murine sarcoma virus (SARCOMA VIRUSES, MURINE).
A 6-kDa polypeptide growth factor initially discovered in mouse submaxillary glands. Human epidermal growth factor was originally isolated from urine based on its ability to inhibit gastric secretion and called urogastrone. Epidermal growth factor exerts a wide variety of biological effects including the promotion of proliferation and differentiation of mesenchymal and EPITHELIAL CELLS. It is synthesized as a transmembrane protein which can be cleaved to release a soluble active form.
Conversion of an inactive form of an enzyme to one possessing metabolic activity. It includes 1, activation by ions (activators); 2, activation by cofactors (coenzymes); and 3, conversion of an enzyme precursor (proenzyme or zymogen) to an active enzyme.
The relationship between the dose of an administered drug and the response of the organism to the drug.
A stable synthetic analog of methionine enkephalin (ENKEPHALIN, METHIONINE). Actions are similar to those of methionine enkephalin. Its effects can be reversed by narcotic antagonists such as naloxone.
Peptides released by NEURONS as intercellular messengers. Many neuropeptides are also hormones released by non-neuronal cells.
Inorganic salts that contain the -HCO3 radical. They are an important factor in determining the pH of the blood and the concentration of bicarbonate ions is regulated by the kidney. Levels in the blood are an index of the alkali reserve or buffering capacity.
A contrast medium in diagnostic radiology with properties similar to those of diatrizoic acid. It is used primarily as its sodium and meglumine (IOTHALAMATE MEGLUMINE) salts.
The introduction of a phosphoryl group into a compound through the formation of an ester bond between the compound and a phosphorus moiety.
21-Amino-acid peptides produced by vascular endothelial cells and functioning as potent vasoconstrictors. The endothelin family consists of three members, ENDOTHELIN-1; ENDOTHELIN-2; and ENDOTHELIN-3. All three peptides contain 21 amino acids, but vary in amino acid composition. The three peptides produce vasoconstrictor and pressor responses in various parts of the body. However, the quantitative profiles of the pharmacological activities are considerably different among the three isopeptides.
The study of the chemical and physical phenomena of radioactive substances.
Substances used for their pharmacological actions on any aspect of neurotransmitter systems. Neurotransmitter agents include agonists, antagonists, degradation inhibitors, uptake inhibitors, depleters, precursors, and modulators of receptor function.
A cyclized derivative of L-GLUTAMIC ACID. Elevated blood levels may be associated with problems of GLUTAMINE or GLUTATHIONE metabolism.
The domestic dog, Canis familiaris, comprising about 400 breeds, of the carnivore family CANIDAE. They are worldwide in distribution and live in association with people. (Walker's Mammals of the World, 5th ed, p1065)
A highly basic, 28 amino acid neuropeptide released from intestinal mucosa. It has a wide range of biological actions affecting the cardiovascular, gastrointestinal, and respiratory systems and is neuroprotective. It binds special receptors (RECEPTORS, VASOACTIVE INTESTINAL PEPTIDE).
Compounds that are used in medicine as sources of radiation for radiotherapy and for diagnostic purposes. They have numerous uses in research and industry. (Martindale, The Extra Pharmacopoeia, 30th ed, p1161)
Tumors or cancer of the PROSTATE.
Guanosine 5'-(trihydrogen diphosphate), monoanhydride with phosphorothioic acid. A stable GTP analog which enjoys a variety of physiological actions such as stimulation of guanine nucleotide-binding proteins, phosphoinositide hydrolysis, cyclic AMP accumulation, and activation of specific proto-oncogenes.
Salts and esters of hippuric acid.
Derivatives of phosphatidic acids in which the phosphoric acid is bound in ester linkage to the hexahydroxy alcohol, myo-inositol. Complete hydrolysis yields 1 mole of glycerol, phosphoric acid, myo-inositol, and 2 moles of fatty acids.
A non-essential amino acid. In animals it is synthesized from PHENYLALANINE. It is also the precursor of EPINEPHRINE; THYROID HORMONES; and melanin.
A cell line established in 1962 from disaggregated Swiss albino mouse embryos. This fibroblast cell line is extremely popular in research.
Regulatory proteins that act as molecular switches. They control a wide range of biological processes including: receptor signaling, intracellular signal transduction pathways, and protein synthesis. Their activity is regulated by factors that control their ability to bind to and hydrolyze GTP to GDP. EC 3.6.1.-.
The amount of a substance secreted by cells or by a specific organ or organism over a given period of time; usually applies to those substances which are formed by glandular tissues and are released by them into biological fluids, e.g., secretory rate of corticosteroids by the adrenal cortex, secretory rate of gastric acid by the gastric mucosa.
Agents, usually topical, that relieve itching (pruritus).
Accumulation of a drug or chemical substance in various organs (including those not relevant to its pharmacologic or therapeutic action). This distribution depends on the blood flow or perfusion rate of the organ, the ability of the drug to penetrate organ membranes, tissue specificity, protein binding. The distribution is usually expressed as tissue to plasma ratios.
A 51-amino acid pancreatic hormone that plays a major role in the regulation of glucose metabolism, directly by suppressing endogenous glucose production (GLYCOGENOLYSIS; GLUCONEOGENESIS) and indirectly by suppressing GLUCAGON secretion and LIPOLYSIS. Native insulin is a globular protein comprised of a zinc-coordinated hexamer. Each insulin monomer containing two chains, A (21 residues) and B (30 residues), linked by two disulfide bonds. Insulin is used as a drug to control insulin-dependent diabetes mellitus (DIABETES MELLITUS, TYPE 1).
A nonapeptide messenger that is enzymatically produced from KALLIDIN in the blood where it is a potent but short-lived agent of arteriolar dilation and increased capillary permeability. Bradykinin is also released from MAST CELLS during asthma attacks, from gut walls as a gastrointestinal vasodilator, from damaged tissues as a pain signal, and may be a neurotransmitter.
Classic quantitative assay for detection of antigen-antibody reactions using a radioactively labeled substance (radioligand) either directly or indirectly to measure the binding of the unlabeled substance to a specific antibody or other receptor system. Non-immunogenic substances (e.g., haptens) can be measured if coupled to larger carrier proteins (e.g., bovine gamma-globulin or human serum albumin) capable of inducing antibody formation.
Connective tissue cells which secrete an extracellular matrix rich in collagen and other macromolecules.
The increase in a measurable parameter of a PHYSIOLOGICAL PROCESS, including cellular, microbial, and plant; immunological, cardiovascular, respiratory, reproductive, urinary, digestive, neural, musculoskeletal, ocular, and skin physiological processes; or METABOLIC PROCESS, including enzymatic and other pharmacological processes, by a drug or other chemical.
A common name used for the genus Cavia. The most common species is Cavia porcellus which is the domesticated guinea pig used for pets and biomedical research.
A 27-amino acid peptide with histidine at the N-terminal and isoleucine amide at the C-terminal. The exact amino acid composition of the peptide is species dependent. The peptide is secreted in the intestine, but is found in the nervous system, many organs, and in the majority of peripheral tissues. It has a wide range of biological actions, affecting the cardiovascular, gastrointestinal, respiratory, and central nervous systems.
Genetically identical individuals developed from brother and sister matings which have been carried out for twenty or more generations or by parent x offspring matings carried out with certain restrictions. This also includes animals with a long history of closed colony breeding.
The outer covering of the body that protects it from the environment. It is composed of the DERMIS and the EPIDERMIS.
An amino acid that occurs in endogenous proteins. Tyrosine phosphorylation and dephosphorylation plays a role in cellular signal transduction and possibly in cell growth control and carcinogenesis.
A storage reservoir for BILE secretion. Gallbladder allows the delivery of bile acids at a high concentration and in a controlled manner, via the CYSTIC DUCT to the DUODENUM, for degradation of dietary lipid.
Injections into the cerebral ventricles.
Cell surface proteins that bind somatostatin and trigger intracellular changes which influence the behavior of cells. Somatostatin is a hypothalamic hormone, a pancreatic hormone, and a central and peripheral neurotransmitter. Activated somatostatin receptors on pituitary cells inhibit the release of growth hormone; those on endocrine and gastrointestinal cells regulate the absorption and utilization of nutrients; and those on neurons mediate somatostatin's role as a neurotransmitter.
Intracellular messenger formed by the action of phospholipase C on phosphatidylinositol 4,5-bisphosphate, which is one of the phospholipids that make up the cell membrane. Inositol 1,4,5-trisphosphate is released into the cytoplasm where it releases calcium ions from internal stores within the cell's endoplasmic reticulum. These calcium ions stimulate the activity of B kinase or calmodulin.
Inorganic compounds that contain aluminum as an integral part of the molecule.
Tumors or cancer of the LUNG.
Nucleotides in which the base moiety is substituted with one or more sulfur atoms.
The fluid containing digestive enzymes secreted by the pancreas in response to food in the duodenum.
Ducts that collect PANCREATIC JUICE from the PANCREAS and supply it to the DUODENUM.
The liquid secretion of the stomach mucosa consisting of hydrochloric acid (GASTRIC ACID); PEPSINOGENS; INTRINSIC FACTOR; GASTRIN; MUCUS; and the bicarbonate ion (BICARBONATES). (From Best & Taylor's Physiological Basis of Medical Practice, 12th ed, p651)
The process by which a DNA molecule is duplicated.
Cells found throughout the lining of the GASTROINTESTINAL TRACT that contain and secrete regulatory PEPTIDE HORMONES and/or BIOGENIC AMINES.
A set of BACTERIAL ADHESINS and TOXINS, BIOLOGICAL produced by BORDETELLA organisms that determine the pathogenesis of BORDETELLA INFECTIONS, such as WHOOPING COUGH. They include filamentous hemagglutinin; FIMBRIAE PROTEINS; pertactin; PERTUSSIS TOXIN; ADENYLATE CYCLASE TOXIN; dermonecrotic toxin; tracheal cytotoxin; Bordetella LIPOPOLYSACCHARIDES; and tracheal colonization factor.
Compounds containing the hexamethylenebis(trimethylammonium) cation. Members of this group frequently act as antihypertensive agents and selective ganglionic blocking agents.
The intracellular transfer of information (biological activation/inhibition) through a signal pathway. In each signal transduction system, an activation/inhibition signal from a biologically active molecule (hormone, neurotransmitter) is mediated via the coupling of a receptor/enzyme to a second messenger system or to an ion channel. Signal transduction plays an important role in activating cellular functions, cell differentiation, and cell proliferation. Examples of signal transduction systems are the GAMMA-AMINOBUTYRIC ACID-postsynaptic receptor-calcium ion channel system, the receptor-mediated T-cell activation pathway, and the receptor-mediated activation of phospholipases. Those coupled to membrane depolarization or intracellular release of calcium include the receptor-mediated activation of cytotoxic functions in granulocytes and the synaptic potentiation of protein kinase activation. Some signal transduction pathways may be part of larger signal transduction pathways; for example, protein kinase activation is part of the platelet activation signal pathway.
Experimental transplantation of neoplasms in laboratory animals for research purposes.
A subfamily in the family MURIDAE, comprising the hamsters. Four of the more common genera are Cricetus, CRICETULUS; MESOCRICETUS; and PHODOPUS.
Linear POLYPEPTIDES that are synthesized on RIBOSOMES and may be further modified, crosslinked, cleaved, or assembled into complex proteins with several subunits. The specific sequence of AMINO ACIDS determines the shape the polypeptide will take, during PROTEIN FOLDING, and the function of the protein.
A malignant neoplasm derived from glandular epithelium, in which cystic accumulations of retained secretions are formed. The neoplastic cells manifest varying degrees of anaplasia and invasiveness, and local extension and metastases occur. Cystadenocarcinomas develop frequently in the ovaries, where pseudomucinous and serous types are recognized. (Stedman, 25th ed)
Lining of the STOMACH, consisting of an inner EPITHELIUM, a middle LAMINA PROPRIA, and an outer MUSCULARIS MUCOSAE. The surface cells produce MUCUS that protects the stomach from attack by digestive acid and enzymes. When the epithelium invaginates into the LAMINA PROPRIA at various region of the stomach (CARDIA; GASTRIC FUNDUS; and PYLORUS), different tubular gastric glands are formed. These glands consist of cells that secrete mucus, enzymes, HYDROCHLORIC ACID, or hormones.
RNA sequences that serve as templates for protein synthesis. Bacterial mRNAs are generally primary transcripts in that they do not require post-transcriptional processing. Eukaryotic mRNA is synthesized in the nucleus and must be exported to the cytoplasm for translation. Most eukaryotic mRNAs have a sequence of polyadenylic acid at the 3' end, referred to as the poly(A) tail. The function of this tail is not known for certain, but it may play a role in the export of mature mRNA from the nucleus as well as in helping stabilize some mRNA molecules by retarding their degradation in the cytoplasm.
A nonselective alpha-adrenergic antagonist. It is used in the treatment of hypertension and hypertensive emergencies, pheochromocytoma, vasospasm of RAYNAUD DISEASE and frostbite, clonidine withdrawal syndrome, impotence, and peripheral vascular disease.
Tumors or cancer of the DUODENUM.
Inflammation of the MUCOSA of both the SMALL INTESTINE and the LARGE INTESTINE. Etiology includes ISCHEMIA, infections, allergic, and immune responses.
Antineoplastic agent that is also used as a veterinary anesthetic. It has also been used as an intermediate in organic synthesis. Urethane is suspected to be a carcinogen.
A class of compounds composed of repeating 5-carbon units of HEMITERPENES.
The sum of the weight of all the atoms in a molecule.
An ENTEROTOXIN from VIBRIO CHOLERAE. It consists of two major protomers, the heavy (H) or A subunit and the B protomer which consists of 5 light (L) or B subunits. The catalytic A subunit is proteolytically cleaved into fragments A1 and A2. The A1 fragment is a MONO(ADP-RIBOSE) TRANSFERASE. The B protomer binds cholera toxin to intestinal epithelial cells, and facilitates the uptake of the A1 fragment. The A1 catalyzed transfer of ADP-RIBOSE to the alpha subunits of heterotrimeric G PROTEINS activates the production of CYCLIC AMP. Increased levels of cyclic AMP are thought to modulate release of fluid and electrolytes from intestinal crypt cells.
Cells propagated in vitro in special media conducive to their growth. Cultured cells are used to study developmental, morphologic, metabolic, physiologic, and genetic processes, among others.
One of the virulence factors produced by BORDETELLA PERTUSSIS. It is a multimeric protein composed of five subunits S1 - S5. S1 contains mono ADPribose transferase activity.
Quantitative determination of receptor (binding) proteins in body fluids or tissue using radioactively labeled binding reagents (e.g., antibodies, intracellular receptors, plasma binders).
A deoxyribonucleotide polymer that is the primary genetic material of all cells. Eukaryotic and prokaryotic organisms normally contain DNA in a double-stranded state, yet several important biological processes transiently involve single-stranded regions. DNA, which consists of a polysugar-phosphate backbone possessing projections of purines (adenine and guanine) and pyrimidines (thymine and cytosine), forms a double helix that is held together by hydrogen bonds between these purines and pyrimidines (adenine to thymine and guanine to cytosine).
Paxillin is a signal transducing adaptor protein that localizes to FOCAL ADHESIONS via its four LIM domains. It undergoes PHOSPHORYLATION in response to integrin-mediated CELL ADHESION, and interacts with a variety of proteins including VINCULIN; FOCAL ADHESION KINASE; PROTO-ONCOGENE PROTEIN PP60(C-SRC); and PROTO-ONCOGENE PROTEIN C-CRK.
A molecule that binds to another molecule, used especially to refer to a small molecule that binds specifically to a larger molecule, e.g., an antigen binding to an antibody, a hormone or neurotransmitter binding to a receptor, or a substrate or allosteric effector binding to an enzyme. Ligands are also molecules that donate or accept a pair of electrons to form a coordinate covalent bond with the central metal atom of a coordination complex. (From Dorland, 27th ed)
The interruption or removal of any part of the vagus (10th cranial) nerve. Vagotomy may be performed for research or for therapeutic purposes.
The oldest recognized genus of the family PASTEURELLACEAE. It consists of several species. Its organisms occur most frequently as coccobacillus or rod-shaped and are gram-negative, nonmotile, facultative anaerobes. Species of this genus are found in both animals and humans.
The prototypical antimalarial agent with a mechanism that is not well understood. It has also been used to treat rheumatoid arthritis, systemic lupus erythematosus, and in the systemic therapy of amebic liver abscesses.
The consumption of edible substances.
Isotopes that exhibit radioactivity and undergo radioactive decay. (From Grant & Hackh's Chemical Dictionary, 5th ed & McGraw-Hill Dictionary of Scientific and Technical Terms, 4th ed)
Unstable isotopes of indium that decay or disintegrate emitting radiation. In atoms with atomic weights 106-112, 113m, 114, and 116-124 are radioactive indium isotopes.
Transplantation between animals of different species.
Lining of the INTESTINES, consisting of an inner EPITHELIUM, a middle LAMINA PROPRIA, and an outer MUSCULARIS MUCOSAE. In the SMALL INTESTINE, the mucosa is characterized by a series of folds and abundance of absorptive cells (ENTEROCYTES) with MICROVILLI.
Signal molecules that are involved in the control of cell growth and differentiation.
A system of NEURONS that has the specialized function to produce and secrete HORMONES, and that constitutes, in whole or in part, an ENDOCRINE SYSTEM or organ.
A nonmetallic, diatomic gas that is a trace element and member of the halogen family. It is used in dentistry as flouride (FLUORIDES) to prevent dental caries.
Tumors or cancer of the BRONCHI.
A sesquiterpene lactone found in roots of THAPSIA. It inhibits CA(2+)-TRANSPORTING ATPASE mediated uptake of CALCIUM into SARCOPLASMIC RETICULUM.
A peptide of about 22-amino acids isolated from the DUODENUM. At low pH it inhibits gastric motor activity, whereas at high pH it has a stimulating effect.
Food and dietary formulations including elemental (chemically defined formula) diets, synthetic and semisynthetic diets, space diets, weight-reduction formulas, tube-feeding diets, complete liquid diets, and supplemental liquid and solid diets.
The making of a radiograph of an object or tissue by recording on a photographic plate the radiation emitted by radioactive material within the object. (Dorland, 27th ed)
Neurons which send impulses peripherally to activate muscles or secretory cells.
An ionophorous, polyether antibiotic from Streptomyces chartreusensis. It binds and transports CALCIUM and other divalent cations across membranes and uncouples oxidative phosphorylation while inhibiting ATPase of rat liver mitochondria. The substance is used mostly as a biochemical tool to study the role of divalent cations in various biological systems.
Characteristic restricted to a particular organ of the body, such as a cell type, metabolic response or expression of a particular protein or antigen.
Calcium and magnesium salts used therapeutically in hepatobiliary dysfunction.
Guanosine 5'-(tetrahydrogen triphosphate). A guanine nucleotide containing three phosphate groups esterified to the sugar moiety.
Irregular microscopic structures consisting of cords of endocrine cells that are scattered throughout the PANCREAS among the exocrine acini. Each islet is surrounded by connective tissue fibers and penetrated by a network of capillaries. There are four major cell types. The most abundant beta cells (50-80%) secrete INSULIN. Alpha cells (5-20%) secrete GLUCAGON. PP cells (10-35%) secrete PANCREATIC POLYPEPTIDE. Delta cells (~5%) secrete SOMATOSTATIN.
GLYCEROL esterified with FATTY ACIDS.
Pathological development in the ILEUM including the ILEOCECAL VALVE.
A usually small, slow-growing neoplasm composed of islands of rounded, oxyphilic, or spindle-shaped cells of medium size, with moderately small vesicular nuclei, and covered by intact mucosa with a yellow cut surface. The tumor can occur anywhere in the gastrointestinal tract (and in the lungs and other sites); approximately 90% arise in the appendix. It is now established that these tumors are of neuroendocrine origin and derive from a primitive stem cell. (From Stedman, 25th ed & Holland et al., Cancer Medicine, 3d ed, p1182)
A cell surface receptor involved in regulation of cell growth and differentiation. It is specific for EPIDERMAL GROWTH FACTOR and EGF-related peptides including TRANSFORMING GROWTH FACTOR ALPHA; AMPHIREGULIN; and HEPARIN-BINDING EGF-LIKE GROWTH FACTOR. The binding of ligand to the receptor causes activation of its intrinsic tyrosine kinase activity and rapid internalization of the receptor-ligand complex into the cell.
Elements of limited time intervals, contributing to particular results or situations.
The sequence of PURINES and PYRIMIDINES in nucleic acids and polynucleotides. It is also called nucleotide sequence.
A genus of the family Muridae having three species. The present domesticated strains were developed from individuals brought from Syria. They are widely used in biomedical research.
An aquatic genus of the family, Pipidae, occurring in Africa and distinguished by having black horny claws on three inner hind toes.
A cell line derived from cultured tumor cells.
A slowly hydrolyzed CHOLINERGIC AGONIST that acts at both MUSCARINIC RECEPTORS and NICOTINIC RECEPTORS.
The lipid- and protein-containing, selectively permeable membrane that surrounds the cytoplasm in prokaryotic and eukaryotic cells.
Surface ligands, usually glycoproteins, that mediate cell-to-cell adhesion. Their functions include the assembly and interconnection of various vertebrate systems, as well as maintenance of tissue integration, wound healing, morphogenic movements, cellular migrations, and metastasis.
Systems for the delivery of drugs to target sites of pharmacological actions. Technologies employed include those concerning drug preparation, route of administration, site targeting, metabolism, and toxicity.
Unstable isotopes of fluorine that decay or disintegrate emitting radiation. F atoms with atomic weights 17, 18, and 20-22 are radioactive fluorine isotopes.
A family of synthetic protein tyrosine kinase inhibitors. They selectively inhibit receptor autophosphorylation and are used to study receptor function.
Hydrocarbons with more than one double bond. They are a reduced form of POLYYNES.
A 29-amino acid pancreatic peptide derived from proglucagon which is also the precursor of intestinal GLUCAGON-LIKE PEPTIDES. Glucagon is secreted by PANCREATIC ALPHA CELLS and plays an important role in regulation of BLOOD GLUCOSE concentration, ketone metabolism, and several other biochemical and physiological processes. (From Gilman et al., Goodman and Gilman's The Pharmacological Basis of Therapeutics, 9th ed, p1511)
The relationship between the chemical structure of a compound and its biological or pharmacological activity. Compounds are often classed together because they have structural characteristics in common including shape, size, stereochemical arrangement, and distribution of functional groups.
A quality of cell membranes which permits the passage of solvents and solutes into and out of cells.
A widely used non-cardioselective beta-adrenergic antagonist. Propranolol has been used for MYOCARDIAL INFARCTION; ARRHYTHMIA; ANGINA PECTORIS; HYPERTENSION; HYPERTHYROIDISM; MIGRAINE; PHEOCHROMOCYTOMA; and ANXIETY but adverse effects instigate replacement by newer drugs.
A class of cell surface receptors for TACHYKININS with a preference for SUBSTANCE P. Neurokinin-1 (NK-1) receptors have been cloned and are members of the G protein coupled receptor superfamily. They are found on many cell types including central and peripheral neurons, smooth muscle cells, acinar cells, endothelial cells, fibroblasts, and immune cells.
An organ of digestion situated in the left upper quadrant of the abdomen between the termination of the ESOPHAGUS and the beginning of the DUODENUM.
Benzopyrroles with the nitrogen at the number one carbon adjacent to the benzyl portion, in contrast to ISOINDOLES which have the nitrogen away from the six-membered ring.
Neoplasms which arise from or metastasize to the PITUITARY GLAND. The majority of pituitary neoplasms are adenomas, which are divided into non-secreting and secreting forms. Hormone producing forms are further classified by the type of hormone they secrete. Pituitary adenomas may also be characterized by their staining properties (see ADENOMA, BASOPHIL; ADENOMA, ACIDOPHIL; and ADENOMA, CHROMOPHOBE). Pituitary tumors may compress adjacent structures, including the HYPOTHALAMUS, several CRANIAL NERVES, and the OPTIC CHIASM. Chiasmal compression may result in bitemporal HEMIANOPSIA.
Cell surface proteins that bind signalling molecules external to the cell with high affinity and convert this extracellular event into one or more intracellular signals that alter the behavior of the target cell (From Alberts, Molecular Biology of the Cell, 2nd ed, pp693-5). Cell surface receptors, unlike enzymes, do not chemically alter their ligands.
A non-hydrolyzable analog of GTP, in which the oxygen atom bridging the beta to the gamma phosphate is replaced by a nitrogen atom. It binds tightly to G-protein in the presence of Mg2+. The nucleotide is a potent stimulator of ADENYLYL CYCLASES.
Drugs used for their effects on the gastrointestinal system, as to control gastric acidity, regulate gastrointestinal motility and water flow, and improve digestion.
Volume of biological fluid completely cleared of drug metabolites as measured in unit time. Elimination occurs as a result of metabolic processes in the kidney, liver, saliva, sweat, intestine, heart, brain, or other site.
The action of a drug in promoting or enhancing the effectiveness of another drug.
Electrophoresis in which a polyacrylamide gel is used as the diffusion medium.
The system of glands that release their secretions (hormones) directly into the circulatory system. In addition to the ENDOCRINE GLANDS, included are the CHROMAFFIN SYSTEM and the NEUROSECRETORY SYSTEMS.
The uptake of naked or purified DNA by CELLS, usually meaning the process as it occurs in eukaryotic cells. It is analogous to bacterial transformation (TRANSFORMATION, BACTERIAL) and both are routinely employed in GENE TRANSFER TECHNIQUES.
A nicotinic cholinergic antagonist often referred to as the prototypical ganglionic blocker. It is poorly absorbed from the gastrointestinal tract and does not cross the blood-brain barrier. It has been used for a variety of therapeutic purposes including hypertension but, like the other ganglionic blockers, it has been replaced by more specific drugs for most purposes, although it is widely used a research tool.
The interval between two successive CELL DIVISIONS during which the CHROMOSOMES are not individually distinguishable. It is composed of the G phases (G1 PHASE; G0 PHASE; G2 PHASE) and S PHASE (when DNA replication occurs).
Liquid chromatographic techniques which feature high inlet pressures, high sensitivity, and high speed.
An emulsifying agent produced in the LIVER and secreted into the DUODENUM. Its composition includes BILE ACIDS AND SALTS; CHOLESTEROL; and ELECTROLYTES. It aids DIGESTION of fats in the duodenum.
A CALMODULIN-dependent enzyme that catalyzes the phosphorylation of proteins. This enzyme is also sometimes dependent on CALCIUM. A wide range of proteins can act as acceptor, including VIMENTIN; SYNAPSINS; GLYCOGEN SYNTHASE; MYOSIN LIGHT CHAINS; and the MICROTUBULE-ASSOCIATED PROTEINS. (From Enzyme Nomenclature, 1992, p277)
Proteins prepared by recombinant DNA technology.
The essential part of the hearing organ consists of two labyrinthine compartments: the bony labyrinthine and the membranous labyrinth. The bony labyrinth is a complex of three interconnecting cavities or spaces (COCHLEA; VESTIBULAR LABYRINTH; and SEMICIRCULAR CANALS) in the TEMPORAL BONE. Within the bony labyrinth lies the membranous labyrinth which is a complex of sacs and tubules (COCHLEAR DUCT; SACCULE AND UTRICLE; and SEMICIRCULAR DUCTS) forming a continuous space enclosed by EPITHELIUM and connective tissue. These spaces are filled with LABYRINTHINE FLUIDS of various compositions.
Experimentally induced new abnormal growth of TISSUES in animals to provide models for studying human neoplasms.

Bombesin stimulates adhesion, spreading, lamellipodia formation, and proliferation in the human colon carcinoma Isreco1 cell line. (1/651)

The neuropeptide bombesin and its mammalian homologue, gastrin-releasing peptide (GRP), enhance proliferation in some but not all human tumor cell lines. The pathophysiological relevance of the bombesin/GRP receptor (GRP-R), which is expressed in 30% of human colon tumor cell lines and in 24-40% of native tumors, has not been clearly assessed at this time. We studied the effects of bombesin in the recently characterized human colon carcinoma Isreco1 cell line. Competitive reverse transcription-PCR showed a high GRP-R mRNA level in Isreco1 cells, and binding studies confirmed the expression of bombesin/GRP-subtype receptors (Kd = 0.42 nM; Bmax = 18,000 sites/cell). Exposure to bombesin resulted in an increase of intracellular calcium concentrations. Bombesin (1 nM) induced cell spreading at 24 h (21.7+/-1.6% versus 6.4+/-0.8% in control cells; P<0.01) and markedly increased the formation of lamellipodia. In addition, adhesion of Isreco1 cells to collagen I-coated culture dishes was stimulated in the presence of 1 nM bombesin (69+/-6% versus 42+/-1% in control cells; P<0.01). Finally, bombesin significantly increased [3H]thymidine uptake by Isreco1 cells in a dose-dependent manner, with a first significant response at 0.1 nM and a maximal effect at 100 nM bombesin (192.2+/-9.7% of control). These results clearly indicate that bombesin exerts morphological, adhesive, and proliferative effects on Isreco1 cells, suggesting that expression of the bombesin/GRP-R may contribute to the malignant properties of colon carcinoma cells.  (+info)

Diazepam-binding inhibitor33-50 elicits Ca2+ oscillation and CCK secretion in STC-1 cells via L-type Ca2+ channels. (2/651)

We recently isolated and characterized 86-amino acid CCK-releasing peptide from porcine intestinal mucosa. The sequence of this peptide is identical to that of porcine diazepam-binding inhibitor (DBI). Intraduodenal administration of DBI stimulates the CCK release and elicits pancreatic secretion in rats. In this study we utilized a murine tumor cell line (STC-1 cells) that contains CCK to examine if DBI directly acts on these cells to stimulate CCK release. We investigated the cellular mechanisms responsible for this action. We showed that DBI33-50, a biologically active fragment of DBI1-86, significantly stimulated CCK secretion in STC-1 cells. This action was abolished by Ca2+-free medium. The mean basal intracellular Ca2+ concentration ([Ca2+]i) was 52 nM in fura 2-loaded STC-1 cells. DBI33-50 (1-1,000 nM) elicited Ca2+ oscillations; DBI33-50 (10 nM) increased the oscillation frequency to 5 cycles/10 min and elicited a net [Ca2+]i increase (peak - basal) to 157 nM. In contrast, bombesin and forskolin caused an initial transient [Ca2+]i followed by a small sustained [Ca2+]i plateau. Withdrawal of extracellular Ca2+ abolished Ca2+ oscillations stimulated by DBI33-50. L-type Ca2+ channel blockers nifedipine and diltiazem (3-10 microM) markedly attenuated DBI-stimulated Ca2+ oscillations. In other cell types L-type Ca2+ channels are activated by cAMP-protein kinase A. DBI33-50 failed to stimulate cAMP formation in STC-1 cells. Similarly, DBI33-50 had no effect on myo-inositol 1,4, 5-trisphosphate concentration ([IP3]), whereas bombesin caused an eightfold increase in [IP3] over basal. In addition, inhibitors of phospholipase C (U-73122), phospholipase A2 (ONO-RS-082), and protein tyrosine kinase (genistein) did not alter the Ca2+ oscillations elicited by DBI33-50. It appears that DBI33-50 acts directly on STC-1 cells to elicit Ca2+ oscillations via the voltage-dependent L-type Ca2+ channels, resulting in the secretion of CCK. Mediation of this action is by intracellular mechanisms independent of the traditional signal transduction pathways, including phospholipase C, phospholipase A2, protein tyrosine kinase, and cAMP systems.  (+info)

Neuropeptide-mediated facilitation and inhibition of sensory inputs and spinal cord reflexes in the lamprey. (3/651)

The effects of neuromodulators present in the dorsal horn [tachykinins, neuropeptide Y (NPY), bombesin, and GABAB agonists] were studied on reflex responses evoked by cutaneous stimulation in the lamprey. Reflex responses were elicited in an isolated spinal cord preparation by electrical stimulation of the attached tail fin. To be able to separate modulator-induced effects at the sensory level from that at the motor or premotor level, the spinal cord was separated into three pools with Vaseline barriers. The caudal pool contained the tail fin. Neuromodulators were added to this pool to modulate sensory inputs evoked by tail fin stimulation. The middle pool contained high divalent cation or low calcium Ringer to block polysynaptic transmission and thus limit the input to the rostral pool to that from ascending axons that project through the middle pool. Ascending inputs and reflex responses were monitored by making intracellular recordings from motor neurons and extracellular recordings from ventral roots in the rostral pool. The tachykinin neuropeptide substance P, which has previously been shown to potentiate sensory input at the cellular and synaptic levels, facilitated tail fin-evoked synaptic inputs to neurons in the rostral pool and concentration dependently facilitated rostral ventral root activity. Substance P also facilitated the modulatory effects of tail fin stimulation on ongoing locomotor activity in the rostral pool. In contrast, NPY and the GABAB receptor agonist baclofen, both of which have presynaptic inhibitory effects on sensory afferents, reduced the strength of ascending inputs and rostral ventral root responses. We also examined the effects of the neuropeptide bombesin, which is present in sensory axons, at the cellular, synaptic, and reflex levels. As with substance P, bombesin increased tail fin stimulation-evoked inputs and ventral root responses in the rostral pool. These effects were associated with the increased excitability of slowly adapting mechanosensory neurons and the potentiation of glutamatergic synaptic inputs to spinobulbar neurons. These results show the possible behavioral relevance of neuropeptide-mediated modulation of sensory inputs at the cellular and synaptic levels. Given that the types and locations of neuropeptides in the dorsal spinal cord of the lamprey show strong homologies to that of higher vertebrates, these results are presumably relevant to other vertebrate systems.  (+info)

Characterization of airway and vascular responses in murine lungs. (4/651)

1. We characterized the responses of murine airways and pulmonary vessels to a variety of endogenous mediators in the isolated perfused and ventilated mouse lung (IPL) and compared them with those in precision-cut lung slices. 2. Airways: The EC50 (microM) for contractions of airways in IPL/slices was methacholine (Mch), 6.1/1.5>serotonin, 0.7/2.0>U46619 (TP-receptor agonist), 0.1/0.06>endothelin-1, 0.1/0.05. In the IPL, maximum increase in airway resistance (RL) was 0.6, 0.4, 0.8 and 11 cmH2O s ml(-1), respectively. Adenosine (< or =1 mM), bombesin (< or =100 microM), histamine (< or =10 mM), LTC4 (< or =1 microM), PAF (0.25 microM) and substance P (< or =100 microM) had only weak effects (<5% of Mch) on RL. 3. Vessels: The EC50 (microM) for vasoconstriction in the IPL was LTC4, 0.06>U46619, 0.05+info)

Characteristics of the muscularis mucosae in the acid-secreting region of the rabbit stomach. (5/651)

It has been suggested that muscularis mucosae excitation may augment gastric acid secretion, implying that this muscle should contract to secretagogues or stimulation of its motor innervation. The aim of this study was to characterize in vitro the responses of the muscularis mucosae in the rabbit gastric corpus to substances that modulate acid release and to intrinsic nerve stimulation. Muscularis mucosae from both fundic and antral ends of the corpus had identical mechanical properties, contracted to ACh, ADP, ATP, and histamine but relaxed to vasoactive intestinal polypeptide. Fundic but not antral muscularis mucosae contracted to bombesin and PGE2 and PGF2alpha, whereas adenosine, AMP, CCK, gastrin, secretin, and somatostatin were without effect on any preparation. In both regions electrical field stimulation evoked TTX-sensitive responses consisting of an atropine-resistant contraction followed by an NG-nitro-L-arginine methyl ester- and indomethacin-resistant relaxation. It is concluded from the regional variability in the pharmacological properties of the gastric muscularis mucosae that if its motor activity is linked to acid secretion this would be achieved by a neurally mediated relaxation rather than a paracrine- and/or endocrine-induced alteration in tone.  (+info)

NO releases bombesin-like immunoreactivity from enteric synaptosomes by cross-activation of protein kinase A. (6/651)

The effect of nitric oxide (NO) on the release of bombesin-like immunoreactivity (BLI) was examined in synaptosomes of rat small intestine. The NO donor S-nitroso-N-acetylpenicillamine (SNAP; 10(-7) to 10(-4) M) significantly stimulated BLI release. In the presence of the NO scavenger oxyhemoglobin (10(-3) M) or the guanylate cyclase inhibitor ODQ (10(-5) M), SNAP-induced BLI release was antagonized. In addition, SNAP increased the synaptosomal cGMP content and elevation of cGMP levels by zaprinast (3 x 10(-5) M), an inhibitor of the cGMP-specific phosphodiesterase (PDE) type 5, and increased basal and SNAP-induced BLI release. NO-induced BLI release was blocked by Rp-adenosine 3',5'-cyclic monophosphorothioate (3 x 10(-5) M and 10(-4) M), an inhibitor of the cAMP-dependent protein kinase A, whereas KT-5823 (3 x 10(-6) M) and Rp-8-(4-chlorophenylthio)-cGMP (5 x 10(-5) M), inhibitors of the cGMP-dependent protein kinase G, had no effect. Because cGMP inhibits the cAMP-specific PDE3, thereby increasing cAMP levels, the role of PDE3 was investigated. Trequinsin (10(-8) M), a specific blocker of PDE3, stimulated basal BLI release but had no additive effect on NO-induced release, suggesting a similar mechanism of action. These data demonstrate that because of a cross-activation of cAMP-dependent protein kinase A by endogenous cGMP BLI can be released by NO from enteric synaptosomes.  (+info)

Capsaicin-sensitive fibers are required for the anorexic action of systemic but not central bombesin. (7/651)

Bombesin (BN) suppresses food intake in rats whether given centrally or systemically. Although the brain BN-sensitive receptors are known to be essential for the anorexic effect of systemic BN, the mode of communication between the gut and the brain remains unclear. This study assessed whether the anorexic effect of systemic BN is mediated humorally or via neural circuits. Afferent neurons were lesioned using capsaicin (50 mg/kg sc) on postnatal day 2, and responses to BN were assessed during adulthood. Capsaicin treatment decreased body weight gain significantly from postnatal age 4-7 wk. Peripheral BN (4-16 micrograms/kg ip) dose dependently suppressed food intake in control animals. However, this effect was completely blocked in capsaicin-treated rats. In contrast to systemic effects, feeding-suppressant effects of centrally administered BN (0.01-0.5 microgram icv) were not affected by capsaicin treatment. This research suggests that peripheral BN communicates with the brain via a neuronal system(s) whose afferent arm is constituted of capsaicin-sensitive C and/or Adelta-fibers, whereas the efferent arm of this satiety- and/or anorexia-mediating circuitry is capsaicin resistant.  (+info)

Inositol 1,3,4-trisphosphate acts in vivo as a specific regulator of cellular signaling by inositol 3,4,5,6-tetrakisphosphate. (8/651)

Ca2+-activated Cl- channels are inhibited by inositol 3,4,5, 6-tetrakisphosphate (Ins(3,4,5,6)P4) (Xie, W., Kaetzel, M. A., Bruzik, K. S., Dedman, J. R., Shears, S. B., and Nelson, D. J. (1996) J. Biol. Chem. 271, 14092-14097), a novel second messenger that is formed after stimulus-dependent activation of phospholipase C (PLC). In this study, we show that inositol 1,3,4-trisphosphate (Ins(1,3,4)P3) is the specific signal that ties increased cellular levels of Ins(3,4,5,6)P4 to changes in PLC activity. We first demonstrated that Ins(1,3,4)P3 inhibited Ins(3,4,5,6)P4 1-kinase activity that was either (i) in lysates of AR4-2J pancreatoma cells or (ii) purified 22,500-fold (yield = 13%) from bovine aorta. Next, we incubated [3H]inositol-labeled AR4-2J cells with cell permeant and non-radiolabeled 2,5,6-tri-O-butyryl-myo-inositol 1,3, 4-trisphosphate-hexakis(acetoxymethyl) ester. This treatment increased cellular levels of Ins(1,3,4)P3 2.7-fold, while [3H]Ins(3, 4,5,6)P4 levels increased 2-fold; there were no changes to levels of other 3H-labeled inositol phosphates. This experiment provides the first direct evidence that levels of Ins(3,4,5,6)P4 are regulated by Ins(1,3,4)P3 in vivo, independently of Ins(1,3,4)P3 being metabolized to Ins(3,4,5,6)P4. In addition, we found that the Ins(1, 3,4)P3 metabolites, namely Ins(1,3)P2 and Ins(3,4)P2, were >100-fold weaker inhibitors of the 1-kinase compared with Ins(1,3,4)P3 itself (IC50 = 0.17 microM). This result shows that dephosphorylation of Ins(1,3,4)P3 in vivo is an efficient mechanism to "switch-off" the cellular regulation of Ins(3,4,5,6)P4 levels that comes from Ins(1,3, 4)P3-mediated inhibition of the 1-kinase. We also found that Ins(1,3, 6)P3 and Ins(1,4,6)P3 were poor inhibitors of the 1-kinase (IC50 = 17 and >30 microM, respectively). The non-physiological trisphosphates, D/L-Ins(1,2,4)P3, inhibited 1-kinase relatively potently (IC50 = 0.7 microM), thereby suggesting a new strategy for the rational design of therapeutically useful kinase inhibitors. Overall, our data provide new information to support the idea that Ins(1,3,4)P3 acts in an important signaling cascade.  (+info)

TY - JOUR. T1 - Inhibition of growth of OV-1063 human epithelial ovarian cancers and c-jun and c-fos oncogene expression by bombesin antagonists. AU - Chatzistamou, I.. AU - Schally, Andrew V. AU - Sun, B.. AU - Armatis, P.. AU - Szepeshazi, K.. PY - 2000/10/2. Y1 - 2000/10/2. N2 - Receptors for bombesin are present on human ovarian cancers and bombesin-like peptides could function as growth factors in this carcinoma. Therefore, we investigated the effects of bombesin/gastrin-releasing peptide (GRP) antagonists RC-3940-II and RC-3095 on the growth of human ovarian carcinoma cell line OV-1063, xenografted into nude mice. Treatment with RC-3940-II at doses of 10 μg and 20 μg per day s.c. decreased tumour volume by 60.9% (P , 0.05) and 73.5% (P , 0.05) respectively, after 25 days, compared to controls. RC-3095 at a dose of 20 μg per day reduced the volume of OV-1063 tumours by 47.7% (P = 0.15). In comparison, luteinizing hormone-releasing hormone (LH-RH) antagonist Cetrorelix at a dose of 100 ...
Litorin 55749-97-8 MSDS report, Litorin MSDS safety technical specifications search, Litorin safety information specifications ect.
Members of the bombesin family of peptides potently stimulate insulin release by HIT-T15 cells, a clonal pancreatic cell line. The response to bombesin consists of a large burst in secretion during the first 30 s, followed by a smaller elevation of the secretory rate, which persists for 90 min. The aim of this study was to identify the intracellular messengers involved in this biphasic secretory response. Addition of 100 nM-bombesin to cells for 20 s increased the cellular accumulation of [3H]diacylglycerol (DAG) by 40% and that of [3H]inositol monophosphate (InsP), bisphosphate (InsP2) and trisphosphate (InsP3) by 40%, 300%, and 800%, respectively. In contrast, cyclic AMP concentrations were unaffected. Bombesin stimulation of [3H]InsP3 formation was detected at 2 s, before the secretory response, which was not measurable until 5 s. Furthermore, the potency of bombesin to stimulate [3H]InsP3 generation (ED50 = 14 +/- 9 nM) agreed with its potency to stimulate insulin release (ED50 = 6 +/- 2 ...
Peptid oslobađanja gastrina (GRP) je regulatorni molekul koji učestvuje u brojnim fiziološkim i patofiziološkim procesima. Najbolje poznato dejstvo ovog peptida je stimulacija oslobađanja gastrina iz G ćelija želuca.. Gen iz kojeg je GRP izveden kodira brojne peptide slične bombesinu.[1][2][3][4] Njegov 148-aminokiselina dug preproprotein, nakon odvajanja signalnog peptida, se dalje transformiše da bi se formirao bilo 27 aminokiselina dug peptid oslobađanja gastrina ili 10 aminokiselina dug neuromedin C. Ovi manji peptidi regulišu brojne funkcije gastrointestinalnog i centralnog nervnog sistema, uključujući otpuštanje gastrointestinalnih hormona, kontrakciju ćelija glatkih mišića, i proliferaciju epitelijalnih ćelija.[1]. ...
TY - JOUR. T1 - Inhibition of mutant p53 expression and growth of DMS-153 small cell lung carcinoma by antagonists of growth hormone-releasing hormone and bombesin. AU - Kanashiro, Celia A.. AU - Schally, Andrew V.. AU - Groot, Kate. AU - Armatis, Patricia. AU - Bernardino, Andrea L.F.. AU - Varga, Jozsef L.. PY - 2003/12/23. Y1 - 2003/12/23. N2 - We investigated the effects of growth hormone-releasing hormone (GHRH) antagonists, JV-1-65 and JV-1-63, and bombesin/gastrin-releasing peptide (BN/GRP) antagonist RC-3940-II on DMS-153 human small cell lung carcinoma xenografted into nude mice. Treatment with 10 μg/day JV-1-65 or RC-3940-11 decreased tumor volume by 28% (P , 0.05) and 77% (P , 0.01), respectively, after 42 days compared with controls. Combination of JV-1-65 and RC-3940-11 induced the greatest inhibition of tumor proliferation (95%; P , 0.01), suggesting a synergism. Western blotting showed that the antitumor effects of these antagonists were associated with inhibition of the ...
GRP is a mammalian homolog of amphibian bombesin, a polypeptide initially isolated from the skin of the frog Bombina bombina (7, 31). GRP is a 27-amino acid peptide that targets a metabotropic receptor, GRPR, that is also referred to as BB2. The other two closely related mammalian bombesin peptide-like receptors are BB1 or neuromedin B receptor (NMBR) that prefers to bind neuromedin B (NMB) and BB3, an orphan bombesin receptor subtype 3 (BRS3) (31). These receptors are all GPCR members and have been implicated in a wide range of physiological activities including feeding, smooth muscle contraction, and regulation of sucrose intake (40, 55). Mice lacking GRPR are grossly normal, suggesting that GRPR is not required for animal survival (24). NMBR is important for thermoregulation but not necessary for smooth muscle contraction or for suppression of feeding behavior (56). In the CNS, the physiological effect of GRPR has been studied in the anterior cingulated cortex, hippocampus, and amygdala (8, ...
How is Murine Gastrin-Releasing Peptide Receptor abbreviated? mGRPr stands for Murine Gastrin-Releasing Peptide Receptor. mGRPr is defined as Murine Gastrin-Releasing Peptide Receptor very rarely.
We studied the effects of a new bombesin/gastrin-releasing peptide (GRP) receptor antagonist, Leu13-psi-(CH2NH)-Leu14-bombesin, on the secretion of gastrin and somatostatin and on the motor activity of isolated perfused porcine antrum in response to infusions of GRP at 10(-10) or 10(-9) mol/l and in …
It is well known that cytokines are highly involved in the disease process of rheumatoid arthritis (RA). Recently, targeting of neuropeptides has been suggested to have potential therapeutic effects in RA. The aim of this study was to investigate possible interrelations between five neuropeptides (bombesin/gastrin-releasing peptide (BN/GRP), substance P (SP), vasoactive intestinal peptide, calcitonin-gene-related peptide, and neuropeptide Y) and the three cytokines tumour necrosis factor (TNF)-α, IL-6, and monocyte chemoattractant protein-1 in synovial fluid of patients with RA. We also investigated possible interrelations between these neuropeptides and soluble TNF receptor 1 in serum from RA patients. Synovial fluid and sera were collected and assayed with ELISA or RIA. The most interesting findings were correlations between BN/GRP and SP and the cytokines. Thus, in synovial fluid, the concentrations of BN/GRP and SP grouped together with IL-6, and SP also grouped together with TNF-α and monocyte
Neuropeptides, such as substance P (SP) and bombesin/gastrin-releasing peptide (BN/GRP), and neurotrophins are involved in neuro-immunomodulatory processes and have marked trophic, growth-promoting and inflammation-modulating properties. The impact of these modulators in rheumatoid arthritis (RA) is, however, unclear. An involvement of the innervation, including the peptidergic innervation, is frequently proposed as an important factor for arthritic disease. Many patients with RA, but not all, benefit from treatment with anti-TNF medications.. The studies presented here aimed to investigate the roles of neuropeptides, with an emphasis on BN/GRP and SP, and neurotrophins, especially with attention to brain-derived neurotrophic factor (BDNF), in human and murine knee joint tissue. The expression patterns of these substances and their receptors in synovial tissue from patients with either RA or osteoarthritis (OA) were studied in parallel with the levels of these factors in blood and synovial fluid ...
Abstract. Gastrin-releasing peptide receptor (GRPR) is overexpressed in human prostate cancer and is being used as a target for mol. imaging. In this study, we report on the direct comparison of 3 novel GRPR-targeted radiolabeled tracers: Al18F-JMV5132, 68Ga-JMV5132, and 68Ga-JMV4168 (JMV5132 is NODA-MPAA-βAla-βAla-[H-D-Phe-Gln-Trp-Ala-Val-Gly-His-Sta-Leu-NH2], JMV4168 is DOTA-βAla-βAla-[H-D-Phe-Gln-Trp-Ala-Val-Gly-His-Sta-Leu-NH2], and NODA-MPAA is 2-[4-(carboxymethyl)-7-{[4-(carboxymethyl) phenyl]methyl}-1,4,7-triazacyclononan-1-yl]acetic acid). Methods: The GRPR antagonist JMV594 (H-D-Phe-Gln-Trp-Ala-Val-Gly-His-Sta-Leu-NH2) was conjugated to NODA-MPAA for labeling with Al18F. JMV5132 was radiolabeled with 68Ga and 18F, and JMV4168 was labeled with 68Ga for comparison. The inhibitory concn. of 50% values for binding GRPR of JMV4168, JMV5132, natGa-JMV4168, and natGa-JMV5132 were detd. in a competition-binding assay using GRPR-overexpressing PC-3 tumors. The tumor-targeting characteristics ...
TY - JOUR. T1 - Actions of gastrin-releasing peptide and related mammalian and amphibian peptides on ion transport in the porcine proximal jejunum. AU - Chandan, Ritu. AU - Newell, Susan M.. AU - Brown, David R.. PY - 1988/10. Y1 - 1988/10. N2 - The 27-amino acid peptide gastrin-releasing peptide (GRP) and the decapeptide neuromedin B (NMB) are structurally related to bombesin (BB) and exist within the mammalian small intestine. We examined the actions of porcine GRP and NMB on ion transport in the porcine proximal jejunum in vitro and compared their activities to those of their respective C-terminal amphibian homologs BB and ranatensin (RT). The 4 peptides transiently increased potential difference and short-circuit currrent (Isc) in jejunal mucosal sheets after their serosal administration in subnanomolar concentrations with an order of potency: GRP ≈ RT ≥ NMB , BB. BB and RT were more effective in elevating Isc than GRP and NMB; all peptides had variable effects on tissue conductance. ...
TY - JOUR. T1 - Roles for substance P and gastrin-releasing peptide as neurotransmitters released by primary afferent pruriceptors. AU - Akiyama, Tasuku. AU - Tominaga, Mitsutoshi. AU - Davoodi, Auva. AU - Nagamine, Masaki. AU - Blansit, Kevin. AU - Horwitz, Alexander. AU - Carstens, Mirela Iodi. AU - Carstens, Earl. PY - 2013. Y1 - 2013. N2 - Recent studies support roles for neurokinin-1 (NK-1) and gastrin-releasing peptide (GRP) receptor-expressing spinal neurons in itch. We presently investigated expression of substance P (SP) and GRP in pruritogen-responsive primary sensory neurons and roles for these neuropeptides in itch signaling. Responses of dorsal root ganglion (DRG) cells to various pruritogens were observed by calcium imaging. DRG cells were then processed for SP, GRP, and isolectin B-4 (IB4; a marker for nonpeptidergic neurons) immunofluorescence. Of prurito-gen-responsive DRG cells, 11.8 -26.8%, 21.8-40.0%, and 21.4-26.8% were immunopositive for SP, GRP, and IB4, respectively. In ...
The bombesin receptor family is a member of the G protein-coupled receptor superfamily and consists of three subtypes of receptors: BB1 (neuromedin B receptor), BB2 (gastrin-releasing peptide receptor), and BB3. These receptors are widely distributed in mammals especially in the CNS and gastrointestinal tract and have numerous effects both physiologically and in pathologic processes including having an autocrine growth action on normal tissues and tumors; potent CNS effects (satiety, circadian rhythm, various behaviors); and potent effects in the immune, gastrointestinal, respiratory and urogenital systems.The human BB2 receptor has a greater than 50-fold higher affinity for gastrin-releasing peptide than neuromedin B. Interaction of ligand and BB2 activates the Gαq/11 pathway and increase the intracellular calcium concentration. GenScripts BB2-expressing stable cell line was made in CHO-K1 host cell and optimized for calcium assays.
Gastrin-releasing peptide (GRP) is the mammalian analogue of bombesin. Both neuroendocrine peptides have similar distribution, functions and immunoreactivity. The immunoreactivity for GRP has been demonstrated in the esophagus, stomach and small intestine. This peptide is reported to have various biological and pharmacological properties, which include the release of gastrointestinal hormones, control of satiety, gastrointestinal motility and stimulation of cellular proliferation which results in wound healing. It is also implicated in the proliferation of many gastrointestinal (GI), renal and prostatic tumours. Transient increase in GRP synthesis in the brain and serum concentration, which was later followed by decreased serum concentration, has been reported in hyperglycemic states. The aim of this investigation was to determine the effect of hyperglycemia on GRP secreting neurons in the sub mucosa of the GIT and how this may affect some of the GI complications of diabetes. Result showed decreased
Gastrin releasing peptide(GRP) is a 27 amino acid peptide isolated from the porcine gut. The last ten amino acids at the C-terminus of gastrin releasing peptide correspond with one amino acid alteration (3) to the last ten amino acids of bombesin, viz: H-Gly-Asn-His-Trp-Ala-Val-Gly-His-Leu-Met-NH2 .It has been reported (J. H. Walsh and J. R. Reeve, Peptides 6, (3), 63-68, (1985) that bombesin and bombesin-like peptides such as gastrin releasing peptide (GRP) are secreted by human small-cell lung cancer (SCLC) cells. It has been postulated (P. J. Woll and E. Rozengurt, PNAS 85, 1859-1863, (1988)) that gastrin releasing factor antagonists would bind competitively to bombesin receptors in animals and would therefore be of use in the treatment of SCLC and/or in the control of clinical symptoms associated with this disease and due to hypersecretion of this peptide hormone. Analogues of bombesin/ GRP have been shown to inhibit the binding of gastrin releasing peptide to a SCLC cell line and to inhibit ...
Comoglio, P.M., 1988: Autocrine activation of the tyrosine kinase associated with the bombesin receptor in small cell lung carcinoma
Neuromedin B, a bombesin-like peptide, and its receptor, are expressed in white adipose tissue with undefined roles. Female mice with disruption of neuromedin B receptor (NB-R) exhibited partial resistance to diet-induced obesity leading to our hypothesis that NB-R is involved in adipogenesis. Here, we showed that adipose stem/stromal cells (ASC) from perigonadal fat of female NB-R-knockout mice, exposed to a differentiation protocol in vitro, accumulated less lipid (45%) than wild type, suggesting reduced capacity to differentiate under adipogenic input. To further explore mechanisms, preadipocytes 3T3-L1 cells were incubated in the presence of NB-R antagonist (PD168368) during the first 3 days in culture. Cells were analyzed in the end of the treatment (Day 3) and later when fully differentiated (Day 21). NB-R antagonist induced lower number of cells at day 3 and 21 (33-39%), reduced cell proliferation at day 3 (−53%) and reduced lipid accumulation at day 21 (−86%). The mRNA expressions of ...
TY - JOUR. T1 - A new high affinity technetium-99m-bombesin analogue with low abdominal accumulation. AU - Lin, Kuo Shyan. AU - Luu, Andrew. AU - Baidoo, Kwamena E.. AU - Hashemzadeh-Gargari, Hossein. AU - Chen, Ming Kai. AU - Brenneman, Kenneth. AU - Pili, Roberto. AU - Pomper, Martin. AU - Carducci, Michael A.. AU - Wagner, Henry N.. PY - 2005/1/1. Y1 - 2005/1/1. N2 - 99mTc-labeled bombesin analogues have shown promise for noninvasive detection of many tumors that express bombesin (BN)/gastrin- releasing peptide (GRP) receptors. 99mTc-labeled peptides, however, have a tendency to accumulate in the liver and intestines due to hepatobiliary clearance as a result of the lipophilicity of the 99mTc chelates. This makes the imaging of lesions in the abdominal area difficult. In this study, we have synthesized a new high affinity 99mTc-labeled BN analogue, [DTPA1, Lys3(99mTc-Pm-DADT), Tyr 4]BN, having a built-in pharmacokinetic modifier, DTPA, and labeled with 99mTc using a hydrophilic diaminedithiol ...
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Bombesin pseudo-peptide analogues containing a hydroxamide function on the C-terminal part of the molecule, e.g. H-D-Phe-Gln-Trp-Ala-Val-Gly-His-Leu-NHOBzl 1 and H-D-Phe-Gln-Trp-Ala-Val-Gly-His-Leu-NHOH 2 were synthesized. These compounds were tested for their ability to recognize the bombesin receptor on rat pancreatic acini and on 3T3 cells, to stimulate (i) amylase secretion from rat pancreatic ...
|p|The |strong|RC-28|/strong| is a special chamber containing two bath compartments separated by an adjustable dam. The dam functions both as a gate and barrier
Home , Papers , Physiological Function of Gastrin-Releasing Peptide and Neuromedin B Receptors in Regulating Itch Scratching Behavior in the Spinal Cord of Mice. ...
Gastrin-Releasing Peptide: Neuropeptide and gut hormone that helps regulate GASTRIC ACID secretion and motor function. Once released from nerves in the antrum of the STOMACH, the neuropeptide stimulates release of GASTRIN from the GASTRIN-SECRETING CELLS.
Neuroblastoma is the most common extracranial solid tumor in infants and children. Our lab and others have shown trophic actions of gastrin-releasing peptide (GRP), and its analogue bombesin (BBS), in neuroblastomas. Our lab also found that undifferentiated neuroblastomas express increased levels of GRP receptor (GRPR). Activation of the phosphatidylinositol-3-kinase (PI3K)/Akt pathway, a crucial regulator of cell survival, is associated with poor outcome in neuroblastomas and our lab¡¦s previous work has shown that GRPR regulates the expression of PI3K/Akt pathway components. However, the signaling mechanisms involved in this process are not clearly defined. Therefore, the objective of this project was to determine how GRP/GRPR, by way of PI3K pathway, regulates neuroblastoma growth. \r\n\r\nGRP/BBS treatment rapidly increased phosphorylation of both Akt and GSK-3ƒÒ in neuroblastoma cells. Antagonism or silencing of GRPR attenuated BBS-induced phosphorylation of Akt. PI3K inhibition also ...
Neuroblastomas express increased levels of gastrin-releasing peptide receptor (GRP-R). However, the exact molecular mechanisms involved in GRP-R-mediated cell signaling in neuroblastoma growth and metastasis are unknown. Here, we report that focal adhesion kinase (FAK), as a critical downstream target of GRP-R, is an important regulator of neuroblastoma tumorigenicity. We found that FAK expression correlates with GRP-R expression in human neuroblastoma sections and cell lines. GRP-R overexpression in SK-N-SH cells increased FAK, integrin α3 and β1 expressions and cell migration. These cells demonstrated flatter cell morphology with broad lamellae, in which intense FAK expression was localized to the leading edges of lamellipodia. Interestingly, FAK activation was, in part, dependent on integrin α3 and β1 expression. Conversely, GRP-R silencing decreased FAK as well as Mycn levels in BE(2)-C cells, which displayed a denser cellular morphology. Importantly, rescue experiments in GRP-R silenced BE(2)-C
Background The overexpression from the chemokine receptor 4 (CXCR4) in various epithelial, mesenchymal, and hematopoietic cancers makes CXCR4 a good diagnostic and therapeutic target. and 213Bwe3+ (for endoradiotherapy). Nevertheless, the experiences obtained during the advancement of pentixafor show that, weighed against [68Ga]pentixafor, unlabeled pentixafor and additional radiometalated pentixafor derivatives show considerably SYN-115 lower CXCR4 receptor affinities. Therefore, as opposed to additional peptides, such as for example somatostatin receptor (SSTR), gastrin-releasing peptide receptor (GRPR), or v3 binding peptides, the affinity of [68Ga]pentixafor towards CXCR4 depends upon the complete ligand-spacer-chelator-radiometal construct. As a result, a far more or much less unbiased bioactive substructure or pharmacophor (e.g., the pentapeptide primary A depicted in Fig.?1) cant be identified. Within this research, we looked into pentixafor derivatives with choice cyclic and acyclic ...
Peptides , Gastrins , Gastrin Releasing Peptide, human; Gastrin-releasing peptide, a 27-amino acid peptide isolated from the gut, stimulates the release of Gastrin, and shares a common C-terminal decapeptide homology with bombesin. Gastrin-releasing peptide is an important growth-modulating factor in developing lung epithelium. It is used as a tumor marker in the diagnosis of small-cell lung carcinoma, since it is known to be produced by these cancer cells.; VPLPAGGGTVLTKMYPRGNHWAVGHLM-NH2; H-Val-Pro-Leu-Pro-Ala-Gly-Gly-Gly-Thr-Val-Leu-Thr-Lys-Met-Tyr-Pro-Arg-Gly-Asn-His-Trp-Ala-Val-Gly-His-Leu-Met-NH2
Introduction and Objectivies: Neuropeptides such as gastrin-releasing peptide (GRP) confer androgen-independent (AI) growth of LNCaP cells through binding to G protein coupled receptors on the cell surface. Three non-receptor tyrosine kinases, Src, FAK and Etk are activated and subsequently activate androgen receptor in the absence of its cognate ligand. We hypothesize that inhibition of Src activity reduces GRP-mediated AI growth and migration in vitro and in vivo. Methods: Phosphorylation status of Src, FAK and Etk in LNCaP-GRP cell lines were examined by Western blot analysis. Inhibition of Src activity was performed through specific Src family kinase (SFK) inhibitor AZD0530 or transfection with RNA interference for Src and evaluated by growth and migration assays. Expression of androgen biosynthetic enzymes such as AKR1 C1/2, C3 and HSD3 B1 was compared between LNCaP control and GRP lines by RT-PCR. Castrated SCID mice were orthotopically implanted with GRP cells and treated with or without ...
TY - JOUR. T1 - Acid-soluble precursors and derivatives of phospholipids increase after stimulation of quiescent swiss 3T3 mouse fibroblasts with serum. AU - Warden, Craig H. AU - Friedkin, M.. AU - Geiger, P. J.. PY - 1980/5/30. Y1 - 1980/5/30. N2 - Automated phosphate analysis of acid-soluble pools of phosphate esters was employed to reveal possible biochemical changes during the transition of Swiss 3T3 mouse fibroblasts from quiescence to active replication of DNA. After 12 hours of stimulation with 10% fetal bovine serum the most notable were 3-fold increases in pools of phospholipid precursors and derivatives. These included glycerophosphocholine, glycerophosphoethanolamine, phosphocholine and phosphoethanolamine. Concurrent but less dramatic increases in pools of ATP, CTP and fructose 1,6-diphosphate were also obtained.. AB - Automated phosphate analysis of acid-soluble pools of phosphate esters was employed to reveal possible biochemical changes during the transition of Swiss 3T3 mouse ...
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TY - CHAP. T1 - Bombesin stimulates growth of human small cell lung carcinoma in vivo. AU - Alexander, R. W.. AU - Upp, J. R.. AU - Poston, G. J.. AU - Gupta, V.. AU - Townsend, Courtney. AU - Thompson, J. C.. PY - 1987. Y1 - 1987. UR - http://www.scopus.com/inward/record.url?scp=0023610349&partnerID=8YFLogxK. UR - http://www.scopus.com/inward/citedby.url?scp=0023610349&partnerID=8YFLogxK. M3 - Chapter. AN - SCOPUS:0023610349. VL - 38. SP - 450. EP - 452. BT - Surgical Forum. ER - ...
As model system, a solid-tumor patient-derived xenograft (PDX) model characterized by high peptide receptor expression and histological tissue homogeneity was used to study radiopeptide targeting. In this solid-tumor model, high tumor uptake of targeting peptides was expected. However, in vivo SPECT images showed substantial heterogeneous radioactivity accumulation despite homogenous receptor distribution in the tumor xenografts as assessed by in vitro autoradiography. We hypothesized that delivery of peptide to the tumor cells is dictated by adequate local tumor perfusion. To study this relationship, sequential SPECT/CT and MRI were performed to assess the role of vascular functionality in radiopeptide accumulation. High-resolution SPECT and dynamic contrast-enhanced (DCE)-MRI were acquired in six mice bearing PC295 PDX tumors expressing the gastrin-releasing peptide (GRP) receptor. Two hours prior to SPECT imaging, animals received 25 MBq 111In(DOTA-(βAla)2-JMV594) (25 pmol). Images were acquired
The synthesis and biological evaluation on thermoregulation of 39 peptides related to bombesin (structural analogues or other naturally occurring peptides) are described. The bioassay system reported measures the ability of peptides injected intracisternally to lower body temperature of cold (4 degrees C) exposed rats. The most potent analogues of bombesin were those in which positions one to five (not included) were altered, indicating that the decapeptide C terminal was sufficient for full potency. Gln at the seventh position and Gly at the 11th position could be replaced by D-Gln and D-Ala (but not D-Pro or D-Phe), respectively, without any change in potency. Methionine at the 14 position could be replaced with its D isomer with retention of 10% biological activity. Any other alteration of the C terminus (deletions or free acid with the exception of the N-methylamide) drastically reduced the biological potency of those peptides. Among other naturally occurring peptides, alytesin was found to ...
other oligopeptides with gastroprotective properties. Neuropeptides. In 1979, the team of Y. Taché and coauthors reported for the first time that peptides act in the brain to protect against the development of gastric erosions induced by cold restraint stress in rats [11,26,41]. They injected the 14-amino acid neuropeptide bombesin into the cisterna magna and noted the changes in the autonomic nervous system activity, resulting in the simultaneous inhibition of gastric acid and pepsin secretion and motility [42].In future decades the involvement of neuropeptides in the regulation of the function of gut was confirmed by numerous papers of other authors [6,28,29,41,38,39,43]. Thus, it was shown that opioid peptides, the most numerous family of neuropeptides, have much broader physiological effects than the regulation of emotions. The elucidation of the biological effects of opioid peptides showed their important role in the integration of nervous, endocrine and immune system, since the receptors ...
Mary Sunday, MD PhD has recently been awarded a Pilot Project Grant entitled Oxygen, Gastrin-Releasing Peptide (GRP), and Radiation-Induced Pulmonary Fibrosis from the NIH Centers for Medical Countermeasures Against Radiation (CMCR), a part of the NIH RadCCORE Program. The goal of this investigation is to determine human relevance of prior mouse studies to prevent radiation
Established in 1982 from an adrenal gland metastasis of a small cell lung cancer from a man in relapse following treatment; cells were described to be tumorigenic in nude mice and to express elevated levels of L-dopa decarboxylase, neuron-specific enolase, creatine kinase and bombesin-like ...
CMR 2005: 3.09: Preclinical efficacy of 177Lu-AMBA, a radiotherapeutic targeting the GRP receptor (page 61). L.E. Lantry, M.E. Maddalena, J.S. Fox, J. Chen, S.M. Eaton, N.J. Bogdan, R. Thomas, E. Cappelletti, L. Lattuada, H. Nguyen, K.E. Linder, R.E. Swenson, M.F. Tweedle and A.D. Nunn. Version of Record online: 19 APR 2006 , DOI: 10.1002/cmmi.22. ...
This gene encodes a 7-transmembrane G protein-coupled receptor that binds neuromedin B, which is a growth factor and mitogen for gastrointestinal epithelial tissue and for normal and neoplastic lung. This receptor may play a role in smooth muscle contraction, neuronal responses, and the regulation of cell growth. Antagonists of this receptor have a potential therapeutic use in inhibiting tumor cell growth. Polymorphisms in this gene may be associated with a susceptibility for schizophrenia. Alternative splicing of this gene results in multiple transcript variants. [provided by RefSeq, Apr 2016 ...
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Stimulates the release of gastrin and other gastrointestinal hormones (By similarity). Contributes to the perception of prurient stimuli and to the transmission of itch signals in the spinal cord that promote scratching behavior. Contributes primarily to nonhistaminergic itch sensation. Contributes to long-term fear memory, but not normal spatial memory (By similarity). Contributes to the regulation of food intake (PubMed:17208656).
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The gastrin releasing peptide receptor (GRP-R) is over-expressed on several tumors and cancer cell lines including pancreas, prostate, breasts, gastrointestinal and small cell lung cancer (SCLC). targeted cells is usually a prerequisite to triggering effective internalization. For restorative reasons, efficient internalization from the radioconjugate is apparently important in providing the best radioactivity dose towards the targeted cells. Structural adjustments to these radiopharmaceuticals possess included variance in the peptide series, the nature from the chelate and radiometal, and the space from the spacer attaching both components (Physique 1). For instance, an agonist BBN AUY922 analogue, Perform3A-CH2CO-G-4-aminobenzoyl-Q-W-A-V-G-H-L-M-NH2 (AMBA) was synthesized and tagged with 177Lu for prostate malignancy focusing on (22). 177Lu-AMBA displays a higher affinity for the GRP-R (IC50 = 2.50 0.50 nM) and 76.8% internalization. The in vitro binding properties of 177Lu-AMBA had been ...
Nmbr - Nmbr (Myc-DDK-tagged ORF) - Rat neuromedin B receptor (Nmbr), (10 ug) available for purchase from OriGene - Your Gene Company.
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1.an = 3n - 1 2. an = 2(2n - 3) 3.an = 4^n 4.an = (2/3)^n 5. an = (-1)^n(n + 5) 6. an = (-1)^n + 1(n + 6) 7. an= n+3/2n-1 8. a1 = -5 and an = an-1 - 3 for n ≥ 2 9. a1 = -6 and an = -2an-1 for n ≥ 2 10.a1 = 4 and an = 3an-1 + 2 for n ≥ 2 11. Find a8 when a1... ...
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Receptors, Bombesin at the US National Library of Medicine Medical Subject Headings (MeSH) This article incorporates text from ... 1991). "Two distinct bombesin receptor subtypes are expressed and functional in human lung carcinoma cells". J. Biol. Chem. 266 ... "Bombesin Receptors: BB1". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology ... 1996). "Bombesin-like peptide receptors in human bronchial epithelial cells". Peptides. 17 (1): 111-8. doi:10.1016/0196-9781(95 ...
1991). "Two distinct bombesin receptor subtypes are expressed and functional in human lung carcinoma cells". J. Biol. Chem. 266 ... "Bombesin Receptors: BB2". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology ... Corjay MH, Dobrzanski DJ, Way JM, Viallet J, Shapira H, Worland P, Sausville EA, Battey JF (1991). "Two distinct bombesin ... Benya RV, Kusui T, Pradhan TK, Battey JF, Jensen RT (1995). "Expression and characterization of cloned human bombesin receptors ...
Bombesin. -. -. PP: Other. Gastrin releasing peptide. GRP. -. -. PP: Other. Kisspeptin. GPR54. -. Gasotransmitter. Nitric oxide ...
These include secretin, acetylcholine, ATP, and bombesin. Cholangiocytes act through bile-acid independent bile flow, which is ...
ISBN 978-0-89766-441-7. Gmerek, Debra E.; Cowan, A. (1988). "Role of Opioid Receptors in Bombesin-induced Grooming". Annals of ...
The gene from which GRP is derived encodes a number of bombesin-like peptides. Its 148-amino acid preproprotein, following ... Merali Z, McIntosh J, Anisman H (2000). "Role of bombesin-related peptides in the control of food intake". Neuropeptides. 33 (5 ... Merali Z, McIntosh J, Anisman H (October 1999). "Role of bombesin-related peptides in the control of food intake". ... Frankel A, Tsao MS, Viallet J (1994). "Receptor subtype expression and responsiveness to bombesin in cultured human bronchial ...
... (NMB) is a bombesin-related peptide in mammals. It was originally purified from pig spinal cord, and later shown ... Mammalian bombesin receptors: nomenclature, distribution, pharmacology, signaling, and functions in normal and disease states ... "Molecular cloning of cDNAs encoding the human bombesin-like peptide neuromedin B. Chromosomal localization and comparison to ...
The peptide hormone bombesin also stimulates gastrin from G cells. Gastrin-releasing peptide, as well as the presence of amino ...
... : an antibacterial agent from the root bark of Morus alba against oral pathogens Non-peptide bombesin receptor ... Kuwanon G is an antimicrobial bombesin receptor antagonist, isolated from Morus alba. ...
The best-characterized peptides are GRP, the mammalian form of bombesin, and CGRP; these substances exert direct mitogenic ...
Panula P, Hadjiconstantinou M, Yang HY, Costa E (Oct 1983). "Immunohistochemical localization of bombesin/gastrin-releasing ...
The Bombesin peptide has been shown to be overexpressed in BB2 receptors in prostate cancer. CB-TE2A a stable chelation system ... "MicroPET Imaging of Breast Cancer Using Radiolabeled Bombesin Analogs Targeting the Gastrin-releasing Peptide Receptor". Breast ... for 64Cu was incorporated with Bombesin analogs for in vitro and in vivo studies of prostate cancer. PET/CT imagining studies ...
"Activation of p300 histone acetyltransferase activity and acetylation of the androgen receptor by bombesin in prostate cancer ...
"Bombesin Receptors: BB3". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology ... "Bombesin Receptors: BB3". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology ... 1996). "Bombesin-like peptide receptors in human bronchial epithelial cells.". Peptides 17 (1): 111-8. PMID 8822519. doi: ... 1997). "Mice lacking bombesin receptor subtype-3 develop metabolic defects and obesity.". Nature 390 (6656): 165-9. PMID ...
1995). „Expression and characterization of cloned human bombesin receptors". Mol. Pharmacol. 47 (1): 10-20. PMID 7838118.. CS1 ... Merali Z, McIntosh J, Anisman H (2000). „Role of bombesin-related peptides in the control of food intake". Neuropeptides. 33 (5 ... 2002). „Identification and characterisation of functional bombesin receptors in human astrocytes". Eur. J. Pharmacol. 438 (1-2 ... Frankel A, Tsao MS, Viallet J (1994). „Receptor subtype expression and responsiveness to bombesin in cultured human bronchial ...
Hormones such as cholecystokinin, bombesin, neurotensin, anorectin, calcitonin, enterostatin, leptin and corticotropin- ...
Moreover, the catalytic activation of PKD3 in response to RacV12, Galpha (13/12) signalling, bombesin correlated with Ser-731/ ... and Rac are important components in the signal transduction pathways that mediate bombesin receptor induced PKD3 activation. ...
2002). "Cloning, expression, and mapping of a gene that is upregulated in adipose tissue of mice deficient in bombesin receptor ...
... blocks bombesin- and LPA-induced EGF receptor transactivation and DNA synthesis in rat-1 cells". Exp. Cell Res. 290 (2): 437-46 ...
"Immunohistochemical localization of bombesin/gastrin-releasing peptide and substance P in primary sensory neurons". The ...
Motilin Neurotensin Substance P Somatostatin Bombesin Serotonin Joshi, Vijaya D. (2006). Anatomy and Physiology for Nursing and ...
... may refer to: BB3, a postcode district the BB postcode area Bombesin-like receptor 3, also known as BB3 Big Brother 3, a ...
GPCRs include: receptors for sensory signal mediators (e.g., light and olfactory stimulatory molecules); adenosine, bombesin, ...
... bombesin - bombesin receptor - Bone morphogenetic protein - bradykinin - bradykinin receptor - BRCA1 - buffer solution - C- ...
... the pro-growth autocrine signaling of cancer cells via secreted peptides such as mammalian homologs related to bombesin. Some ...
... calcitonin and bombesin/gastrin-releasing peptide, while lacking, or rarely and weakly expressing, androgen receptor and ... and bombesin/gastrin-releasing peptide. Neuroendocrine tumor cells express cytokeratins that are typically expressed by luminal ... bombesin/gastrin-releasing peptide (GRP), thyroid stimulating hormone-like peptide, parathyroid hormone-related protein (PTHrP ...
... one of several Bombesin-like peptides Neuromuscular-blocking drugs New methylene blue, an organic staining agent None More ...
... bombesin-like peptides (gastrin-releasing peptide, neuromedin B and C), and neurotensin, and inhibited by hypothalamic dopamine ...
Bombesin receptor InterPro: IPR001556 Bombesin-like receptor 3 (BRS3) Neuromedin B receptor (NMBR) Gastrin-releasing peptide ...
... secreting gastrin secreting secretin nonsecreting cholecystokinin secreting insulin secreting glucagon nonsecreting bombesin ...
The response to bombesin consists of a large burst in secretion during the first 30 s, followed by a smaller elevation of the ... Members of the bombesin family of peptides potently stimulate insulin release by HIT-T15 cells, a clonal pancreatic cell line. ... The biphasic stimulation of insulin secretion by bombesin involves both cytosolic free calcium and protein kinase C. S L Swope ... Bombesin stimulation of [3H]InsP3 formation was detected at 2 s, before the secretory response, which was not measurable until ...
Receptors for bombesin are present on human ovarian cancers and bombesin-like peptides could function as growth factors in this ... N2 - Receptors for bombesin are present on human ovarian cancers and bombesin-like peptides could function as growth factors in ... AB - Receptors for bombesin are present on human ovarian cancers and bombesin-like peptides could function as growth factors in ... abstract = "Receptors for bombesin are present on human ovarian cancers and bombesin-like peptides could function as growth ...
1995). „Expression and characterization of cloned human bombesin receptors". Mol. Pharmacol. 47 (1): 10-20. PMID 7838118.. CS1 ... Merali Z, McIntosh J, Anisman H (2000). „Role of bombesin-related peptides in the control of food intake". Neuropeptides. 33 (5 ... 2002). „Identification and characterisation of functional bombesin receptors in human astrocytes". Eur. J. Pharmacol. 438 (1-2 ... Frankel A, Tsao MS, Viallet J (1994). „Receptor subtype expression and responsiveness to bombesin in cultured human bronchial ...
Bombesin is a 14-amino acid peptide originally isolated from the skin of the European fire-bellied toad (Bombina bombina). It ... Bombesin is also a tumor marker for small cell carcinoma of lung, gastric cancer, pancreatic cancer, and neuroblastoma. ... Neuromedin B Neuromedin U Gonzalez N, Moody TW, Igarashi H, Ito T, Jensen RT (February 2008). "Bombesin-related peptides and ... Yamada K, Wada E, Wada K (November 2000). "Bombesin-like peptides: studies on food intake and social behaviour with receptor ...
The bombesin receptors are a group of G-protein coupled receptors which bind bombesin. Three bombesin receptors are currently ... previously known as Bombesin-like receptor 3 BRS3 "Bombesin Receptors". IUPHAR Database of Receptors and Ion Channels. ...
Bombesin suppresses feeding in rats.. Gibbs J, Fauser DJ, Rowe EA, Rolls BJ, Rolls ET, Maddison SP. ... Bombesin (BBS) is a tetradecapeptide originally isolated from amphibian skin1. BBS-like immunoactivity is widely distributed in ...
Bombesin *Molecular FormulaC71H110N24O18S ...
Activation of bombesin receptor Subtype-3 by [D-Tyr,sup,6,/sup,,β-Ala,sup,11,/sup,,Phe,sup,13,/sup,,Nle,sup,14,/sup,]bombesin, ... Activation of bombesin receptor Subtype-3 by [D-Tyr,sup,6,/sup,,β-Ala,sup,11,/sup,,Phe,sup,13,/sup,,Nle,sup,14,/sup,]bombesin, ... Rattus norvegicus bombesin receptor subtype 3 (Brs3), mRNA Rattus norvegicus bombesin receptor subtype 3 (Brs3), mRNA. gi, ... Anatomical characterization of bombesin receptor subtype-3 mRNA expression in the rodent central nervous system. [J Comp Neurol ...
Rabbit polyclonal Bombesin Receptor 3 antibody validated for IHC and tested in Human. With 2 independent reviews. Immunogen ... Anti-Bombesin Receptor 3 antibody. See all Bombesin Receptor 3 primary antibodies. ... Ab62284 (10ug/ml) staining human Bombesin Receptor 3 in pregnant uterus tissue by immunohistochemistry using formalin fixed, ... Synthetic peptide corresponding to Human Bombesin Receptor 3 (intracellular) conjugated to Keyhole Limpet Haemocyanin (KLH). ...
Bombesin is a 14 amino acid peptide originally isolated from the skin of a frog. It has two known homologues in mammals called ... Retrieved from "https://www.wikidoc.org/index.php?title=Bombesin&oldid=670047" ...
Bombesin has two known homologues in mammals called neuromedin B and gastrin releasing peptide. Bombesin works on the ... Bombesin is a 14 amino acid peptide originally isolated from the skin of a frog. ... gastrointestinal tract neuroendocrine hormone and bombesin stimulates gastrin release from G cel... ... Bombesin is a 14 amino acid peptide originally isolated from the skin of a frog. Bombesin has two known homologues in mammals ...
... bombesin explanation free. What is bombesin? Meaning of bombesin medical term. What does bombesin mean? ... Looking for online definition of bombesin in the Medical Dictionary? ... bombesin. /bom·be·sin/ (bom´bĕ-sin) a tetradecapeptide neurotransmitter and hormone found in the brain and gut.. bombesin. [bom ... Related to bombesin: Motilin, dyshormonogenetic goiter bombesin. [bom´bĕ-sin] a tetradecapeptide neurotransmitter and hormone ...
Browse our Bombesin Receptor Activated Protein product catalog backed by our Guarantee+. ... Bombesin Receptor Activated Protein products available through Novus Biologicals. ... Diseases related to Bombesin Receptor Activated Protein. Discover more about diseases related to Bombesin Receptor Activated ... Bioinformatics Tool for Bombesin Receptor Activated Protein. Discover related pathways, diseases and genes to Bombesin Receptor ...
Rabbit Polyclonal Anti-Gastrin-releasing Peptide/Bombesin/Neuromedin C Antibody. Validated: WB, IHC, IHC-P. Tested Reactivity: ... Home » Gastrin-releasing Peptide/Bombesin/Neuromedin C » Bombesin Antibodies » Gastrin-releasing Peptide/Bombesin/Neuromedin C ... Blogs on Gastrin-releasing Peptide/Bombesin/Neuromedin C. There are no specific blogs for Gastrin-releasing Peptide/Bombesin/ ... Gastrin-releasing Peptide/Bombesin/Neuromedin C Antibody Summary. Immunogen. Synthetic 18 amino acid peptide from 2nd ...
Bombesin is a 14 amino acid peptide originally isolated from the skin of a frog. It has two known homologues in mammals called ... Background of Bombesin antibody. Bombesin is a 14 amino acid peptide originally isolated from the skin of a frog. It has two ...
... are selective ligands of the human bombesin receptor subtype-3 (BRS-3). They are therefore useful for the treatment, control, ... Certain novel substituted imidazoles are ligands of the human bombesin receptor and, in particular, ... Porcher, "Bombesin receptor subtype-3 is expressed by the enteric nervous . . . ", Cell Tissue Res. (2005), 21-31, vol. 320. ... Lebacq-Verheyden, "Bombesin and gastrin-releasing peptide: . . . ", Handbook of Exper. Pharmacol. (1990), 71-124, vol. 95. ...
The radiopharmaceutical {sup 99m}Tc-HYNlC-Bombesin is part of the gastrin-releasing peptide (GRP) analogues of bombesin that ... Validation of the production process of core-equipment HYNIC-Bombesin-Sn; Validacion del proceso de produccion del nucleo- ... In this paper, the prospective validation core-equipment HYNlC-Bombesin-Sn, which was shown consistently that the product meets ... Tc-HYNlC-Bombesin. The process was successfully validated and thereby ensuring the efficiency and effectiveness of this agent ...
bombesin ligand page. Quantitative data and detailed annnotation of the targets of licensed and experimental drugs. ... there is some ambiguity in the literature and on other resources as to the exact stereochemistry of bombesin. The structure ...
... png ImageSize=400px IUPACName= OtherNames= Section1= Chembox Identifiers CASNo=31362 50 2 PubChem=16133891 SMILES= ... Bombesin-like receptor 3 - The bombesin like receptor 3 (BRS 3) is a G protein coupled receptor.cite journal , author = Fathi Z ... Bombesin. Chembox new. ImageFile=Bombesin.png. ImageSize=400px. IUPACName=. OtherNames=. Section1= Chembox Identifiers. CASNo= ... Bombesin is a 14 amino acid. peptide. originally isolated from the skin. of a frog. . It has two known homolog. s in mammals. ...
Rapid desensitization and resensitization of bombesin-stimulated phospholipase D activity in Swiss 3T3 cells C P Briscoe ; C P ... the half-maximal stimulatory concentration of bombesin was an order of magnitude lower than that required for bombesin- ... The kinetics of bombesin-stimulated phospholipase D (PLD) activity were examined in Swiss 3T3 fibroblasts. The stimulated ... The roles of multiple pathways in regulating bombesin-stimulated phospholipase D activity in Swiss 3T3 fibroblasts Biochem J ( ...
Bombesin effects on human GI functions. Authors. Delle Fave, GAnnibale, BDe Magistris, LSeveri, CBruzzone, RPuoti, MMelchiorri ... In this article some of the actions of amphibian skin peptide Bombesin (BBS) on human gastrointestinal and pancreatic functions ... In this article some of the actions of amphibian skin peptide Bombesin (BBS) on human gastrointestinal and pancreatic functions ...
Bombesin/gastrin releasing peptide polyclonal antibodies from RDI Div of researchd Industries Intl/RRDI Divison of researchd ... ANTI-Bombesin/Gasrin releasing peptide (polyclonal) Polyclonal Antibody to Bombesin/GRP Cat#RDI-PRO16004 $312.00 Category ... Bombesin/GRP occurs frequently in the bronchial carcinoids. Absorption with 10-100 µg bombesin and GRP per ml diluted antiserum ... Immunogen Bombesin (#7113, Peninsula), conjugated to BSA Description/Specificity: Bombesin is an amphibian peptide and the ...
... has been shown to have a strong effect on core temperature lowering in rats: M. Brown et al., Science 196, 996 (1977 ... a bombesin-like immunoreactive peptide is found in both brain and gut, cf. J. M. Polak et al., Lancet 1, 1109 (1976). Other ... High levels of intracellular bombesin have also been found in human small-cell lung carcinoma: T. W. Moody et al., ibid. 214, ...
Autocrine activation of the tyrosine kinase associated with the bombesin receptor in small cell lung carcinoma ... 4 tyrosine bombesin stimulated phospholipase c activity in a membrane fraction from fibroblasts and small cell lung carcinoma ... Bombesin and gastrin releasing peptide increase tyrosine phosphorylation of focal adhesion kinase and paxillin in non-small ... A novel bombesin receptor antagonist inhibits autocrine signals in a small cell lung carcinoma cell line. Biochemical & ...
Bombesin is a gastrin-releasing peptide (GRP) analog that stimulates intestinal function; it was originally found in Bombina ... Yamada K, Wada E, Wada K. Bombesin-like peptides: studies on food intake and social behaviour with receptor knock-out mice. Ann ... Bombesin facilitates GABAergic transmission and depresses epileptiform activity in the entorhinal cortex. Hippocampus. 2014 Jan ... Bombesin exhibits antiepileptic/anticonvulsant potential, potentiating GABA release by increasing extracellular Ca2+ influx and ...
Radiolabeling of bombesin conjugates with [superscript 99m]Tc were optimized. The propyl amide C-terminally modified bombesin ... In an attempt to develop non-mitogenic bombesin analogs with antagonist targeting-vectors at the C-terminus, seven bombesin ... Further investigations of the role that chain lengths of the C-terminal vector play on the biological activity of the bombesin ... ACCESS RESTRICTED TO THE UNIVERSITY OF MISSOURI AT REQUEST OF AUTHOR.] Bombesin-like peptides bind to gastrin-releasing peptide ...
Targeting Human Prostate Cancer PC3 with Bombesin-Anti-DTPA Fab Bispecific Complexes and DTPA-polymer-drug conjugates for ... Pretargeting human prostate cancer PC3 xenografts with Bispecific Bombesin anti-diethylene triamine penta acetic acid (DTPA) ... Pretargeting with Bombesin alone showed no uptake of the radiolabeled polymers in tumors (0.44±0.17). When radiolabeled ... and PC3 cells pretargeted with Bispecific Bombesin-Anti-DTPA antibody Complex (BBACx), in vitro tumor toxicity was greater than ...
Bombesin and TPA (12-O-tetradecanoylphorbol 13-acetate) stimulate choline generation in Swiss 3T3 cells by a common mechanism. ... Bombesin and TPA (12-O-tetradecanoylphorbol 13-acetate) stimulate choline generation in Swiss 3T3 cells by a common mechanism ... Bombesin and TPA (12-O-tetradecanoylphorbol 13-acetate) stimulate choline generation in Swiss 3T3 cells by a common mechanism ... Bombesin and TPA (12-O-tetradecanoylphorbol 13-acetate) stimulate choline generation in Swiss 3T3 cells by a common mechanism ...
D-Phe6]bombesin(6-13)methyl ester ligand page. Quantitative data and detailed annnotation of the targets of licensed ...
Bombesin (BBN) is a fourteen amino acid peptide that binds to cancer cells overexpressing the gastrin-releasing peptide (GRP) ... Exploring protocols for synthesis of bombesin peptides derivatives to be used as GRP cancer receptor biomarkers [abstract]. ...
Publications] Maekawa, F. et al.: Distributions of two chicken bombesin receptors, bombesin receptor subtype-3.5(chBRS-3.5)and ... Journal Article] Distribution of two chicken bombesin receptors, bombesin receptor subtype-3.5 (chBRS-3.5) and gastrin- ... Journal Article] Distribution of two chicken bombesin receptors, bombesin receptor subtype-3.5 (chBRS-3.5) and gastrin- ... Journal Article] Distribution of two chicken bombesin receptors, bombesin receptor subtype-3.5 (chBRS-3.5) and gastrin- ...
  • Therefore, we investigated the effects of bombesin/gastrin-releasing peptide (GRP) antagonists RC-3940-II and RC-3095 on the growth of human ovarian carcinoma cell line OV-1063, xenografted into nude mice. (elsevier.com)
  • Receptors for bombesin are present on human ovarian cancers and bombesin-like peptides could function as growth factors in this carcinoma. (elsevier.com)
  • RT-PCR analysis showed that OV-1063 tumours expressed mRNA for bombesin receptor subtypes BRS-1, BRS-2, and BRS-3. (elsevier.com)
  • The bombesin receptors are a group of G-protein coupled receptors which bind bombesin. (wikipedia.org)
  • Bombesin activates three different G-protein coupled receptors known as BBR1 2 and 3. (genscript.com)
  • Bombesin also activates these receptors in the brain. (genscript.com)
  • Bombesin cross reacts with GRP receptors. (academic.ru)
  • it was originally found in Bombina toads and binds bombesin receptors (BBRs) and GRP receptors. (lktlabs.com)
  • The binding affinity profiles of the developed C-terminus modified bombesin-cyclen conjugates to the tumors overexpressing GRP-receptors were assessed using in-vitro competitive displacement of [superscript 125]I-BBN from human PC-3 prostate cancer cell line. (umsystem.edu)
  • The results obtained from the presented study demonstrate the potential of using bombesin analogs possessing antagonist C-terminal vectors as a candidate of choice for specific in vivo targeting of the tumors overexpressing GRP-receptors. (umsystem.edu)
  • Analysis of feeding and lipid metabolism regulation by bombesin-like peptide receptors. (nii.ac.jp)
  • We also have successfully cloned two bombesin-like peptide receptors, chGRP-R and chBRS-3.5 from chick brain. (nii.ac.jp)
  • These results recapitulate important roles of bombesin peptide receptors in vertebrates. (nii.ac.jp)
  • Journal Article] Distribution of two chicken bombesin receptors, bombesin receptor subtype-3.5 (chBRS-3.5) and gastrin-releasing peptide receptor (chGRP-R) mRNAs in the chicken telenephalon. (nii.ac.jp)
  • Journal Article] Molecular cloning and characterization of avian bombesin-like peptide receptors : new tools for investigating molecular basis for ligand selectivity. (nii.ac.jp)
  • Mammalian bombesin (Bn) receptors comprise 3 subtypes: BB1, BB2, BB3. (innoprot.com)
  • 99m Tc-labeled bombesin analogues have shown promise for noninvasive detection of many tumors that express bombesin (BN)/gastrin- releasing peptide (GRP) receptors. (elsevier.com)
  • Bombesin (BN)-like peptides and receptors for these peptides are widely distributed in mammalian peripheral tissues and the central nervous system. (mysciencework.com)
  • It has been postulated (P. J. Woll and E. Rozengurt, PNAS 85, 1859-1863, (1988)) that gastrin releasing factor antagonists would bind competitively to bombesin receptors in animals and would therefore be of use in the treatment of SCLC and/or in the control of clinical symptoms associated with this disease and due to hypersecretion of this peptide hormone. (allindianpatents.com)
  • Peptides, 1996, 17, 1337).After Bombesin/GRP cell receptors were established on SCLC cells, receptors were also found to be present on human prostate cells. (allindianpatents.com)
  • Prostate, 1994, 25: 29-38) showed tht the PC-3 and DU-145 human prostate cancer cell lines possess specific high- affinity receptors for bombesin/ GRP and are suitable models for the evaluation of anti-neoplastic activity of new bombesin/ GRP antagonists in the treatment of androgen- dependent prostate cancer. (allindianpatents.com)
  • Over-expression of GRP receptors for Bombesin has been reported to be found in malignant tissues, especially in prostate cancer. (ac.ir)
  • This Bombesin (BBN), a tetradecapeptide analog of human gastrin-releasing peptide (GRP) with a high binding affinity for GRP receptors (GRPR), is over- expressed in early stages of androgen-dependent prostate carcinomas, but not in advanced stages. (scirp.org)
  • Bombesin BN is a neuropeptide with a high affinity for these GRP receptors. (duhnnae.com)
  • The involvement of the bombesin receptors neuromedin receptor (NMBR) and gastrin-releasing peptide receptor (GRP-R) was also evaluated. (unicampania.it)
  • Qu X, Xiao D, Weber HC (2003) Biologic relevance of mammalian bombesin-like peptides and their receptors in human malignancies. (springer.com)
  • The aim of this research was to synthesize 177Lu-dendrimer(PAMAM-G4)-folate-bombesin with gold nanoparticles (AuNPs) in the dendritic cavity and to evaluate the radiopharmaceutical potential for targeted radiotherapy and the simultaneous detection of folate receptors (FRs) and gastrin-releasing peptide receptors (GRPRs) overexpressed in breast cancer cells. (uaemex.mx)
  • Receptors for bombesin are present on human ovarian cancers and bombesin-like peptides could function as growth factors in this carcinoma. (elsevier.com)
  • Bombesin is a 14-amino acid peptide originally isolated from the skin of the European fire-bellied toad (Bombina bombina). (wikipedia.org)
  • Synthetic peptide corresponding to Human Bombesin Receptor 3 (intracellular) conjugated to Keyhole Limpet Haemocyanin (KLH). (abcam.com)
  • Bombesin is a 14 amino acid peptide originally isolated from the skin of a frog . (wikidoc.org)
  • Bombesin has two known homologues in mammals called neuromedin B and gastrin releasing peptide. (genscript.com)
  • In the prostate gland NEP deactivates bombesin , endothelin-1 and calcitonin-gene-related peptide. (thefreedictionary.com)
  • Immunohistochemistry-Paraffin: Gastrin-releasing Peptide/Bombesin/Neuromedin C Antibody [NLS830] - Human Skin, Melanoma. (novusbio.com)
  • Immunohistochemistry: Gastrin-releasing Peptide/Bombesin/Neuromedin C Antibody [NLS830] - Analysis of anti-GRPR antibody with human pancreas, islet of Langerhans at 4 ug/ml. (novusbio.com)
  • Immunohistochemistry-Paraffin: Gastrin-releasing Peptide/Bombesin/Neuromedin C Antibody [NLS830] - Analysis of anti-GRPR antibody with human lung, non-small cell carcinoma. (novusbio.com)
  • Gastrin-releasing peptide receptor (GRPR) is a Bombesin Receptor. (novusbio.com)
  • The radiopharmaceutical {sup 99m}Tc-HYNlC-Bombesin is part of the gastrin-releasing peptide (GRP) analogues of bombesin that are radiolabelled with technetium 99 metastable for molecular images obtention. (worldwidescience.org)
  • As with many natural peptide ligands, there is some ambiguity in the literature and on other resources as to the exact stereochemistry of bombesin. (guidetopharmacology.org)
  • In this article some of the actions of amphibian skin peptide Bombesin (BBS) on human gastrointestinal and pancreatic functions are reviewed. (hku.hk)
  • Description/Specificity: Bombesin is an amphibian peptide and the mammalian counterpart is referred to as Gastrin Releasing Peptide (GRP). (researchd.com)
  • Bombesin-like peptides bind to gastrin-releasing peptide receptor subtype 2 (BB2) with significantly high binding affinity and specificity. (umsystem.edu)
  • However, pretreating cells with ionomycin decreased the effects of bombesin on both [Ca2+]i and insulin release, suggesting that elevation of [Ca2+]i was instrumental in the secretory response to this peptide. (biochemj.org)
  • Bombesin (BBN) is a fourteen amino acid peptide that binds to cancer cells overexpressing the gastrin-releasing peptide (GRP) receptor. (umsystem.edu)
  • The present invention discloses a novel peptide of the following general formula- D-Phe-Gln-Rl-R2-Val-R3-His-R-4-NH2 wherein Rl is Trp or D-Trp R2 is Ala, Aib or Deg R3 is Gly, Aib, Deg, Dpg or Ac5c R4 is Leu or lle These novel peptides are antagonists to bombesin and bombesin like peptides are useful in the treatment of cancer. (allindianpatents.com)
  • Bombesin is a 14 amino acid peptide which was first isolated from the skin of the frog Bombina bombina (Anastasi et al. (allindianpatents.com)
  • Analogues of bombesin/ GRP have been shown to inhibit the binding of gastrin releasing peptide to a SCLC cell line and to inhibit the growth of SCLC cells in-vitro and in-vivo (S. Mahmoud et al. (allindianpatents.com)
  • On the basis of structural homology and similar biological activity, gastrin-releasing peptide (GRP) has been considered the mammalian equivalent of amphibian bombesin. (elsevier.com)
  • Gastrin releasing peptide receptor (GRPR), also known as bombesin (BBN) receptor subtype II, is part of the group G protein-coupled receptor family of bombesin, and it has been reported to be useful in various types of cancer, including breast, prostate, colorectal, pancreatic, glioma, lung and gastrointestinal stromal cancers [3]. (scirp.org)
  • Bombesin action is peptide specific, exerted at a spinal site, and expressed through the sympathetic nervous system. (elsevier.com)
  • We propose to test our theory by incorporating nitroimidazoles (hypoxia trapping agents) into the structure of the Bombesin (BBN) peptide. (nebraska.edu)
  • Bombesin purified from amphibian skin, is homologous of mammalian gastrin-releasing peptide and is active in mammals. (unicampania.it)
  • The growth of the human gastrinoma model (PT) in athymic nude mice is stimulated by bombesin (BBS), an amphibian peptide homologous to both human gastrin-releasing peptide (GRP) and neuromedin B (NMB). (utmb.edu)
  • Central administration of bombesin (BN) (into the ventricular system) increased circulating levels of ACTH, corticosterone, epinephrine, norepinephrine and glucose, indicating that this peptide activates the hypothalamic-pituitary-adrenal (HPA) axis and sympathetic nervous system. (carleton.ca)
  • A decade later, the mammalian counterpart of bombesin was identified using an anti-bombesin antibody and named gastrin-releasing peptide (GRP). (springer.com)
  • Bombesin-like peptides, including NMB and gastrin-releasing peptide (GRP), are released by malignant tumor cells and become autocrine growth elements and mitogens that impact proliferation and cell routine development [3-5]. (livingseas.org)
  • Because a pentapeptide domain of α 1 AT (amino acids 370-374, Phe-Val-Phe-Leu-Met) is sufficient for binding to the SEC receptor and the sequence of this domain is remarkably similar to those of substance P, several other tachykinins, bombesin, and the amyloid-β peptide, we have examined the possibility that these other ligands bind to the SEC receptor. (elsevier.com)
  • ligands for the SEC receptor including peptide 105Y (based on α 1 AT sequence 359-374), α 1 AT-protease complexes, and bombesin do not compete for binding of substance P to a stable transfected cell line expressing the substance P receptor. (elsevier.com)
  • Therefore, we investigated the effects of bombesin/gastrin-releasing peptide (GRP) antagonists RC-3940-II and RC-3095 on the growth of human ovarian carcinoma cell line OV-1063, xenografted into nude mice. (elsevier.com)
  • To determine whether antagonists of growth hormone-releasing hormone (GHRH) and bombesin/gastrin-releasing peptide (BN/GRP) can inhibit the orthotopic and metastatic growth of PC-3 human androgen-independent prostate cancers. (beatingcancercenter.com)
  • Treatment of quiescent Swiss 3T3 mouse fibroblasts with bombesin resulted in a rapid 6-8-fold stimulation of cytosolic Ser/Thr kinase activities toward the S6 peptide (RRLSSLR), myelin basic protein (MBP), and the G peptide (SPQPSRRGSESSEE). (unipd.it)
  • The S6 peptide kinases as well as the two MBP kinases stimulated in response to bombesin are similar to those activated by epidermal growth factor in Swiss 3T3 fibroblasts which suggests that the early events of the signal transduction pathway mediated by these growth factors in Swiss 3T3 cells may converge in the activation of common Ser/Thr kinases. (unipd.it)
  • Bombesin, which acts as a sole mitogen for Swiss 3T3 fibroblasts, also produced a several-fold increase in the kinase activity toward the RRREEESEEE peptide, a specific substrate for CK-2. (unipd.it)
  • 9:00 EFFECTS OF BOMBESIN ON PROLACTIN SECRETION AND PITUITARY PROLACTIN LEVELS IN ADULT MALE RATS, Christi Kitchens [*], Cindy Rogers, and Thomas Toney, Georgia College & State University, Milledgeville, GA 31061. (thefreedictionary.com)
  • Inhibitory effects of bombesin/ GRP antagonist RC-3095 and somatostatin analogue RC-160 were also seen on growth of HT-29 human colon cancer xenografts in nude mice (Radulovic S et al. (allindianpatents.com)
  • We also studied the effects of bombesin on cell proliferation and motility and its direct effect on wound repair by observing the wound closure after mechanical injury. (unicampania.it)
  • 20073 Bombesin antibody staining of Rat dorsal horn. (acris-antibodies.com)
  • When radiolabeled polymers were replaced with DTPA-Doxorubicin-poly-l-glutamic acid (D-Dox-PGA) and PC3 cells pretargeted with Bispecific Bombesin-Anti-DTPA antibody Complex (BBACx), in vitro tumor toxicity was greater than free Dox toxicity by 2 fold. (controlledreleasesociety.org)
  • Intravenous infusion of the monoclonal bombesin antibody 2A11 abolished intravenous bombesin (10 μg/kg · h)-induced 33% inhibition of gastric response to pentagastrin but did not alter intrathecal bombesin (200 ng)-induced 38% inhibition of gastric response to pentagastrin. (elsevier.com)
  • Bombesin (BBS) is a tetradecapeptide originally isolated from amphibian skin1. (nih.gov)
  • bombesin - Pharmacologically active tetradecapeptide found in skins of European amphibians of the family Discoglossidae, principally Bombina bombina and Bombina variegata variegata. (academic.ru)
  • The tetradecapeptide bombesin was first isolated and characterized from the skin of the frog Bombina bombina in 1970. (springer.com)
  • Bombesin works on the gastrointestinal tract neuroendocrine hormone and bombesin stimulates gastrin release from G cells. (genscript.com)
  • The inhibitory effect of bombesin (200 ng) on pentagastrin-stimulated gastric secretion was reversed by bilateral adrenalectomy or removal of celiac and mesenteric ganglia. (elsevier.com)
  • The aim of this study was to elucidate the effect of Bombesin in an in vitro experimental model on a mechanically injured human keratinocyte monolayer. (unicampania.it)
  • Bombesin is also a tumor marker for small cell carcinoma of lung, gastric cancer, pancreatic cancer, and neuroblastoma. (wikipedia.org)
  • High levels of intracellular bombesin have also been found in human small-cell lung carcinoma. (thefreedictionary.com)
  • Consistent with its effects on [3H]InsP3 formation, bombesin raised the intracellular free Ca2+ concentration [(Ca2+]i) from a basal value of 0.28 +/- 0.01 microM to a peak of 1.3 +/- 0.1 microM by 20 s. (biochemj.org)
  • SIIA cells were treated with bombesin, and intracellular calcium mobilization was measured by means of fura-2 spectrofluorometry. (utmb.edu)
  • Chromatography of frog (Bombina orientalis) gut extracts demonstrated two peaks of bombesin-like immunoreactivity (BLI), one similar in size to GRP and one similar in size to amphibian bombesin. (elsevier.com)
  • They do not express L-dopa carboxylase or bombesin-like immunoreactivity. (atcc.org)
  • and variant SCLC cell lines (15 lines) which have undetectable levels of l -dopacarboxylase and bombesin-like immunoreactivity, but continue to express neuron-specific enolase and the brain isozyme of creatine kinase. (aacrjournals.org)
  • In an attempt to develop non-mitogenic bombesin analogs with antagonist targeting-vectors at the C-terminus, seven bombesin analogs were synthesized using HMBA resin. (umsystem.edu)
  • The synthetic procedures were optimized for convenient preparation of bombesin analogs possessing different moieties at the C-terminus. (umsystem.edu)
  • Three C-terminally modified bombesin analogs were synthesized and conjugated to a 6-bromohexanoic acid linker and subsequently to the cyclic tetraazabifunctional chelate, cyclen, using optimized solid-phase strategy. (umsystem.edu)
  • Further investigations of the role that chain lengths of the C-terminal vector play on the biological activity of the bombesin analogs in terms of being agonist, antagonist, or partial agonist are needed. (umsystem.edu)
  • Environment: The applicant will have access to Dr. Hoffman's laboratory (2,600 sq.ft.) fully equipped for the proposed synthesis and evaluation of the hypoxia enhanced Bombesin analogs. (nebraska.edu)
  • Bombesin is also a tumor marker for gastric cancer and neuroblastoma. (wikidoc.org)
  • Anatomical characterization of bombesin receptor subtype-3 mRNA expression in the rodent central nervous system. (nih.gov)
  • See the reference protein sequence for bombesin receptor subtype-3 (NP_690058.1). (nih.gov)
  • Certain novel substituted imidazoles are ligands of the human bombesin receptor and, in particular, are selective ligands of the human bombesin receptor subtype-3 (BRS-3). (patentgenius.com)
  • Journal Article] Leptin resistance and enhancement of feeding facilitation by melanin-concentrating hormone in mice lacking bombesin receptor subtype-3. (nii.ac.jp)
  • Journal Article] Leptin resistance and enhancement of feeding facilitaion by melanin-concentrating hormone in mice lacking bombesin receptor subtype-3. (nii.ac.jp)
  • AequoScreen® Double Transfected Cell Lines: Bombesin, BB3 subtype. (perkinelmer.de)
  • Northern blot analysis showed that fGRP is encoded by a mRNA of 980 bases, clearly different from the 750-base mRNA which encodes frog bombesin. (elsevier.com)
  • Northern blot analysis and in situ hybridization showed fGRP mRNA in frog brain and stomach and bombesin mRNA in frog skin, brain, and stomach. (elsevier.com)
  • Further, bombesin stimulates expression of c-jun and jun-B mRNA and protein and increases binding activity of AP-1 proteins. (utmb.edu)
  • RT-PCR analysis showed that OV-1063 tumours expressed mRNA for bombesin receptor subtypes BRS-1, BRS-2, and BRS-3. (elsevier.com)
  • These observations are consistent with those of other researchers who noted that another gastrointestinal neuropeptide called bombesin also appeared to inhibit feeding more potently at night (Kulkosky et al. (thefreedictionary.com)
  • Here we assessed the effect of a neuropeptide, bombesin, on keratinocytes during regeneration from scratch wounding. (unicampania.it)
  • The most potent analogues of bombesin were those in which positions one to five (not included) were altered, indicating that the decapeptide C terminal was sufficient for full potency. (meta.org)
  • Our results indicate that antagonists of bombesin/GRP inhibit the growth of OV-1063 ovarian cancers by mechanisms that probably involve the downregulation of c-jun and c-fos proto-oncogenes. (elsevier.com)
  • ChGRP-R is highly identical with mammalian and amphibian GRP-R, and this receptor showed high affinity for both GRP and bombesin. (nii.ac.jp)
  • ChBRS-3.5, having sequence similarities to both mammalian BRS-3 and amphibian BB4, showed moderate affinity for bombesin, but low affinity for both GRP and NMB. (nii.ac.jp)
  • 1995, 71, 1087), suggesting that bombesin- like peptides may have a role in the pathogenesis of colorectal cancer, and bombesin receptor antagonists may be of value in the treatment of receptor- positive tumours. (allindianpatents.com)
  • Novel 111In-labelled bombesin analogues for molecular imaging of prostate tumours - Descarga este documento en PDF. (duhnnae.com)
  • Studies with the anti-bombesin/GRP antibodies lead to the hypothesis that it may be possible to disrupt the autocrine growth cycle of bombesin/GRP using designed peptidereceptor antagonists. (allindianpatents.com)
  • The three Bombesin receptor subtypes couple primarily to the Gq/11 and G12/13 family of G proteins. (innoprot.com)
  • Bombesin suppresses feeding in rats. (nih.gov)
  • Bombesin (100-500 ng) injected intrathecally (T9-10) inhibited gastric acid secretion stimulated by pentagastrin and the GABA B agonist baclofen in urethane-anesthetized rats and basal gastric acid secretion in conscious, pylorus-ligated rats. (elsevier.com)
  • These results demonstrate that bombesin injected into the subarachnoid space of the spinal cord inhibits vagally stimulated and pentagastrinstimulated gastric secretion in rats. (elsevier.com)
  • Bombesin inhibits LH release in ovariectomized (OVX), estrogen primed rats. (nel.edu)
  • 177Ludendrimer( AuNP)-folate-bombesin may be useful as an optical and nuclear imaging agent for breast tumors overexpressing GRPR and FRs, as well as for targeted radiotherapy. (uaemex.mx)
  • GRPR, part of the bombesin (BBN) family, are overexpressed in many tumors, including breast and prostate cancer, and therefore represent an attractive target for future development. (stanford.edu)
  • Isolation and Structure of Bombesin and Alytesin, two Analogous Active Peptides from the Skin of the European Amphibians Bombina and Alytes" by A. ANASTASI, V. ERSPAMER and M. BuccI http://download.springer.com/static/pdf/258/art%253A10.1007%252FBF02145873.pdf?auth66=1384653010_1b792225201410812f5c123e46ce10a5&ext=.pdf[permanent dead link] Weber HC (February 2009). (wikipedia.org)
  • Pretargeting with Bombesin alone showed no uptake of the radiolabeled polymers in tumors (0.44±0.17). (controlledreleasesociety.org)
  • The neuromedin B receptor (NMB-R), an associate from the mammalian bombesin receptor family members, is generally overexpressed in a variety of tumors. (livingseas.org)
  • Launch Neuromedin B 51372-29-3 (NMB), an associate of a family group of mammalian bombesin-like peptides, exerts different physiological results on several features, including smooth-muscle contraction, exocrine and endocrine secretion, legislation of blood circulation pressure and sugar levels, and regular cellular development [1,2]. (livingseas.org)
  • In this research, mucosal localizations of bombesin, glucagon and somatostatin-14 immunoreactive in some regions of digestive tract of Gallus gallus domestica during the prenatal and postnatal periods were examined using ail immunohistochemical technique. (sdu.edu.tr)
  • In adult period, bombesin, glucagon and somatostatin-14 immunoreactive cells weren' t found in glandular epithelium of gizzard. (sdu.edu.tr)
  • Bombesin regulates cyclin D1 expression through the early growth response protein Egr-1 in prostate cancer cells. (genscript.com)
  • To determine the role of the DAG produced upon bombesin stimulation, we examined the effects of another activator of protein kinase C, the phorbol ester 12-O-tetradecanoylphorbol 13-acetate (TPA). (biochemj.org)
  • These data indicate that the initial secretory burst induced by bombesin results from the synergistic action of the high [Ca2+]i produced by InsP3 and DAG-activated protein kinase C. However, activation of protein kinase C alone appears to be sufficient for a sustained secretory response. (biochemj.org)
  • The results thus suggest that stimulation of the cells with either bombesin or TPA activates phospholipase D-catalysed phosphatidylcholine breakdown by a common mechanism involving the activation of protein kinase C. (biochemj.org)
  • That frogs have independent genes for both GRP and bombesin raises the possibility that mammals have an as yet uncharacterized gene encoding a true mammalian bombesin. (elsevier.com)
  • Bombesin/GRP occurs frequently in the bronchial carcinoids. (researchd.com)
  • Ab62284 (10ug/ml) staining human Bombesin Receptor 3 in pregnant uterus tissue by immunohistochemistry using formalin fixed, paraffin embedded tissue. (abcam.com)
  • Pretargeting human prostate cancer PC3 xenografts with Bispecific Bombesin anti-diethylene triamine penta acetic acid (DTPA) Fab Complexes (BBAFCx) and targeted with Tc-99m labeled DTPA-succinylated polylysine (DSPL) enabled molecular imaging of small prostate cancer lesions (1.5x1 mm lesions, 6.54±1.58 %ID/g). (controlledreleasesociety.org)
  • Bombesin also increased the penetration of the two human prostatic carcinoma cell lines, the relatively indolent LNCaP cells and the aggressively growing and invasive PC-3 cells, in an in vitro invasion of reconstituted basement membrane (Matrigel)(Hoosein NM et al. (allindianpatents.com)
  • Bombesin-induced inhibition of pentagastrin-stimulated gastric acid secretion was not altered by cervical cord transection. (elsevier.com)
  • Furthermore, the potency of bombesin to stimulate [3H]InsP3 generation (ED50 = 14 +/- 9 nM) agreed with its potency to stimulate insulin release (ED50 = 6 +/- 2 nM). (biochemj.org)
  • Among other naturally occurring peptides, alytesin was found to have 100% of bombesin potency whereas litorin, neurotensin, xenopsin, substance P, physalaemin, and eledoisin were found to be in the order of 10(4) times less potent. (meta.org)
  • Ghorbantabar Omrani H, Rezazadeh F, Sadeghzadeh N. Preparation and Radiochemical Evaluation of 99mTc-HYNIC-[Lys3,Tyr4] bombesin (3-14) for Prostate Cancer Detection. (ac.ir)
  • Here, we aimed at radiochemical and stability evaluation of a new bombesin derivative labeled with 99m Tc via HYNIC as a chelating agent and Tricine/EDDA as coligands that might be used for diagnosis of prostate cancer. (ac.ir)
  • This new bombesin derivative was easily labeled with 99m Tc using exchange labeling and has some promising characteristics for prostate cancer detection. (ac.ir)
  • Este articulo propone un Procedimiento que permite planificar, ejecutar y controlar la validacion de los metodos analiticos en el Departamento de Control de Calidad del Centro de Inmunologia Molecular. (worldwidescience.org)