Medicinal chemistry of somatostatin analogs leading to the DTPA and DOTA conjugates of the multi-receptor-ligand SOM230.

Abstract:

:The somatostatin field has been a success story in terms of medicinal chemistry and drug discovery offering a variety of therapeutic opportunities. A rational medicinal chemistry approach capitalising on structure activity relationships has led to the discovery of SOM230, a novel, stable cyclohexapeptide somatostatin analog which exhibits multi-receptor binding to human somatostatin receptor (SSTR) subtypes (SSTR 1-5). Recently, we extended this research utilising the hydroxproline urethane extension of SOM230 for the attachment of the chelators DTPA and DOTA, which enable early diagnosis of SSTR positive tumors and radiotherapy.

journal_name

J Endocrinol Invest

authors

Lewis I,Albert R,Kneuer R,Pless J,Simeon C,Kerrad S,Hoyer D,Bruns C

subject

Has Abstract

pub_date

2005-01-01 00:00:00

pages

15-20

issue

11 Suppl International

eissn

0391-4097

issn

1720-8386

journal_volume

28

pub_type

杂志文章
  • Reversible cerebral ischemia in patients with pheochromocytoma.

    abstract::Cerebral ischemia and symptoms of stroke can occur as a rare manifestation in patients with pheochromocytoma. We describe a 45-year-old woman who was admitted because of a right-sided hemiparesis due to an ischemic lesion in the left hypothalamus. The clinical diagnosis of a pheochromocytoma was proven by highly eleva...

    journal_title:Journal of endocrinological investigation

    pub_type: 杂志文章

    doi:10.1007/BF03343544

    authors: Lehmann FS,Weiss P,Ritz R,Harder F,Staub JJ

    更新日期:1999-03-01 00:00:00

  • Clinical and genetic characteristics of familial hypercholesterolemia patients with type 2 diabetes.

    abstract:PURPOSE:Though type 2 diabetes mellitus (T2DM) is an important and independent risk factor for coronary artery disease (CAD) in the general population, the impact of T2DM on CAD in patients with familial hypercholesterolemia (FH) is less understood. Thus, the current study aimed to examine the features of FH patients w...

    journal_title:Journal of endocrinological investigation

    pub_type: 杂志文章

    doi:10.1007/s40618-018-0959-0

    authors: Sun D,Cao YX,You XD,Zhou BY,Li S,Guo YL,Zhang Y,Wu NQ,Zhu CG,Gao Y,Dong QT,Liu G,Dong Q,Li JJ

    更新日期:2019-05-01 00:00:00

  • Immunoreactive thyroglobulin in sera and saliva of patients with various thyroid disorders: role of autoantibodies.

    abstract::The present study was designed to assess the transfer of thyroglobulin (Tg) and anti-Tg antibodies (TgAb) to saliva in subjects with positive TgAb in their sera. Group I consisted of normal euthyroid control subjects (n = 10). Group II were patients with various thyroid disorders and no TgAb in their sera (n = 6). Gro...

    journal_title:Journal of endocrinological investigation

    pub_type: 杂志文章

    doi:10.1007/BF03349955

    authors: Van Herle AJ,Rosenblit PD,Van Herle TL,Van Herle P,Greipel M,Kellett K

    更新日期:1989-03-01 00:00:00

  • The pathogenesis of pseudohyperaldosteronism from carbenoxolone.

    abstract::Carbenoxolone is a derivative of glycyrrhetinic acid used for the treatment of peptic ulcer and gastritis, with salt and water retention a very common side-effect. To investigate this drug-induced pseudohyperaldosteronism we have studied 6 male volunteers before, during and after treatment with carbenoxolone for 7 day...

    journal_title:Journal of endocrinological investigation

    pub_type: 杂志文章

    doi:10.1007/BF03350002

    authors: Armanini D,Scali M,Zennaro MC,Karbowiak I,Wallace C,Lewicka S,Vecsei P,Mantero F

    更新日期:1989-05-01 00:00:00

  • Is elevated urotensin II level a predictor for increased cardiovascular risk in subjects with acromegaly?

    abstract:PURPOSE:Acromegaly is a rare disorder existed in the result of overproduction of growth hormone (GH). The disorder is associated with increased cardiovascular risk factors and metabolic abnormalities. Urotensin II (UII), a secreted vasoactive peptide hormone, belonging somatostatin superfamily, plays an essential role ...

    journal_title:Journal of endocrinological investigation

    pub_type: 杂志文章

    doi:10.1007/s40618-018-0905-1

    authors: Demirpence M,Guler A,Yilmaz H,Sayin A,Pekcevik Y,Turkon H,Colak A,Ari EM,Aslanipour B,Kocabas GU,Calan M

    更新日期:2019-02-01 00:00:00

  • Cardiac structure and functions in patients with asymptomatic primary hyperparathyroidism.

    abstract:BACKGROUND:The data about cardiovascular (CV) changes in patients with asymptomatic primary hyperparathyroidism (PHPT) are scarce. AIM:The aim of this study is to compare cardiac structure and functions in patients with asymptomatic PHPT and controls by using tissue Doppler echocardiography. SUBJECTS AND METHODS:Thir...

    journal_title:Journal of endocrinological investigation

    pub_type: 杂志文章

    doi:10.3275/8961

    authors: Aktas Yılmaz B,Akyel A,Kan E,Ercin U,Tavil Y,Bilgihan A,Cakır N,Arslan M,Balos Toruner F

    更新日期:2013-11-01 00:00:00

  • The age of patients with thyrotoxicosis factitia in Italy from 1973 to 1996.

    abstract::Thyrotoxicosis factitia, a syndrome due to the surreptitious ingestion of excess thyroid hormones, has generally been diagnosed in young or middle-aged women with psychopathological disturbances. We reviewed all the cases seen at our Institution over a 24-yr period, from 1973 to 1996. All 25 patients were women. Analy...

    journal_title:Journal of endocrinological investigation

    pub_type: 杂志文章

    doi:10.1007/BF03350892

    authors: Bogazzi F,Bartalena L,Scarcello G,Campomori A,Rossi G,Martino E

    更新日期:1999-02-01 00:00:00

  • Effects of naloxone on adrenal cortex regulation in patients with primary aldosteronism.

    abstract::Excess production of proopiomelanocortin (POMC)-derived peptides with aldosterone-stimulating activity has been suggested to play a pathogenetic role in idiopathic hyperaldosteronism (IHA). To further investigate this issue, the opiate receptor antagonist naloxone was administered to 14 patients with primary aldostero...

    journal_title:Journal of endocrinological investigation

    pub_type: 杂志文章

    doi:10.1007/BF03350149

    authors: Fallo F,Boscaro M,Sonino N,Mantero F

    更新日期:1988-04-01 00:00:00

  • Association between emotional and behavioral problems and metabolic control in children and adolescents with Type 1 diabetes.

    abstract:OBJECTIVE:We aimed to investigate the differences in emotional and behavioral problems and to explore the association between the level of psychiatric problems and the metabolic control in Type 1 diabetes. METHODS:The children with Type 1 diabetes (no.=42) and the "healthy" control group (no.=42), their parents and en...

    journal_title:Journal of endocrinological investigation

    pub_type: 杂志文章

    doi:10.1007/BF03345721

    authors: Akbaş S,Karabekiroğlu K,Ozgen T,Tasdemir G,Karakurt M,Senses A,Böke O,Aydin M

    更新日期:2009-04-01 00:00:00

  • Bringing the body of the iceberg to the surface: the Female Sexual Dysfunction Index-6 (FSDI-6) in the screening of female sexual dysfunction.

    abstract:PURPOSE:Female Sexual Dysfunction (FSD) is a still poorly studied and underdiagnosed condition. The aim of the study was to produce an improved version of FSFI-6 (6-Item Version of the Female Sexual Function Index), entitled Female Sexual Dysfunction Index-6 (FSDI-6), and to estimate its accuracy as a screening instrum...

    journal_title:Journal of endocrinological investigation

    pub_type: 杂志文章

    doi:10.1007/s40618-015-0378-4

    authors: Maseroli E,Fanni E,Fambrini M,Ragghianti B,Limoncin E,Mannucci E,Maggi M,Vignozzi L

    更新日期:2016-04-01 00:00:00

  • Influence of the neonatal suppression of TSH production (neonatal hyperthyroidism) on response to TSH in adulthood.

    abstract::Six-day treatment of neonatal rats with T3 or T4 resulted in a considerable depression of T4 production in response to exogenous TSH in adulthood. This supports the hypothetical conclusion that hormonal imprinting, i.e. the presence of the hormone and its interaction with the cell during the period of receptor maturat...

    journal_title:Journal of endocrinological investigation

    pub_type: 杂志文章

    doi:10.1007/BF03348561

    authors: Csaba G,Nagy SU

    更新日期:1985-12-01 00:00:00

  • Effects of a short-term calcium and vitamin D treatment on serum cytokines, bone markers, insulin and lipid concentrations in healthy post-menopausal women.

    abstract::In vitro studies have shown that 1,25 dihydroxyvitamin D3 [1,25(OH)2D3] decreases cytokine production by monocytes and lymphocytes. In addition, intravenous or oral pulse calcitriol treatment suppresses interleukin 6 (IL6) and interleukin1beta (IL1beta) in hemodialysis patients. We studied the effect of a daily 12-wee...

    journal_title:Journal of endocrinological investigation

    pub_type: 临床试验,杂志文章

    doi:10.1007/BF03347358

    authors: Gannagé-Yared MH,Azoury M,Mansour I,Baddoura R,Halaby G,Naaman R

    更新日期:2003-08-01 00:00:00

  • Chronobiology of catecholamine excretion in normal and diabetic men.

    abstract::The adrenomedullary response to stimuli is often elevated in poorly controlled insulin dependent diabetic patients, and it is controversial whether the adrenomedullary hyperactivity induces the suppression of the circadian rhythm of catecholamines. We have studied the urinary excretion of catecholamines in 11 diabetic...

    journal_title:Journal of endocrinological investigation

    pub_type: 杂志文章

    doi:10.1007/BF03348628

    authors: Del Rio G,Carani C,Baldini A,Marrama P,Della Casa L

    更新日期:1990-07-01 00:00:00

  • Use of low-dose radioiodine ablation for Graves' orbitopathy: results of a pilot, perspective study in a small series of patients.

    abstract:OBJECTIVE:Elimination of thyroid antigens by total thyroid ablation (TTA), namely, thyroidectomy followed by radioiodine, may be beneficial for Graves' Orbitopathy (GO). TTA is usually performed with a 131I dose of 30 mCi. In Italy, this dose must be followed by a 24-h protected hospitalization, with increase in the wa...

    journal_title:Journal of endocrinological investigation

    pub_type: 杂志文章

    doi:10.1007/s40618-017-0754-3

    authors: Leo M,Sabini E,Ionni I,Sframeli A,Mazzi B,Menconi F,Molinaro E,Bianchi F,Brozzi F,Santini P,Elisei R,Nardi M,Vitti P,Marcocci C,Marinò M

    更新日期:2018-03-01 00:00:00

  • An in vitro procedure for the estimation of thyroid hormone releasing factors in sera of thyrotoxic patients.

    abstract::LATS containing sera and a number of Graves' disease sera stimulated T4 release from mouse thyroids in vitro as determined by RIA, thus confirming the presence of a thyroid hormone releasing factor in sera of thyrotoxic patients. The pattern of stimulation was similar to that previously shown for TSH in terms of T4 re...

    journal_title:Journal of endocrinological investigation

    pub_type: 杂志文章

    doi:10.1007/BF03350973

    authors: Maayan ML,Volpert EM,Dawry FP

    更新日期:1978-10-01 00:00:00

  • The inductive effects of progestogens on aromatase activity in stromal cells of human uterine endometrium.

    abstract::Aromatase activity for androstenedione was measured in stromal cells of human uterine endometrium throughout the menstrual cycle. The effect of progestogen on aromatase activity was also examined in the endometrial stromal cells. Aromatase activity tended to be high in the proliferative cells compared to the secretory...

    journal_title:Journal of endocrinological investigation

    pub_type: 杂志文章

    doi:10.1007/BF03349962

    authors: Yamamoto T,Shiroshita K,Kitawaki J,Okada H

    更新日期:1989-03-01 00:00:00

  • "Madonna of the Pinks" and "Madonna Dell'Impannata": Raphael Sanzio (1483-1520).

    abstract:: ...

    journal_title:Journal of endocrinological investigation

    pub_type: 历史文章,杂志文章

    doi:10.1007/s40618-018-0896-y

    authors: Lazzeri D,Al-Mousawi A,Nicoli F

    更新日期:2018-12-01 00:00:00

  • Hypothalamic amenorrhea and cardiovascular hormones: changes of plasma calcitonin gene-related peptide and atrial natriuretic peptide levels.

    abstract::Typical modifications of cardiovascular activity and water and salt homeostasis throughout female reproductive life are well known. Differences in plasma levels of calcitonin gene-related peptide (CGRP) and atrial natriuretic peptide (ANP) have been observed in conditions characterized by different estrogenic levels, ...

    journal_title:Journal of endocrinological investigation

    pub_type: 杂志文章

    doi:10.1007/BF03347311

    authors: Bernardi F,Valentini A,Margutti A,Santuz M,Degli Uberti EC,Petraglia F,Genazzani AR

    更新日期:1998-04-01 00:00:00

  • Identification of genes in thyrocytes regulated by unfolded protein response by using disulfide bond reducing agent of dithiothreitol.

    abstract::Disulfide bonds are formed between the sulfhydryl groups in two cysteine residues of a protein. The formation of these bonds is necessary for the proper folding of a protein into its active three-dimensional form. In this study, the genes associated with disulfide bond formation of proteins from the rat thyroid cell l...

    journal_title:Journal of endocrinological investigation

    pub_type: 杂志文章

    doi:10.1007/BF03345141

    authors: Park S,Hwang I,Shong M,Kwon OY

    更新日期:2003-02-01 00:00:00

  • Plasma and urine cyclic nucleotide levels in patients with hyperthyroidism and hypothyroidism.

    abstract::Plasma levels and 24-h urinary excretion of cyclic AMP and cyclic GMP were measured in 18 patients with hyperthyroidism, 7 patients with hypothyroidism and 25 normal subjects. Mean plasma and urinary levels of both cyclic AMP and cyclic GMP were significantly positive correlations between the serum thyroid hormone lev...

    journal_title:Journal of endocrinological investigation

    pub_type: 杂志文章

    doi:10.1007/BF03350603

    authors: Peracchi M,Bamonti-Catena F,Lombardi L,Reschini E,Toschi V,Maiolo AT,Polli EE

    更新日期:1983-06-01 00:00:00

  • The combined effect of adiposity, fat distribution and age on cardiovascular risk factors and motor disability in a cohort of obese women (aged 18-83).

    abstract::Obesity is associated with a number of serious diseases and with a degree of motor disability, but the extent of the risk and functional derangement within the obese population is not yet completely defined. The study aims to evaluate the combined effect of degree of adiposity, body fat distribution and age on selecte...

    journal_title:Journal of endocrinological investigation

    pub_type: 杂志文章

    doi:10.1007/BF03349195

    authors: Lafortuna CL,Agosti F,Proietti M,Adorni F,Sartorio A

    更新日期:2006-11-01 00:00:00

  • The inhibitory effect of glucose on growth hormone secretion is lost in obesity but not in hypertension.

    abstract::In obesity there is a clear reduction of both spontaneous and stimulated GH secretion. Furthermore, in obese patients the somatotrope responsiveness to provocative stimulation is selectively refractory to the inhibitory effect of glucose load. It has been hypothesized that hyperinsulinism of obese patients could play ...

    journal_title:Journal of endocrinological investigation

    pub_type: 杂志文章

    doi:10.1007/BF03346919

    authors: Limone P,Oleandri SE,Ajmone Catt P,Grottoli S,Frangioni C,Avogadri E,Perrin M,Valetto MR,Maccario M

    更新日期:1997-11-01 00:00:00

  • Prolactin decrease and shift to a normal-like isoform profile during treatment with quinagolide in a patient affected by an invasive prolactinoma.

    abstract::Prolactin (PRL) circulates as multiple molecular weight variants: glycosylated phosphorylated, deamidated and sulphated forms. The profiles of the forms, as determined by isoelectrofocusing (IEF), differ in physiological and pathological conditions. The case of a 72-year-old woman affected by an invasive prolactinoma ...

    journal_title:Journal of endocrinological investigation

    pub_type: 杂志文章

    doi:10.1007/BF03350303

    authors: Guido R,Valenti S,Foppiani L,De Martini D,Cossu M,Giusti M

    更新日期:1997-05-01 00:00:00

  • Comparison between buserelin and dexamethasone testing in the assessment of hirsutism.

    abstract::Many hirsute women may present a form of functional ovarian hyperandrogenism (FOH), since they show an exaggerated 17-hydroxyprogesterone (17-OHP) response to GnRH agonists administration. As the failure of dexamethasone to reduce testosterone levels may be indicative of an ovarian source of androgen secretion, we eva...

    journal_title:Journal of endocrinological investigation

    pub_type: 杂志文章

    doi:10.1007/BF03343965

    authors: Re T,Barbetta L,Dall'Asta C,Faglia G,Ambrosi B

    更新日期:2002-01-01 00:00:00

  • Somatostatin-related therapeutics in ophthalmology: a review.

    abstract::Somatostatin and its derivatives have been predominantly studied and succesfully used in endocrinological diseases. This article reviews the rationale of the use of somatostatin and its derivatives in ophthalmology based on current understanding of its action in the eye and summarizes previously published controlled s...

    journal_title:Journal of endocrinological investigation

    pub_type: 杂志文章,评审

    doi:

    authors: Missotten T,Baarsma GS,Kuijpers RW,van den Born LI,van der Loos T,Croxen R,Hofland LJ,van Hagen PM

    更新日期:2005-01-01 00:00:00

  • The modulation of glucocorticoid receptor content by 3-O-methyl-D-glucose transport in human mononuclear leukocyte in obesity.

    abstract::Glucocorticoid receptors (GR) and 3-O-methyl-D glucose (3-O-MG) transport were determined in mononuclear leukocytes (MNL) from 11 abdominal obese subjects, 10 pituitary-dependent Cushing's syndrome (Cushing's disease) and 10 healthy controls. Using a whole-cell competitive binding assay and 3H-dexamethasone as tracer,...

    journal_title:Journal of endocrinological investigation

    pub_type: 杂志文章

    doi:10.1007/BF03350794

    authors: Güven M,Hatemi H,Taşan E,Altuntaş Y,Ulutin T,Tezcan V,Kanigür-Sultuybek G

    更新日期:1998-11-01 00:00:00

  • Indexes of abdominal adiposity in patients with type 2 diabetes.

    abstract:OBJECTIVE:To assess the relationship of waist circumference and weight/height ratio with height, and their association with components of the metabolic syndrome, in Type 2 diabetic patients. DESIGN:multicenter cross-sectional survey on a cohort enrolled in a prospective observational study. SUBJECTS:13,232 patients (...

    journal_title:Journal of endocrinological investigation

    pub_type: 杂志文章,多中心研究

    doi:10.1007/BF03347475

    authors: Mannucci E,Alegiani SS,Monami M,Sarli E,Avogaro A,DAI (Diabetes and Informatics) Study Group.

    更新日期:2004-06-01 00:00:00

  • Cushing's syndrome patient who exhibited congestive heart failure.

    abstract::Cushing's Syndrome (CS) may sometimes lead to dilated cardiomyopathy, even though this condition can be partially or completely reversed after treatment. In this article we report the case of a 28-yr-old woman with CS secondary to adrenal adenoma who exhibited congestive heart failure as an initial symptom. Two weeks ...

    journal_title:Journal of endocrinological investigation

    pub_type: 杂志文章

    doi:10.1007/BF03346339

    authors: Petramala L,Battisti P,Lauri G,Palleschi L,Cotesta D,Iorio M,De Toma G,Sciomer S,Letizia C

    更新日期:2007-06-01 00:00:00

  • Interrelationships between follicle stimulating hormone and the growth hormone--insulin-like growth factor--IGF-binding proteins axes in human granulosa cells in culture.

    abstract::As it has been hypothesized that IGF-binding proteins (IGFBPs) may have a role as autocrine/paracrine factors in regulating the local actions of the insulin-like growth factors (IGFs) in the ovary, we studied the production of the IGFBPs by human granulosa cells (GC) in culture and the role of IGFBP-3 in the modulatio...

    journal_title:Journal of endocrinological investigation

    pub_type: 杂志文章

    doi:10.1007/BF03347856

    authors: Barreca A,Artini PG,Cesarone A,Arvigo M,D'Ambrogio G,Genazzani AR,Giordano G,Minuto F

    更新日期:1996-01-01 00:00:00

  • Phosphaturic mesenchymal tumors: what an endocrinologist should know.

    abstract::Tumor-induced osteomalacia (TIO), also known as "oncogenic osteomalacia", is a rare cause of osteomalacia. TIO often has an insidious onset characterized clinically by progressive muscle weakness and bone pain with fractures. The hallmark biochemical finding is a persistent low serum phosphorus concentration due to re...

    journal_title:Journal of endocrinological investigation

    pub_type: 杂志文章,评审

    doi:10.1007/s40618-018-0849-5

    authors: Boland JM,Tebben PJ,Folpe AL

    更新日期:2018-10-01 00:00:00