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https://www.readbyqxmd.com/read/28090719/diversity-oriented-synthesis-of-cyclic-azapeptides-by-a-3-macrocyclization-provides-high-affinity-cd36-modulating-peptidomimetics
#1
Jinqiang Zhang, Mukandila Mulumba, Huy Ong, William D Lubell
Macrocyclization has enabled the use of peptides in drug discovery creating a need for methods to synthesize diverse peptide macrocycles. Azapeptides have advanced to clinically used drugs, however, few cyclic azapeptides have been studied. A multiple component "A(3) -macrocyclization" strategy is described for the preparation of diverse cyclic azapeptides and is demonstrated by the synthesis of 15 growth hormone releasing hormone-6 (GHRP-6) analogs. Certain cyclic aza-GHRP-6 analogs exhibited unprecedented affinity for the CD36 receptor, and capacity to modulate Toll-like receptor agonist-induced overproduction of nitric oxide, and reduce pro-inflammatory cytokine and chemokine production in macrophages...
January 16, 2017: Angewandte Chemie
https://www.readbyqxmd.com/read/28076448/igf-1-induces-ghrh-neuronal-axon-elongation-during-early-postnatal-life-in-mice
#2
Lyvianne Decourtye, Erik Mire, Maud Clemessy, Victor Heurtier, Tatiana Ledent, Iain C Robinson, Patrice Mollard, Jacques Epelbaum, Michael J Meaney, Sonia Garel, Yves Le Bouc, Laurent Kappeler
Nutrition during the perinatal period programs body growth. Growth hormone (GH) secretion from the pituitary regulates body growth and is controlled by Growth Hormone Releasing Hormone (GHRH) neurons located in the arcuate nucleus of the hypothalamus. We observed that dietary restriction during the early postnatal period (i.e. lactation) in mice influences postnatal growth by permanently altering the development of the somatotropic axis in the pituitary gland. This alteration may be due to a lack of GHRH signaling during this critical developmental period...
2017: PloS One
https://www.readbyqxmd.com/read/28032599/growth-hormone-releasing-hormone-antagonist-inhibits-the-invasiveness-of-human-endometrial-cancer-cells-by-down-regulating-twist-and-n-cadherin-expression
#3
Hsien-Ming Wu, Hong-Yuan Huang, Andrew V Schally, Angel Chao, Hung-Hsueh Chou, Peter C K Leung, Hsin-Shih Wang
More than 25% of patients diagnosed with endometrial carcinoma have invasive primary cancer accompanied by metastases. Growth hormone-releasing hormone (GHRH) plays an important role in reproduction. Here, we examined the effect of a GHRH antagonist on the motility of endometrial cancer cells and the mechanisms of action of the antagonist in endometrial cancer. Western blotting and immunohistochemistry (IHC) were used to determine the expression of the GHRH receptor protein. The activity of Twist and N-cadherin was determined by Western blotting...
December 10, 2016: Oncotarget
https://www.readbyqxmd.com/read/27974186/classical-and-non-classical-causes-of-gh-deficiency-in-the-paediatric-age
#4
REVIEW
Natascia Di Iorgi, Giovanni Morana, Anna Elsa Maria Allegri, Flavia Napoli, Roberto Gastaldi, Annalisa Calcagno, Giuseppa Patti, Sandro Loche, Mohamad Maghnie
Growth hormone deficiency (GHD) may result from a failure of hypothalamic GHRH production or release, from congenital disorders of pituitary development, or from central nervous system insults including tumors, surgery, trauma, radiation or infiltration from inflammatory diseases. Idiopathic, isolated GHD is the most common sporadic form of hypopituitarism. GHD may also occur in combination with other pituitary hormone deficiencies, and is often referred to as hypopituitarism, combined pituitary hormone deficiency (CPHD), multiple pituitary hormone deficiency (MPHD) or panhypopituitarism...
December 2016: Best Practice & Research. Clinical Endocrinology & Metabolism
https://www.readbyqxmd.com/read/27932410/anthropometric-factors-have-significant-influence-on-the-outcome-of-the-ghrh-arginine-test-establishment-of-normative-data-for-an-automated-immunoassay-specifically-measuring-22%C3%A2-kda-human-growth-hormone
#5
Timo Deutschbein, Martin Bidlingmaier, Jochen Schopohl, Christian J Strasburger, Stephan Petersenn
CONTEXT: Adult growth hormone (GH) deficiency (GHD) is diagnosed by provocative testing of GH secretion. OBJECTIVE: To improve the diagnostic accuracy of GH-releasing hormone (GHRH) plus arginine (GARG) testing, we evaluated the influence of age, BMI and sex and established normative data for an automatic immunoassay specifically measuring 22 kDa human GH. DESIGN/SETTING: Prospective multicenter study. PARTICIPANTS: Eighty-seven patients with hypothalamic-pituitary disease and 200 healthy controls...
March 2017: European Journal of Endocrinology
https://www.readbyqxmd.com/read/27930339/growth-hormone-releasing-hormone-receptor-antagonists-inhibit-human-gastric-cancer-through-downregulation-of-pak1-stat3-nf-%C3%AE%C2%BAb-signaling
#6
Jinfeng Gan, Xiurong Ke, Jiali Jiang, Hongmei Dong, Zhimeng Yao, Yusheng Lin, Wan Lin, Xiao Wu, Shumei Yan, Yixuan Zhuang, Wai Kit Chu, Renzhi Cai, Xianyang Zhang, Herman S Cheung, Norman L Block, Chi Pui Pang, Andrew V Schally, Hao Zhang
Gastric cancer (GC) ranks as the fourth most frequent in incidence and second in mortality among all cancers worldwide. The development of effective treatment approaches is an urgent requirement. Growth hormone-releasing hormone (GHRH) and GHRH receptor (GHRH-R) have been found to be present in a variety of tumoral tissues and cell lines. Therefore the inhibition of GHRH-R was proposed as a promising approach for the treatment of these cancers. However, little is known about GHRH-R and the relevant therapy in human GC...
December 20, 2016: Proceedings of the National Academy of Sciences of the United States of America
https://www.readbyqxmd.com/read/27911838/antagonists-of-growth-hormone-releasing-hormone-receptor-induce-apoptosis-specifically-in-retinoblastoma-cells
#7
Wai Kit Chu, Ka Sin Law, Sun On Chan, Jason Cheuk Sing Yam, Li Jia Chen, Hao Zhang, Herman S Cheung, Norman L Block, Andrew V Schally, Chi Pui Pang
Retinoblastoma (RB) is the most common intraocular cancer in children worldwide. Current treatments mainly involve combinations of chemotherapies, cryotherapies, and laser-based therapies. Severe or late-stage disease may require enucleation or lead to fatality. Recently, RB has been shown to arise from cone precursor cells, which have high MDM2 levels to suppress p53-mediated apoptosis. This finding leads to the hypothesis that restoring apoptosis mechanisms in RBs could specifically kill the cancer cells without affecting other retinal cells...
December 13, 2016: Proceedings of the National Academy of Sciences of the United States of America
https://www.readbyqxmd.com/read/27871293/genetic-and-epigenetic-alterations-in-the-gnas-locus-and-clinical-consequences-in-pseudohypoparathyroidism-italian-common-healthcare-pathways-adoption
#8
L de Sanctis, F Giachero, G Mantovani, G Weber, M Salerno, G I Baroncelli, M F Elli, P Matarazzo, M Wasniewska, L Mazzanti, G Scirè, D Tessaris
BACKGROUND: Genetic and epigenetic alterations in the GNAS locus are responsible for the Gsα protein dysfunctions causing Pseudohypoparathyroidism (PHP) type Ia/c and Ib, respectively. For these heterogeneous diseases characterized by multiple hormone resistances and Albright's Hereditary Osteodystrophy (AHO) the current classification results inadequate because of the clinical overlap between molecular subtypes and a standard clinical approach is still missing. In the present paper several members of the Study Group Endocrine diseases due to altered function of Gsα protein of the Italian Society of Pediatric Endocrinology and Diabetology (ISPED) have reviewed and updated the clinical-molecular data of the largest case series of (epi)/genetically characterized AHO/PHP patients; they then produced a common healthcare pathway for patients with these disorders...
November 21, 2016: Italian Journal of Pediatrics
https://www.readbyqxmd.com/read/27853416/neuropeptide-control-of-feeding-behavior-in-birds-and-its-difference-with-mammals
#9
REVIEW
Tetsuya Tachibana, Kazuyoshi Tsutsui
Feeding is an essential behavior for animals to sustain their lives. Over the past several decades, many neuropeptides that regulate feeding behavior have been identified in vertebrates. These neuropeptides are called "feeding regulatory neuropeptides." There have been numerous studies on the role of feeding regulatory neuropeptides in vertebrates including birds. Some feeding regulatory neuropeptides show different effects on feeding behavior between birds and other vertebrates, particularly mammals. The difference is marked with orexigenic neuropeptides...
2016: Frontiers in Neuroscience
https://www.readbyqxmd.com/read/27816751/growth-hormone-releasing-hormone-induced-transactivation-of-epidermal-growth-factor-receptor-in-human-triple-negative-breast-cancer-cells
#10
Eva Vacas, Laura Muñoz-Moreno, Pedro L Valenzuela, Juan C Prieto, Andrew V Schally, María J Carmena, Ana M Bajo
Triple-negative breast cancer (TNBC) is a subset of breast cancers which is negative for expression of estrogen and progesterone receptors and human epidermal growth factor receptor-2 (HER2). Chemotherapy is currently the only form of treatment for women with TNBC. Growth hormone-releasing hormone (GHRH) and epidermal growth factor (EGF) are autocrine/paracrine growth factors in breast cancer and a substantial proportion of TNBC expresses receptors for GHRH and EGF. The aim of this study was to evaluate the interrelationship between both these signaling pathways in MDA-MB-468 human TNBC cells...
December 2016: Peptides
https://www.readbyqxmd.com/read/27777568/growth-hormone-releasing-hormone-in-diabetes
#11
Leonid E Fridlyand, Natalia A Tamarina, Andrew V Schally, Louis H Philipson
Growth hormone-releasing hormone (GHRH) is produced by the hypothalamus and stimulates growth hormone synthesis and release in the anterior pituitary gland. In addition, GHRH is an important regulator of cellular functions in many cells and organs. Expression of GHRH G-Protein Coupled Receptor (GHRHR) has been demonstrated in different peripheral tissues and cell types, including pancreatic islets. Among the peripheral activities, recent studies demonstrate a novel ability of GHRH analogs to increase and preserve insulin secretion by beta-cells in isolated pancreatic islets, which makes them potentially useful for diabetes treatment...
2016: Frontiers in Endocrinology
https://www.readbyqxmd.com/read/27774107/growth-hormone-releasing-hormone-and-its-analogues-significance-for-mscs-mediated-angiogenesis
#12
Xiangyang Xia, Quanwei Tao, Qunchao Ma, Huiqiang Chen, Jian'an Wang, Hong Yu
Mesenchymal stromal cells (MSCs) are promising candidates for regenerative medicine because of their multipotency, immune-privilege, and paracrine properties including the potential to promote angiogenesis. Accumulating evidence suggests that the inherent properties of cytoprotection and tissue repair by native MSCs can be enhanced by various preconditioning stimuli implemented prior to cell transplantation. Growth hormone-releasing hormone (GHRH), a stimulator in extrahypothalamus systems including tumors, has attracted great attentions in recent years because GHRH and its agonists could promote angiogenesis in various tissues...
2016: Stem Cells International
https://www.readbyqxmd.com/read/27746436/metastatic-pancreatic-neuroendocrine-tumor-that-progressed-to-ectopic-adrenocorticotropic-hormone-acth-syndrome-with-growth-hormone-releasing-hormone-ghrh-production
#13
Rie Tadokoro, Shotaro Sato, Fumiko Otsuka, Makoto Ueno, Shinichi Ohkawa, Hideki Katakami, Matsuo Taniyama, Shoichiro Nagasaka
The patient was a 61-year-old woman who had a well-differentiated pancreatic neuroendocrine tumor (PNET) with lymph node metastasis. After 15 months of octreotide treatment, glucose control deteriorated and pigmentation of the tongue and moon face developed, leading to the diagnosis of ectopic adrenocorticotropic hormone (ACTH) syndrome. An abnormal secretion of growth hormone (GH) was identified, and the plasma growth hormone-releasing hormone (GHRH) level was elevated. A tumor biopsy specimen positively immunostained for ACTH and GHRH...
2016: Internal Medicine
https://www.readbyqxmd.com/read/27743704/gigantism-x-linked-acrogigantism-and-gpr101-mutations
#14
REVIEW
Donato Iacovazzo, Márta Korbonits
X-linked acrogigantism (XLAG) is a recently identified condition of early-onset GH excess resulting from the germline or somatic duplication of the GPR101 gene on chromosome Xq26.3. Thirty patients have been formally reported so far. The disease affects mostly females, occurs usually sporadically, and is characterised by early onset and marked overgrowth. Most patients present with concomitant hyperprolactinaemia. Histopathology shows pituitary hyperplasia or pituitary adenoma with or without associated hyperplasia...
October 2016: Growth Hormone & IGF Research
https://www.readbyqxmd.com/read/27733224/management-of-adult-growth-hormone-deficiency-at-peking-union-medical-college-hospital-a-survey-among-physicians-%C3%A2
#15
Hong-Bo Yang, Meng-Qi Zhang, Hui Pan, Hui-Juan Zhu
<strong>Objective</strong> To evaluate physicians' attitude and knowledge about the management of adult growth hormone deficiency (AGHD) at Peking Union Medical College Hospital and impact factors associated with better decision-making.<strong>Methods</strong> A 21-question anonymous survey was distributed and collected at Peking Union Medical College Hospital, a major teaching hospital in Chinese Academy of Medical Sciences. Data of physicians' educational background, clinical training, patient workload per year and continuing medical education in AGHD were collected...
September 20, 2016: Chinese Medical Sciences Journal, Chung-kuo i Hsüeh K'o Hsüeh Tsa Chih
https://www.readbyqxmd.com/read/27730472/pituitary-growth-hormone-gh-secretion-is-partially-rescued-in-hiv-infected-patients-with-gh-deficiency-ghd-compared-to-hypopituitary-patients
#16
Chiara Diazzi, Giulia Brigante, Giulia Ferrannini, Anna Ansaloni, Lucia Zirilli, Maria Cristina De Santis, Stefano Zona, Giovanni Guaraldi, Vincenzo Rochira
Biochemical growth hormone deficiency is prevalent among human immunodeficiency virus-infected patients, but if this condition is clinically relevant remains challenging. The aim is to prospectively compare the growth hormone deficiency/insulin-like growth factor-1 status of 71 human immunodeficiency virus-infected patients with impaired growth hormone response to growth hormone releasing hormone + Arginine with that of 65 hypopituitary patients affected by a true growth hormone deficiency secondary to pituitary disease...
October 11, 2016: Endocrine
https://www.readbyqxmd.com/read/27701044/corticotropin-releasing-hormone-induces-depression-like-changes-of-sleep-electroencephalogram-in-healthy-women
#17
P Schüssler, M Kluge, W Gamringer, T C Wetter, A Yassouridis, M Uhr, R Rupprecht, A Steiger
We reported previously that repetitive intravenous injections of corticotropin-releasing hormone (CRH) around sleep onset prompt depression-like changes in certain sleep and endocrine activity parameters (e.g. decrease of slow-wave sleep during the second half of the night, blunted growth hormone peak, elevated cortisol concentration during the first half of the night). Furthermore a sexual dimorphism of the sleep-endocrine effects of the hormones growth hormone-releasing hormone and ghrelin was observed. In the present placebo-controlled study we investigated the effect of pulsatile administration of 4×50μg CRH on sleep electroencephalogram (EEG) and nocturnal cortisol and GH concentration in young healthy women...
December 2016: Psychoneuroendocrinology
https://www.readbyqxmd.com/read/27639323/corticotropin-releasing-hormone-crh-immunoreactive-ir-axon-varicosities-target-a-subset-of-growth-hormone-releasing-hormone-ghrh-ir-neurons-in-the-human-hypothalamus
#18
Michael Peroski, Nikoletta Proudan, George Grignol, Istvan Merchenthaler, Bertalan Dudas
It is a general consensus that stress is one of the major factors that suppresses growth. Previous studies revealed that the catecholaminergic and neuropeptide Y (NPY) systems, involved in the activation of stress-related neuronal circuits, influence growth hormone (GH)-release via modulating growth hormone-releasing hormone (GHRH) secretion. Indeed, catecholaminergic and NPY-immunoreactive (IR) axon varicosities abut on the surface of the GHRH neurons forming contacts. These juxtapositions appear to be real synapses and may represent the morphological substrate of the impact of stress on growth...
December 2016: Journal of Chemical Neuroanatomy
https://www.readbyqxmd.com/read/27631552/foxo1-is-required-for-normal-somatotrope-differentiation
#19
Jyoti Kapali, Brock E Kabat, Kelly L Schmidt, Caitlin E Stallings, Mason Tippy, Deborah O Jung, Brian S Edwards, Leah B Nantie, Lori T Raeztman, Amy M Navratil, Buffy S Ellsworth
The etiology for half of congenital hypopituitarism cases is unknown. Our long-term goal is to expand the molecular diagnoses for congenital hypopituitarism by identifying genes that contribute to this condition. We have previously shown that the forkhead box transcription factor, FOXO1, is present in approximately half of somatotropes at embryonic day (e) 18.5, suggesting it may have a role in somatotrope differentiation or function. To elucidate the role of FOXO1 in somatotrope differentiation and function, Foxo1 was conditionally deleted from the anterior pituitary (Foxo1(Δpit))...
November 2016: Endocrinology
https://www.readbyqxmd.com/read/27621108/mild-pituitary-phenotype-in-3-and-12-month-old-aip-deficient-male-mice
#20
Anne-Lise Lecoq, Philippe Zizzari, Mirella Hage, Lyvianne Decourtye, Clovis Adam, Say Viengchareun, Johannes D Veldhuis, Valérie Geoffroy, Marc Lombès, Virginie Tolle, Anne Guillou, Auli Karhu, Laurent Kappeler, Philippe Chanson, Peter Kamenický
Germline mutations in the aryl hydrocarbon receptor-interacting protein (AIP) gene predispose humans to pituitary adenomas, particularly of the somatotroph lineage. Mice with global heterozygous inactivation of Aip (Aip(+/-)) also develop pituitary adenomas but differ from AIP-mutated patients by the high penetrance of pituitary disease. The endocrine phenotype of these mice is unknown. The aim of this study was to determine the endocrine phenotype of Aip(+/-) mice by assessing the somatic growth, ultradian pattern of GH secretion and IGF1 concentrations of longitudinally followed male mice at 3 and 12 months of age...
October 2016: Journal of Endocrinology
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