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  1. Article ; Online: In silico development of new PET radiopharmaceuticals from mTOR inhibitors.

    Ferino-Pérez, Anthuan / Vélayoudom, Fritz-Line / Belia, Lyonel / Glaude, Eddy-Laurent / Gaspard, Sarra / Jáuregui-Haza, Ulises J

    Journal of molecular graphics & modelling

    2021  Volume 111, Page(s) 108057

    Abstract: Rapamycin (or sirolimus) is a macrolide that has shown to be useful as an immunosuppressant and that was studied in metabolic, neurological, or genetic disorders. Rapamycin is a specific natural inhibitor of the mechanistic target of rapamycin (mTOR) ... ...

    Abstract Rapamycin (or sirolimus) is a macrolide that has shown to be useful as an immunosuppressant and that was studied in metabolic, neurological, or genetic disorders. Rapamycin is a specific natural inhibitor of the mechanistic target of rapamycin (mTOR) that is a kinase protein playing a pivotal role in cell growth and proliferation by activation of several metabolic processes. This work aimed to evaluate the utility of several compounds obtained from rapamycin and its semi-synthetic analogs everolimus and temsirolimus as possible radiopharmaceuticals oriented to this protein. Density Functional Theory calculations of these molecules were made and further analysis of the dual descriptor, charges populations, and of the electrostatic potential surfaces were performed. Molecular docking simulations were used to evaluate the interactions of the rapamycin with the studied candidates. They allowed us to propose two strategies for the synthesis of novel compounds based on electrophilic reactions. Molecular docking results also helped us to eliminate molecules that did not interact correctly with the target. Finally, we found for the first time, that the novel compounds synthesized through the electrophilic addition reaction that employed
    MeSH term(s) MTOR Inhibitors ; Molecular Docking Simulation ; Positron-Emission Tomography ; Protein Kinase Inhibitors/pharmacology ; Radiopharmaceuticals ; TOR Serine-Threonine Kinases
    Chemical Substances MTOR Inhibitors ; Protein Kinase Inhibitors ; Radiopharmaceuticals ; TOR Serine-Threonine Kinases (EC 2.7.11.1)
    Language English
    Publishing date 2021-11-24
    Publishing country United States
    Document type Journal Article
    ZDB-ID 1396450-1
    ISSN 1873-4243 ; 1093-3263
    ISSN (online) 1873-4243
    ISSN 1093-3263
    DOI 10.1016/j.jmgm.2021.108057
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  2. Article ; Online: Etiopathogeny of Primary Adrenal Hypercortisolism.

    Vélayoudom-Céphise, Fritz-Line / Haissaguerre, Magali / Tabarin, Antoine

    Frontiers of hormone research

    2016  Volume 46, Page(s) 39–53

    Abstract: Primary adrenal hypercortisolism is mainly due to cortisol-producing adrenocortical adenomas, bilateral micronodular or macronodular disease, and adrenal carcinomas. Important advances in the pathophysiology of primary adrenal hypercortisolism have been ... ...

    Abstract Primary adrenal hypercortisolism is mainly due to cortisol-producing adrenocortical adenomas, bilateral micronodular or macronodular disease, and adrenal carcinomas. Important advances in the pathophysiology of primary adrenal hypercortisolism have been made in the last few years, partly through the use of new molecular biology tools. Most adrenal abnormalities leading to increased cortisol production involve somatic or germinal mutations of genes encoding elements of the cyclic AMP/protein kinase A signaling pathway, as shown in adrenal adenomas in 2014. One peculiar condition is primary macronodular adrenal hyperplasia (PMAH), which has given rise to new pathophysiological concepts such as regulation of cortisol secretion by illegitimate ligands through aberrant expression of G protein-coupled transmembrane receptors in adrenal nodules and stimulation of cortisol production by local adrenocorticotropic hormone production through autocrine/paracrine mechanisms. These findings provide a basis for the development of targeted therapies as an alternative to surgery. The recent identification of germinal mutations of ARMC5 in PMAH raises the possibility that this is much more frequently an inherited disease than previously suspected. It also offers the possibility of earlier diagnosis of PMAH by genetic screening and, hopefully, of earlier intervention to prevent the onset of hypercortisolism and its complications. The pathophysiology of Cushing's syndrome associated with a subset of adrenal adenomas, including subclinical cortisol-secreting incidentalomas and adrenal carcinomas, remains to be determined.
    MeSH term(s) Adrenal Gland Neoplasms/complications ; Cushing Syndrome/etiology ; Cushing Syndrome/genetics ; Humans
    Language English
    Publishing date 2016
    Publishing country Switzerland
    Document type Journal Article ; Review
    ISSN 1662-3762 ; 0301-3073
    ISSN (online) 1662-3762
    ISSN 0301-3073
    DOI 10.1159/000443863
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  3. Article: Endocrine vigilance in COVID-19.

    Velayoudom, Fritz-Line / Alwis Wijewickrama, Piyumi Sachindra / Ranathunga, H Ishara / Somasundaram, Noel

    JPMA. The Journal of the Pakistan Medical Association

    2020  Volume 70Suppl 3, Issue 5, Page(s) S83–S86

    Abstract: Severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) is a novel coronavirus responsible for a pandemic that emerged in December 2019. Heterogeneous clinical forms are described from asymptomatic to severe hypoxaemic acute respiratory syndrome ... ...

    Abstract Severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) is a novel coronavirus responsible for a pandemic that emerged in December 2019. Heterogeneous clinical forms are described from asymptomatic to severe hypoxaemic acute respiratory syndrome with multisystem organ failure. The impact of this coronavirus disease 2019 on the endocrine glands remains unknown. However, the results of previous studies on viruses from the same family allow us to write proposals for patients followed for chronic endocrine diseases. Currently, if these subjects are infected with SARS-CoV-2, they must not stop their treatment. In some cases, hormone replacement doses have to be increased. In case of worsening clinical signs, hormonal biological monitoring must be done. This article will be helpful for improving the management of chronic endocrine diseases that could affect thyroid, adrenals, gonads and pituitary gland functions. Proposals could be applied in COVID-19 infected subjects or in those who have been in contact with COVID-19 infected people.
    MeSH term(s) Betacoronavirus ; COVID-19 ; Chronic Disease ; Coronavirus Infections/complications ; Endocrine System Diseases/complications ; Endocrine System Diseases/therapy ; Humans ; Pandemics ; Pneumonia, Viral/complications ; Risk Factors ; SARS-CoV-2
    Keywords covid19
    Language English
    Publishing date 2020-06-09
    Publishing country Pakistan
    Document type Journal Article
    ZDB-ID 603873-6
    ISSN 0030-9982
    ISSN 0030-9982
    DOI 10.5455/JPMA.16
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  4. Article ; Online: What is the best biological parameter to predict erectile dysfunction in men aged >55 years with type 2 diabetes?

    Raharinavalona, Sitraka A / Chevalier, Nicolas / Gruel, Claude / N'toutoum, André-Christian / Vélayoudom Céphise, Fritz-Line

    Journal of diabetes investigation

    2019  Volume 11, Issue 1, Page(s) 170–173

    Abstract: To date, there is no evidence regarding the best biological marker to predict erectile dysfunction (ED) in men aged >55 years with type 2 diabetes. This prospective study included data from men aged >55 years with type 2 diabetes. ED was assessed by the ... ...

    Abstract To date, there is no evidence regarding the best biological marker to predict erectile dysfunction (ED) in men aged >55 years with type 2 diabetes. This prospective study included data from men aged >55 years with type 2 diabetes. ED was assessed by the International Index of Erectile Function 15-item survey. Total testosterone (TT) levels and bioavailable testosterone were measured; the free testosterone index was calculated. Data from 155 men (aged 64 ± 7 years) were explored. The prevalence of ED and testosterone deficiency was 78.7% and 34.8%, respectively. After univariate analysis, TT and bioavailable testosterone were associated with ED (P = 0.01). After multivariate analysis, and adjustment for age, body mass index, tobacco, alcohol, duration of diabetes, TT, bioavailable testosterone, vitamin D and high-sensitivity C-reactive protein, we found that only high-sensitivity C-reactive protein was significantly predictive of ED. TT could predict ED, but it lacks specificity. We found a potential role of high-sensitivity C-reactive protein as a predictive marker of ED in this targeted population.
    MeSH term(s) Biomarkers/analysis ; Body Mass Index ; Case-Control Studies ; Cross-Sectional Studies ; Erectile Dysfunction/blood ; Erectile Dysfunction/diagnosis ; Female ; Follow-Up Studies ; Humans ; Male ; Middle Aged ; Obesity/physiopathology ; Prognosis ; Prospective Studies ; Surveys and Questionnaires ; Testosterone/blood
    Chemical Substances Biomarkers ; Testosterone (3XMK78S47O)
    Language English
    Publishing date 2019-07-08
    Publishing country Japan
    Document type Journal Article
    ZDB-ID 2625840-7
    ISSN 2040-1124 ; 2040-1116
    ISSN (online) 2040-1124
    ISSN 2040-1116
    DOI 10.1111/jdi.13089
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  5. Article ; Online: Primary hyperparathyroidism and vitamin D deficiency.

    Vélayoudom-Céphise, Fritz-Line / Wémeau, Jean-Louis

    Annales d'endocrinologie

    2015  Volume 76, Issue 2, Page(s) 153–162

    Abstract: Primary hyperparathyroidism (PHPT) and vitamin D (VD) deficiency are frequent conditions due to the widespread application of assays for calcium and VD. PHPT presentation is dominated by diversity in its expression and the current predominance of ... ...

    Abstract Primary hyperparathyroidism (PHPT) and vitamin D (VD) deficiency are frequent conditions due to the widespread application of assays for calcium and VD. PHPT presentation is dominated by diversity in its expression and the current predominance of asymptomatic forms. VD, which plays a major role in calcium and phosphate homeostasis, is also involved in many physiological processes in this disease, such as lipid and glucose metabolism, and in the signalling pathways and functioning of many cell types. The bone and cardiometabolic complications described in PHPT are exacerbated by vitamin D deficiency, the prevalence of which varies according to many parameters (environment, skin pigmentation, associated chronic diseases, liver and kidney function, assay kit used, etc.). In response to this observation, experts in field from medical societies validated the indication for systematic assay of VD occurring with PHPT and the need for replacement in case of deficiency. Several epidemiological studies have confirmed that replacement with natural vitamin D is well tolerated and safe in subjects with PHPT and VD deficiency. This supplementation reduces hyperparathormonemia, does not have symptomatic effects on calciuria, and especially improves the bone and functional condition of patients.
    MeSH term(s) Bone Diseases/etiology ; Humans ; Hyperparathyroidism, Primary/epidemiology ; Hyperparathyroidism, Primary/etiology ; Hyperparathyroidism, Primary/genetics ; Hyperparathyroidism, Primary/physiopathology ; Vitamin D/metabolism ; Vitamin D/therapeutic use ; Vitamin D Deficiency/complications ; Vitamin D Deficiency/genetics ; Vitamin D Deficiency/physiopathology ; Vitamins/therapeutic use
    Chemical Substances Vitamins ; Vitamin D (1406-16-2)
    Language English
    Publishing date 2015-05
    Publishing country France
    Document type Journal Article ; Review
    ZDB-ID 299-9
    ISSN 2213-3941 ; 0003-4266
    ISSN (online) 2213-3941
    ISSN 0003-4266
    DOI 10.1016/j.ando.2015.03.022
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  6. Article ; Online: Triglycerides as a Metabolic Target in Afrocaribbean Infertile Women with Polycystic Ovary Syndrome.

    Brouzeng, Charlotte / Bachelot, Anne / Moriniere, Catherine / Vaillant, Jean / Joguet, Guillaume / Velayoudom, Fritz-Line

    Metabolic syndrome and related disorders

    2019  Volume 17, Issue 10, Page(s) 500–504

    Abstract: Background: ...

    Abstract Background:
    MeSH term(s) Adult ; African Continental Ancestry Group ; Caribbean Region/epidemiology ; Case-Control Studies ; Female ; Humans ; Hypertriglyceridemia/blood ; Hypertriglyceridemia/complications ; Hypertriglyceridemia/ethnology ; Hypertriglyceridemia/therapy ; Infertility, Female/blood ; Infertility, Female/ethnology ; Infertility, Female/therapy ; Obesity/blood ; Obesity/complications ; Obesity/ethnology ; Obesity/therapy ; Patient Care Planning ; Polycystic Ovary Syndrome/blood ; Polycystic Ovary Syndrome/ethnology ; Polycystic Ovary Syndrome/therapy ; Prevalence ; Retrospective Studies ; Triglycerides/blood ; Young Adult
    Chemical Substances Triglycerides
    Language English
    Publishing date 2019-10-08
    Publishing country United States
    Document type Journal Article
    ZDB-ID 2151220-6
    ISSN 1557-8518 ; 1540-4196
    ISSN (online) 1557-8518
    ISSN 1540-4196
    DOI 10.1089/met.2019.0041
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  7. Article ; Online: Graves' disease: Introduction, epidemiology, endogenous and environmental pathogenic factors.

    Wémeau, Jean-Louis / Klein, Marc / Sadoul, Jean-Louis / Briet, Claire / Vélayoudom-Céphise, Fritz-Line

    Annales d'endocrinologie

    2018  Volume 79, Issue 6, Page(s) 599–607

    Abstract: Graves' disease is the most frequent cause of hyperthyroidism. Many questions remain about the choice of diagnostic evaluations and treatment strategy according to clinical context (age, gender, pregnancy, etc.) and about the best management of the main ... ...

    Abstract Graves' disease is the most frequent cause of hyperthyroidism. Many questions remain about the choice of diagnostic evaluations and treatment strategy according to clinical context (age, gender, pregnancy, etc.) and about the best management of the main extrathyroidal complication that is Graves orbitopathy. The exact pathogenic mechanisms are not fully clear. They associate genetic factors, interactions between endogenous and environmental factors, and immune system dysregulation. Graves' orbitopathy is one of the consequences of this partial understanding. Iatrogenic Graves' disease induced by the new targeted therapies are described and could help to better understand the molecular pathways involved in the disease and to develop new therapeutic approaches.
    MeSH term(s) Age of Onset ; Disease Susceptibility/complications ; Disease Susceptibility/epidemiology ; Disease Susceptibility/immunology ; Drug-Related Side Effects and Adverse Reactions/complications ; Drug-Related Side Effects and Adverse Reactions/epidemiology ; Environment ; Gene-Environment Interaction ; Genetic Predisposition to Disease ; Graves Disease/diagnosis ; Graves Disease/epidemiology ; Graves Disease/etiology ; Humans ; Iatrogenic Disease/epidemiology ; Immune System Phenomena/physiology ; Infection/complications ; Infection/epidemiology
    Language English
    Publishing date 2018-09-11
    Publishing country France
    Document type Journal Article ; Review
    ZDB-ID 299-9
    ISSN 2213-3941 ; 0003-4266
    ISSN (online) 2213-3941
    ISSN 0003-4266
    DOI 10.1016/j.ando.2018.09.002
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  8. Article ; Online: A Hungry Bone Syndrome Predicted by 18F-Fluorocholine PET/CT.

    Paepegaey, Anne-Cécile / Velayoudom, Fritz-Line / Housni, Selma / Gauthé, Mathieu / Groussin, Lionel

    Clinical nuclear medicine

    2019  Volume 44, Issue 11, Page(s) 903–904

    Abstract: Predicting hungry bone syndrome (HBS) after surgical cure of primary hyperparathyroidism (PHPT) can be challenging. A 57-year-old man diagnosed with PHPT was assessed preoperatively by F-fluorocholine PET/CT. An intense and diffuse tracer uptake of the ... ...

    Abstract Predicting hungry bone syndrome (HBS) after surgical cure of primary hyperparathyroidism (PHPT) can be challenging. A 57-year-old man diagnosed with PHPT was assessed preoperatively by F-fluorocholine PET/CT. An intense and diffuse tracer uptake of the axial and peripheral skeleton was visualized, in addition to a pathologic uptake suggestive of hyperfunctioning parathyroid gland. After the removal of a parathyroid adenoma, a severe and prolonged HBS requiring high doses of calcium and active metabolites of vitamin D was observed. This observation suggests that intense and diffuse bone uptake on F-fluorocholine PET/CT could be a predictive factor for HBS in patients with PHPT.
    MeSH term(s) Biological Transport ; Bone and Bones/diagnostic imaging ; Bone and Bones/metabolism ; Choline/analogs & derivatives ; Humans ; Male ; Metabolic Diseases/diagnostic imaging ; Metabolic Diseases/metabolism ; Middle Aged ; Parathyroid Neoplasms/diagnostic imaging ; Parathyroid Neoplasms/metabolism ; Parathyroid Neoplasms/surgery ; Positron Emission Tomography Computed Tomography
    Chemical Substances fluorocholine (6029HGL0QP) ; Choline (N91BDP6H0X)
    Language English
    Publishing date 2019-07-05
    Publishing country United States
    Document type Case Reports ; Journal Article
    ZDB-ID 197628-x
    ISSN 1536-0229 ; 0363-9762
    ISSN (online) 1536-0229
    ISSN 0363-9762
    DOI 10.1097/RLU.0000000000002676
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  9. Article: Initiation of the Fixed Combination IDegLira in Patients with Type 2 Diabetes on Prior Injectable Therapy: Insights from the EASY French Real-World Study.

    Tramunt, Blandine / Disse, Emmanuel / Chevalier, Nicolas / Bordier, Lyse / Cazals, Laurent / Dupuy, Olivier / Marre, Michel / Matar, Odette / Meyer, Laurent / Noilhan, Chloé / Sanz, Caroline / Valensi, Paul / Velayoudom, Fritz-Line / Gautier, Jean-François / Gourdy, Pierre

    Diabetes therapy : research, treatment and education of diabetes and related disorders

    2022  Volume 13, Issue 11-12, Page(s) 1947–1963

    Abstract: Introduction: Combining basal insulin (BI) with glucagon-like peptide-1 receptor agonist (GLP-1RA) is recognized as a relevant option to optimize glucose control in type 2 diabetes (T2D). The EASY real-world study aimed to evaluate the modalities of ... ...

    Abstract Introduction: Combining basal insulin (BI) with glucagon-like peptide-1 receptor agonist (GLP-1RA) is recognized as a relevant option to optimize glucose control in type 2 diabetes (T2D). The EASY real-world study aimed to evaluate the modalities of initiation and the effectiveness of the insulin Degludec plus Liraglutide (IDegLira) fixed-ratio combination in the French health care system.
    Methods: A retrospective analysis included all patients with T2D and prior injectable therapy (GLP1-RA and/or insulin) who started treatment with IDegLira from September 2016 to December 2017 in 11 French diabetes centers. Baseline characteristics, reasons for IDegLira initiation, and modes of implementation were collected from the medical records. Changes in HbA
    Results: IDegLira was initiated in 629 patients previously treated with GLP-1RA alone (11.6%), insulin alone (31.5% including 16.5% with BI and 14.9% with multiple daily injections [MDI]) or a free combination of GLP-1RA and insulin (56.9% including 44.8% with BI and 12.1% with MDI), associated or not with oral agents. IDegLira starting dose (mean of 29 ± 11 dose steps) most often exceeded the recommended dose, and was significantly correlated with prior BI but not GLP-1RA dosage. At initiation, mean age, body mass index (BMI) and HbA
    Conclusions: While providing new information on the use of IDegLira in the French healthcare system, these data confirm the effectiveness of this fixed-ratio combination in the management of T2D.
    Language English
    Publishing date 2022-11-04
    Publishing country United States
    Document type Journal Article
    ZDB-ID 2566702-6
    ISSN 1869-6961 ; 1869-6953
    ISSN (online) 1869-6961
    ISSN 1869-6953
    DOI 10.1007/s13300-022-01327-8
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  10. Article: Glycaemic Variability and Hyperglycaemia as Prognostic Markers of Major Cardiovascular Events in Diabetic Patients Hospitalised in Cardiology Intensive Care Unit for Acute Heart Failure.

    Gerbaud, Edouard / Bouchard de La Poterie, Ambroise / Baudinet, Thomas / Montaudon, Michel / Beauvieux, Marie-Christine / Lemaître, Anne-Iris / Cetran, Laura / Seguy, Benjamin / Picard, François / Vélayoudom, Fritz-Line / Ouattara, Alexandre / Kabore, Rémi / Coste, Pierre / Domingues-Dos-Santos, Pierre / Catargi, Bogdan

    Journal of clinical medicine

    2022  Volume 11, Issue 6

    Abstract: 1) Background: Hyperglycaemia and hypoglycaemia are both emerging risk factors for cardiovascular disease. Nevertheless, the potential effect of glycaemic variability (GV) on mid-term major cardiovascular events (MACE) in diabetic patients presenting ... ...

    Abstract (1) Background: Hyperglycaemia and hypoglycaemia are both emerging risk factors for cardiovascular disease. Nevertheless, the potential effect of glycaemic variability (GV) on mid-term major cardiovascular events (MACE) in diabetic patients presenting with acute heart failure (AHF) remains unclear. This study investigates the prognostic value of GV in diabetic patients presenting with acute heart failure (AHF). (2) Methods: this was an observational study including consecutive patients with diabetes and AHF between January 2015 and November 2016. GV was calculated using standard deviation of glycaemia values during initial hospitalisation in the intensive cardiac care unit. MACE, including recurrent AHF, new-onset myocardial infarction, ischaemic stroke and cardiac death, were recorded. The predictive effects of GV on patient outcomes were analysed with respect to baseline characteristics and cardiac status. (3) Results: In total, 392 patients with diabetes and AHF were enrolled. During follow-up (median (interquartile range) 29 (6−51) months), MACE occurred in 227 patients (57.9%). In total, 92 patients died of cardiac causes (23.5%), 107 were hospitalised for heart failure (27.3%), 19 had new-onset myocardial infarction (4.8%) and 9 (2.3%) had an ischaemic stroke. Multivariable logistic regression analysis showed that GV > 50 mg/dL (2.70 mmol/L), age > 75 years, reduced left ventricular ejection fraction (LVEF < 30%) and female gender were independent predictors of MACE: hazard ratios (HR) of 3.16 (2.25−4.43; p < 0.001), 1.54 (1.14−2.08; p = 0.005), 1.47 (1.06−2.07; p = 0.02) and 1.43 (1.05−1.94; p = 0.03), respectively. (4) Conclusions: among other well-known factors of HF, a GV cut-off value of >50 mg/dL was the strongest independent predictive factor for mid-term MACE in patients with diabetes and AHF.
    Language English
    Publishing date 2022-03-11
    Publishing country Switzerland
    Document type Journal Article
    ZDB-ID 2662592-1
    ISSN 2077-0383
    ISSN 2077-0383
    DOI 10.3390/jcm11061549
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