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, 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.
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.
Reactome is pathway database which provides intuitive bioinformatics tools for the visualisation, interpretation and analysis of pathway knowledge.
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]. ...
4.0.1-hotfixescachetimestampsdevelopdpdk-ndagetsilivelibtrace4ndag_formatpfringrc-4.0.1rc-4.0.2rc-4.0.3rc-4.0.4ringdecrementfixringperformanceringtimestampfixes ...
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 ...
Data Availability StatementThe datasets used and/or analyzed through the current research are available through the corresponding writer on reasonable demand. microglial clone 3 cell range, HMC3, was founded in 1995, through SV40-reliant Thalidomide-O-amido-C3-NH2 (TFA) immortalization of human being embryonic microglial cells. Its been lately authenticated from the American Type Tradition Collection (ATCC?) and distributed beneath the name of HMC3 (ATCC?CRL-3304). The HMC3 cells have already been found in six clinical tests, two which indicated by ATCC also? as reference content articles. However, a far more accurate books revision shows that clone 3 was distributed beneath the name of CHME3. ...
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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
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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 - UR - 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 ...
Chemotherapie met AN-152 and AN-207 remt sterk de groei van vergevorderde vormen van kanker ontstaan vanuit endometriose met LHRH receptoren. Nieuwe studies toegevoegd die goede resultaten van gerichte aanpak bevestigen. Artikel update 7 november 2012
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... is a 14-amino acid peptide originally isolated from the skin of the European fire-bellied toad (Bombina bombina) by ... Bombesin is also a tumor marker for small cell carcinoma of lung, gastric cancer, pancreatic cancer, and neuroblastoma. The ... Erspamer 1988 finds bombesin has a similar effect on the chicken to ranatensin, unreliably increasing or decreasing blood ... 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. ...
... comprise a large family of peptides which were initially isolated from amphibian skin, where they ... Bombesin-like peptides, like many other active peptides, are synthesized as larger protein precursors that are enzymatically ... Chin WW, Krane IM, Naylor SL, Helin-Davis D, Spindel ER (1988). "Molecular cloning of cDNAs encoding the human bombesin-like ... In mammals and birds two categories of bombesin-like peptides are known, gastrin-releasing peptide (GRP), which stimulates the ...
Bombesin-like peptide receptors include gastrin-releasing peptide receptor, neuromedin B receptor, and bombesin-like receptor-3 ... bombesin receptor subtype 3, which demonstrates that it has a uniquepharmacology compared with other mammalian bombesin ... The bombesin receptor subtype 3 also known as BRS-3 or BB3 is a protein which in humans is encoded by the BRS3 gene. Mammalian ... "Entrez Gene: BRS3 bombesin-like receptor 3". Mantey SA, Weber HC, Sainz E, Akeson M, Ryan RR, Pradhan TK, Searles RP, Spindel ...
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 ... "Bombesin Receptors: BB1". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology ...
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 ... "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 ...
"There Are Three Distinct Forms of Bombesin: IDENTIFICATION OF [Leu13]BOMBESIN, [Phe13]BOMBESIN, AND [Ser3,Arg10,Phe13]BOMBESIN ... "Bombesin - an overview , ScienceDirect Topics". Retrieved 2022-01-07. Nagalla, Srinivasa R.; Barry, ... The skin of Oriental fire-bellied toads contains bombesin, a peptide first isolated from their relatives, European fire-bellied ... toads (and later other types of frogs, in the genera Rana and Phyllomedusa). Among other effects, bombesin hinders gastric ...
Preston, Shaun R.; Miller, Glenn V.; Primrose, John N. (1996). "Bombesin-like peptides and cancer". Critical Reviews in ...
These include secretin, acetylcholine, ATP, and bombesin. Cholangiocytes act through bile-acid independent bile flow, which is ...
The post-ganglionic fibers of the vagus nerve that innervate bombesin/GRP neurons of the stomach release GRP, which stimulates ... 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". ...
ISBN 978-0-89766-441-7. Gmerek DE, Cowan A (1988). "Role of opioid receptors in bombesin-induced grooming" (PDF). Annals of the ...
... (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 ...
Some of these include Gastrin, Bombesin, Avian Pancreatic Polypeptide, and cholecystokinin. The muscle contractions of the ...
... : 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 ...
"Hybrid Bombesin Analogues: Combining an Agonist and an Antagonist in Defined Distances for Optimized Tumor Targeting". Journal ...
"Activation of p300 histone acetyltransferase activity and acetylation of the androgen receptor by bombesin in prostate cancer ...
Stimulatory factor: bombesin or gastrin-releasing peptide (GRP) Inhibitory factor: somatostatin - acts on somatostatin-2 ... These include: stomach antrum distension vagal stimulation (mediated by the neurocrine bombesin, or GRP in humans) the presence ...
... inhibition of proliferation by vasoactive intestinal peptide and helodermin and enhancement of inhibition by anti-bombesin ...
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 ...
Motilin Neurotensin Substance P Somatostatin Bombesin Serotonin Angiotensin Nitric Oxide Kinins Histamine "The Endocrine System ...
... bombesin, bradykinin, endothelin, γ-aminobutyric acid (GABA), hepatocyte growth factor (HGF), melanocortins, neuropeptide Y, ...
PHI PHM PHV Endogenous Adrenomedullin Apelin Asprosin Bombesin Calcitonin Carnosine CART CLIP DSIP Enteroglucagon Formyl ...
... bombesin - bombesin receptor - bone morphogenetic protein - bradykinin - bradykinin receptor - BRCA1 - buffer solution C- ...
bombesin. BRS-3. bombesin receptor subtype-3. BSA. bovine serum albumin fraction V. CCK. cholecystokinin. CCK-R. ... Bombesin-receptor-subtype-3 (BRS-3) is an orphan G-protein-coupled receptor of the bombesin (Bn) family whose natural ligand is ... 2013) The role of bombesin and bombesin-related peptides in the short-term control of food intake. Prog Mol Biol Transl Sci 114 ... 1987) [D-Phe12]bombesin analogues: a new class of bombesin receptor antagonists. Am J Physiol 252:G439-G442. ...
Promotion by Bombesin of Gastric Carcinogenesis Induced by N-Methyl-N′-nitro-N-nitrosoguanidine in Wistar Rats Masaharu Tatsuta ... Prolonged administration of bombesin at 40 µg/kg led to a significant increase in the incidence and number per rat of gastric ... The effects of bombesin on the incidence, number, histological type, and depth of involvement of gastric cancers induced by N- ... However, bombesin at both dosages did not affect the histological appearance of the lesions or their depth of involvement. At ...
Bombesin and platelet-derived growth factor stimulate phosphatidylcholine breakdown by a common mechanism. ... Dive into the research topics of Bombesin and platelet-derived growth factor stimulate phosphatidylcholine breakdown by a ...
... bombesin, or pentagastrin. Three age groups (3-, 12-, and 24-months) male F344 rats received saline; CCK-8 (5 ng/kg), bombesin ... bombesin, or pentagastrin. Three age groups (3-, 12-, and 24-months) male F344 rats received saline; CCK-8 (5 ng/kg), bombesin ... bombesin, or pentagastrin. Three age groups (3-, 12-, and 24-months) male F344 rats received saline; CCK-8 (5 ng/kg), bombesin ... Aging and the trophic effects of cholecystokinin, bombesin and pentagastrin on the rat pancreas. Pancreas. 1991 Jul;6(4):407- ...
The structures reveal that both bombesin receptors contain an extended and deep pocket to adopt NMB and GRP, with the conserved ... Their functions are mediated by two G protein-coupled bombesin receptors, NMBR and GRPR. Here we present cryo-electron ... These findings also pave the way to facilitate rational design of therapies targeting bombesin receptors for the treatment of ... Neuromedin B (NMB) and gastrin-releasing peptide (GRP), two bombesin analogs, are endogenous itch-specific neuropeptides that ...
... of the bombesin analogue BAY 864367 for PET/CT in a small group of patients with primary and recurrent prostate cancer (PCa). ... F-labeled bombesin analogue. PET scans were assessed at 6 time points, up to 110 min after intravenous administration of 302 ± ...
Bombesin. -. - PP: Other. Gastrin releasing peptide. GRP. -. - Gas. Nitric oxide. NO. -. - Gas. Carbon monoxide. CO. -. - ...
The mitogenic G protein coupled receptor ligands bombesin, thrombin, and lysophosphatidic acid (LPA) and their receptors are ... The mitogenic G protein coupled receptor ligands bombesin, thrombin, and lysophosphatidic acid (LPA) and their receptors are ... The mitogenic G protein coupled receptor ligands bombesin, thrombin, and lysophosphatidic acid (LPA) and their receptors are ... The mitogenic G protein coupled receptor ligands bombesin, thrombin, and lysophosphatidic acid (LPA) and their receptors are ...
Bombesin receptor subtype-3 (BRS-3) is an orphan G-protein-coupled receptor (GPCR) member of the bombesin receptor family. ... Effect of bombesin receptor subtype-3 and its synthetic agonist on signaling, glucose transport and metabolism in myocytes from ...
Bombesin, which acts as a sole mitogen for Swiss 3T3 fibroblasts, also produced a several-fold increase in the kinase activity ... Bombesin, which acts as a sole mitogen for Swiss 3T3 fibroblasts, also produced a several-fold increase in the kinase activity ... The S6 peptide kinases as well as the two MBP kinases stimulated in response to bombesin are similar to those activated by ... The S6 peptide kinases as well as the two MBP kinases stimulated in response to bombesin are similar to those activated by ...
Receptors, Bombesin Associated data * * * ...
de Barros AL, Mota L, Ferreira CeA, Oliveira MC, Góes AM, Cardoso VN . Bombesin derivative radiolabeled with technetium-99m as ... Faintuch BL, Teodoro R, Duatti A, Muramoto E, Faintuch S, Smith CJ . Radiolabeled bombesin analogs for prostate cancer ...
Bombesin inhibits LH release in ovariectomized (OVX), estrogen primed rats.. Baranowska B, Wolinska-Witort E, Baranowska-Bik A ... Journal Article 2006; 27(1-2): 257-259 PubMed PMID: 16648808 Keywords: Animals, Bombesin:pharmacology, Estradiol:pharmacology, ... OBJECTIVE: Bombesin, 14-amino acid peptide, discovered in the gastrointestinal tract, is widely distributed in the central ... Baranowska B, Wolinska-Witort E, Baranowska-Bik A, Bik W, Chmielowska M, Martynska L. Bombesin inhibits LH release in ...
... bombesin, and the bombesin-related GRP (14). CGRP also increased GLP1 release in isolated perfused rat ileum (126). The ... Bombesin: action on gut hormones and calcium in man. J Clin Endocrinol Metab. 1982;54(5):980-985.. View this article via: ... In humans, GRP has been shown to stimulate the release of multiple gut hormones including CCK and GIP (127). The bombesin- ... Mammalian bombesin receptors: nomenclature, distribution, pharmacology, signaling, and functions in normal and disease states. ...
Bombesin (3) Bradykinin (10) Calcitonin Gene Related Peptide (CGRP) (5) Calpain (3) ...
Bombesin Receptors: BB2". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology ... Bombesin Receptors: BB2". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology ... Benya RV, Kusui T, Pradhan TK, et al. (1995). „Expression and characterization of cloned human bombesin receptors.". Mol. ... Corjay MH, Dobrzanski DJ, Way JM, et al. (1991). „Two distinct bombesin receptor subtypes are expressed and functional in human ...
Bombesin (3) Bone Morphogenetic Protein (BMP-2) (1) Bradykinin (10) Buforin 2 (1) ...
Bombesin is an analog of gastrin-releasing peptide and the truncated sequence bombesin(7-14) (BBN) is considered to be capable ... 18F-labeled bombesin analogs for targeting GRP receptor-expressing prostate cancer. J Nucl Med. 2006;47:492-501. ... Bombesin analogues for gastrin-releasing peptide receptor imaging. Nucl Med Biol. 2012;39:461-471. ... Methods: QDs were modified by β-Glu-RGD-BBN (RGD is arginine-glycine-aspartate acid, and BBN is bombesin) peptides and then ...
Effectof bombesin and neurotensin. World J. Gastr. 12, 3410-3415. Kypreou K, Kavvadas P, Karamessinis P, Peroulis M, Alberti A ... beneficial effect of bombesin neurotensin. J. Am. Coll. Surg. 198, 748-57 ...
Bombesin and gastrin-releasing peptide stimulate electrogenic ion transport in cultured human endometrial epithelial cell ...
Design, synthesis, and evaluation of radiolabeled bombesin conjugates for the diagnosis of breast cancer  Retzloff, Lauren ...
Body temperature as a mouse pharmacodynamic response to bombesin receptor subtype-3 agonists and other potential obesity ...
Alternative Names: BN, GRP10, Bombesin, Neuromedin C UniProt P07492 Sie sind hier: * Startseite ...
Bombesin-induced cytosolic Ca2+spiking in pancreatic acinar cells depends on cyclic ADP-ribose and ryanodine receptors. Cell ... Bombesin-induced cytosolic Ca2+spiking in pancreatic acinar cells depends on cyclic ADP-ribose and ryanodine receptors. Cell ...
Also known as mammalian bombesin.. Neuropeptide Y (NPY). Found in many noradrenergic neurons. Present in some secretomotor ...
Another drug, bombesin, uses a toxin found in the skin of the venomous European fire-bellied toad to treat gastrointestinal ... Bombesins ability to bind to neuronal tumors has led to interest in developing a florescent version that could guide surgeons ...
... bombesin, somatostatin, and neuron-specific enolase [NSE]), though this staining does not correlate with clinical activity. ...
Masuda, T., Amann, L., Monaco, G., Sankowski, R., Staszewski, O., Krueger, M., Del Gaudio, F., He, L., Paterson, N., Nent, E., Fernández-Klett, F., Yamasaki, A., Frosch, M., Fliegauf, M., Bosch, L. F. P., Ulupinar, H., Hagemeyer, N., Schreiner, D., Dorrier, C., Tsuda, M., & 10 othersGrothe, C., Joutel, A., Daneman, R., Betsholtz, C., Lendahl, U., Knobeloch, K. P., Lämmermann, T., Priller, J., Kierdorf, K. & Prinz, M., Apr 28 2022, In: Nature. 604, 7907, p. 740-748 9 p.. Research output: Contribution to journal › Article › peer-review ...
RECEPT BOMBESIN. Entry Term(s). Bombesin Receptor Bombesin Receptors Gastrin-Releasing Peptide Receptor Gastrin-Releasing ... Receptors, Bombesin Preferred Concept UI. M0027187. Registry Number. 0. Scope Note. Cell surface proteins that bind bombesin or ... use RECEPTORS, BOMBESIN (NM) to search BOMBESIN RECEPTOR 1982-93 & NEUROMEDIN B RECEPTOR 1992-93. History Note. 94; was ... Receptors, Bombesin Preferred Term Term UI T053817. Date01/01/1999. LexicalTag NON. ThesaurusID NLM (1994). ...
  • Their functions are mediated by two G protein-coupled bombesin receptors, NMBR and GRPR. (
  • The structures reveal that both bombesin receptors contain an extended and deep pocket to adopt NMB and GRP, with the conserved C-terminal motif of GH(F/L)M from both peptides to contact the toggle switch residues for the receptor activation. (
  • Together with mutational and functional data, our structures reveal the mechanism of ligand selectivity and specific activation of the bombesin receptors. (
  • These findings also pave the way to facilitate rational design of therapies targeting bombesin receptors for the treatment of pruritus. (
  • Molecular cloning and characterization of receptors for the mammalian bombesin-like peptides. (
  • GRP 18-27 (neuromedin C), and neuromedin B are endogenous ligands of bombesin receptors in mammals. (
  • Lung tumours are known to overexpress receptors for bombesin-like peptides. (
  • Neuromedin B (NMB) and gastrin-releasing peptide (GRP), two bombesin analogs, are endogenous itch-specific neuropeptides that induce histaminergic and nonhistaminergic itch, respectively. (
  • The receptor of the bombesin/gastrin releasing peptide (GRP), which is overexpressed in PCa with neuroendocrine differentiation, also represents an innovative research field with diagnostic and therapeutic applications through, respectively, positron and beta emitters. (
  • QDs were modified by β-Glu-RGD-BBN (RGD is arginine-glycine-aspartate acid, and BBN is bombesin) peptides and then labeled with 18 F via the 4-nitrophenyl-2- 18 F-fluoropropionate prosthetic group. (
  • Cell surface proteins that bind bombesin or closely related peptides with high affinity and trigger intracellular changes influencing the behavior of cells. (
  • However, thus far, no study has demonstrated the potential role of bombesin-like peptides in identifying A549 lung tumour cells in xenograft animal models. (
  • Bombesin-receptor-subtype-3 (BRS-3) is an orphan G-protein-coupled receptor of the bombesin (Bn) family whose natural ligand is unknown and which does not bind any natural Bn-peptide with high affinity. (
  • Repositorio consejería de sanidad de madrid: Effect of bombesin receptor subtype-3 and its synthetic agonist on signaling, glucose transport and metabolism in myocytes from patients with obesity and type 2 diabetes. (
  • Radiolabeled bombesin analogs for prostate cancer diagnosis: preclinical studies. (
  • Bombesin receptor subtype-3 (BRS-3) is an orphan G-protein-coupled receptor (GPCR) member of the bombesin receptor family. (
  • 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). (
  • 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. (
  • 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. (
  • Uptake of QD-RGD-BBN in PC-3 cells showed no significant decrease in the presence of an excess amount of dimer arginine-glycine-aspartate acid (RGD 2 ) or bombesin(7-14) (BBN) peptide but was blocked significantly in the presence of an excess amount of NH 2 -RGD-BBN. (
  • This indicates that the bombesin-induced activation of these enzymes is mediated by a Ser/Thr phosphorylation event. (
  • The effects of bombesin on the incidence, number, histological type, and depth of involvement of gastric cancers induced by N -methyl- N '-nitro- N -nitrosoguanidine (MNNG) were investigated in male Wistar rats. (
  • Prolonged administration of bombesin at 40 µg/kg led to a significant increase in the incidence and number per rat of gastric cancers of the glandular stomach at Week 52. (
  • In rats that had received alternate-day injections of 20 µg/kg of bombesin, the number of gastric cancers per rat, but not the incidence of cancer, was significantly more than in untreated rats. (
  • Bombesin affects vascular and other smooth muscle, gastric secretion, and renal circulation and function. (
  • Rats received alternate-day s.c. administration of 20 or 40 µg/kg body weight of bombesin in depot form after p.o. treatment with the carcinogen for 25 weeks. (
  • We conclude that, at the dosages tested, the trophic response of pancreas to chronic administration of CCK, bombesin, and pentagastrin, which is normally present in young adult rats, is lost with aging. (
  • Bombesin inhibits LH release in ovariectomized (OVX), estrogen primed rats. (
  • Dosimetry and first clinical evaluation of the new 18F-radiolabeled bombesin analogue BAY 864367 in patients with prostate cancer. (
  • Dr. Marc Reitman , Chief, Diabetes, Endocrinology and Obesity Branch, is interested in the mechanisms underlying energy homeostasis including metabolic rate and body temperature regulation, brown adipose tissue physiology, drug treatments for obesity, and BRS-3 (bombesin receptor subtype-3). (
  • DISCUSSION: The data obtained in this study indicate that Tc-HYNIC-ßAla-Bombesin(7-14) may be useful as an imaging probe to detect A549 lung cancer cells. (
  • We examined the effect of age on the trophic response of the pancreas to chronic treatment with cholecystokinin (CCK), bombesin, or pentagastrin. (
  • The bombesin-stimulated CK-2 activity could not be measured in whole cytosols but was revealed by the anion exchange chromatography step. (
  • Two distinct bombesin receptor subtypes are expressed and functional in human lung carcinoma cells. (
  • Here we examined the quantitative and additive properties of this tumor-promoting event and examined whether this promotion could be nullified by treatment with a bombesin antagonist, which down-regulates epidermal growth factor receptors. (
  • Receptors for bombesin are present on human ovarian cancers and bombesin-like peptides could function as growth factors in this carcinoma. (
  • Expression and characterization of cloned human bombesin receptors. (
  • Bombesin receptors in the brain. (
  • GRP 18-27 (neuromedin C), and neuromedin B are endogenous ligands of bombesin receptors in mammals. (
  • Our laboratory focuses on the structure, function, and regulation of mammalian receptors for bombesin-like peptides. (
  • Both peptides show remarkable sequence identity to bombesin over their carboxy-terminal ends - the region essential for high-affinity binding to receptors and all biologic responses attributed to mammalian bombesin-like peptides. (
  • In addition, they regulate the growth of cultured fibroblasts expressing bombesin receptors and have been implicated as autocrine growth factors that modulate the growth of some human carcinomas. (
  • This wide spectrum of biologic activity raises interesting questions about the receptors for bombesin-like peptides: How many receptors are there? (
  • To learn more about the molecular mechanisms governing the responses elicited by mammalian bombesin-like peptides, our lab has cloned and characterized cDNAs and then genes that encode three structurally similar, but pharmacologically distinct, receptors for such peptides. (
  • With Robert Jensen's lab at NIDDK, we are investigating which segments of bombesin receptors are critical for high affinity binding of agonists and antagonists. (
  • We have created mutant receptors, which can no longer couple to G-proteins, to help determine if coupling is essential for receptor internalization and other events, such as phosphorylation, that occur when bombesin receptors are activated. (
  • It is >10,000-fold selective for BB 3 over the other two mammalian bombesin receptors. (
  • 1 Gastrin-releasing peptide receptor is one of the 4 known bombesin receptors overexpressed in prostate cancer. (
  • Current research interests include the development of receptor antagonists for the bombesin receptors 1 and 3, which are of potential use in inflammatory lung disease and lung cancer, as well as development of urotensin II antagonists of potential therapeutic value in the cardiovascular area. (
  • Dr. Coy's group is also researching the use of peptide agonist analogs, particularly somatostatin and bombesin, for the specific targeting and proactive internalization of cytotoxic agents and anti-sense oncogene constructs into tumor cells which heavily over-express receptors for several families of peptides. (
  • Using effective dosages of RC-3095 (1C3 nmol) and PD168368 (3C10 nmol), the ultimate work was to determine whether scratching elicited by bombesin, which includes fairly high binding affinity for both GRPr and NMBr, could possibly be obstructed by pretreatment with RC-3095 or PD168368 by itself or by administration of an assortment of RC-3095 and PD168368. (
  • It follows that the application of GRPR-targeting, radiolabelled bombesin analogues to the imaging and treatment of various neoplasms has raised considerable interest over the past 20 years [ 9 ]. (
  • The researchers injected mice with a toxin (bombesin-sap) designed to bind to a group of neurons expressing GRPR. (
  • To confirm bombesin-sap was destroying only the neurons containing GRPR, the scientists analyzed subpopulations of neurons in the spinal cord by using lamina-specific molecular markers and found that subpopulations of neurons expressing other neuronal markers were not affected by the toxin. (
  • Prange, Arthur J. / Effects of intracisternal neurotensin, β-endorphin or bombesin on ethanol-induced sedation and hypothermia . (
  • Bombesin is a neuropeptide originally discovered in the skin of the Fire-Bellied Toad, Bombina Bombina. (
  • Bombesin is the neuropeptide of the cold sweat. (
  • May potentiate mitogenesis induced by the neuropeptide bombesin by mediating an increase in the duration of MAPK1/3 (ERK1/2) signaling, which leads to accumulation of immediate-early gene products including FOS that stimulate cell cycle progression (By similarity). (
  • The science of a sigh was discovered by Jack Feldman and colleagues and is distinctly controlled by bombesin-like neuropeptide pathways which signal to breathing control centers in the brain stem. (
  • The bombesin neuropeptide pathways suggest potential pharmacologic approaches for controlling excessive sighing (or overbreathing), which is known to cause a cascade of symptoms including anxiety, hypertension, and metabolic dysfunction and beyond by inducing sighs in individuals that cannot breathe deeply on their own. (
  • In order to characterize the signal transduction pathways responsible for proto-oncogene activation, we treated Swiss 3T3 cells with the tumor promoter phorbol dibutyrate to generate cells deficient in protein kinase C. These cells were then stimulated with platelet extract, bombesin, or epidermal growth factor (EGF) and the levels of c-myc and c-fos mRNA were determined. (
  • Another group of animals received bombesin antagonist RC-3095 for 4 weeks during the time incisions were made, again measuring promotion. (
  • Inhibitory effects of the new bombesin receptor antagonist RC-3095 on the luteinizing hormone release in rats. (
  • AM-37 and ST-36 Are Small Molecule Bombesin Receptor Antagonists. (
  • Bombesin Receptor Family Activation and CNS/Neural Tumors: Review of Evidence Supporting Possible Role for Novel Targeted Therapy. (
  • Mice lacking the orphan G protein-coupled receptor bombesin-like receptor subtype-3 (Brs3) are obese, with reduced energy expenditure and increased food intake. (
  • Bombesin-like receptor 3 (Brs3) expression in glutamatergic, but not GABAergic, neurons is required for regulation of energy metabolism. (
  • Baranowska B. Bombesin modulates the control of energy homeostasis and pituitary hormone release. (
  • Regulation of body temperature and brown adipose tissue thermogenesis by bombesin receptor subtype-3. (
  • His particular interests include studying mouse genetics and pharmacology, using mouse models to understand metabolic rate regulation, body temperature regulation and the role of BRS-3 (bombesin receptor subtype-3), and exploring drug treatments for obesity. (
  • The research highlights that in excitation of these neurons and subsequent secretion of bombesin like neuropeptides activates neurons in the preBotC, the brain stem region responsible for driving inspiration, to initiate sighs by altered neuronal activity which converts normal breathing rhythms into sighs, resulting in a double-sized breath. (
  • 2017) Radiolabeled bombesin derivatives for preclinical oncological imaging. (
  • Search for an Endogenous Bombesin-Like Receptor 3 (BRS-3) Ligand Using Parabiotic Mice. (
  • Cloning, expression, and mapping of a gene that is upregulated in adipose tissue of mice deficient in bombesin receptor subtype-3. (
  • BB2 Bombesin Receptor is aberrantly expressed in numerous cancers such as those of the lung, colon, and prostate. (
  • 18. Imaging of Prostate Cancer Using Gallium-68-Labeled Bombesin. (
  • RT-PCR analysis showed that OV-1063 tumours expressed mRNA for bombesin receptor subtypes BRS-1, BRS-2, and BRS-3. (
  • Platelet extract or bombesin, which stimulate PI turnover, were substantially weaker inducers of c-myc and c-fos mRNA levels in the protein kinase C-depleted cells, although some variability with platelet extract was noted. (
  • Innoprot HiTSeeker BB2 Bombesin Receptor Cell Line allows to assay compounds, or analyze their capability to modulate BB2 receptor. (
  • BB2 Bombesin Receptor Assay from Innoprot allows the measurement of BB2 Bombesin receptor activation by Calcium concentration increase in the cytosol. (
  • Immunohistochemical colocalization of bombesin with Ki67 did not reveal active NEC proliferation. (
  • and the third, called bombesin-receptor subtype 3 (BRS-3), binds neither GRP nor NMB with high affinity. (
  • Many of us searched for to determine LY2090314 research buy cyclooxygenase-2 (COX-2) expression in bombesin-inhibited DCs addressed with theanine throughout vitro and to investigate the protection and also activation results of theanine in DCs. (
  • 257. Suppression of body temperature and metabolism after centrally-administered bombesin. (
  • A few years ago, Feldman's lab showed that a substance called bombesin could increase sighing in rodents. (
  • Inhibition of growth of OV-1063 human epithelial ovarian cancers and c- jun and c- fos oncogene expression by bombesin antagonists. (
  • Together, the researchers identified two clusters of cells in the brain stem that responded to bombesin. (
  • The amount of cellular apoptosis with all the treatment of bombesin and also theanine substantially diminished, making up 20.9%, in comparison with 26.1% regarding cell apoptosis with bombesin. (
  • Activation of bombesin receptor Subtype-3 by [D-Tyr(6),β-Ala(11),Phe(13),Nle(14)]bombesin(6-14) increased glucose uptake and lipogenesis in human and rat adipocytes. (
  • Humans, of course, inherit all the classic defense mechanisms of our ancestral species, including Bombesin-mediated responses and even the Unken Reflex. (
  • This work confirms that the promoting event of a laser incision follows a comparable time course to release of growth factors after such an incision and that it can be eliminated by treatment with bombesin antagonists. (
  • 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. (
  • Techniques Enzyme-linked innmunosorbent analysis (ELISA), invert transcription-polymerase sequence of events (RT-PCR), and also Western blotting were utilized to research the effects involving theanine on COX-2 phrase along with interleukin ()-12/IL-10 release of bombesin-treated DCs. (
  • Methods: Bombesin immunoreactivity was quantified in lung biopsy specimens from 13 children with characteristic clinical presentation and imaging appearance of NEHI. (
  • If it smells skanky, there is probably a persistant fear-response associated with excess release of Bombesin. (