The present invention is directed to the identification of a biomarker specifically located in the plasma membrane of pancreatic beta cells. It was selected by a Systems Biology approach on Massively Parallel Signal Sequencing datasets obtained in human islets and Affymetrix microarray datasets on human islets, purified rat primary beta and non beta cells and insulinoma cells. Based on a set of specific features the biomarker is a unique candidate for imaging and targeting strategies to study the pancreatic beta cell mass in health and disease (T1 D, T2D, pancreatic cancers, obesity, islet transplantation, beta cell regeneration). The five specific features of the selected biomarkers are: 1) Preferentially expressed in pancreatic islets as compared to surrounding tissues; 2) Higher expression in pancreatic beta cells than in pancreatic alpha cells or than in other islet non-beta cells; 3) Expression levels in pancreatic beta cells are higher or comparable to glucokinase which is an enzyme specifically expressed in the pancreatic beta cell; 4) Located in the membrane and as such targetable with antibodies, peptides or small molecules which allows imaging, targeting and immunohistochemistry; and 5) Expression is not induced during the process of inflammation of the beta cell mass and the protein is not enriched in T-cells and dendritic cells or in other cells participating in the inflammation process.

Eizirik; Decio L.

Flamez; Daisy

Salmon; Isabelle

Berton; Alix

Roland; Isabelle

Marechal; Daniel

Beckers; Marie-Claire

Hood; Leroy

Goodman; Nathan

Kutlu; Burak

Universite Libre de Bruxelles

Plasma membrane biomarkers preferentially expressed in pancreatic beta cells useful in imaging or targeting beta cells

Compounds of structural formula I as herein defined are disclosed as useful in a method for modulating the androgen receptor in a tissue selective manner in a patient in need of such modulation, as well as in a method of activating the function of the androgen receptor in a patient, and in particular the method wherein the function of the androgen receptor is blocked in the prostate of a male patient or in the uterus of a female patient and activated in bone and/or muscle tissue. These compounds are useful in the treatment of conditions caused by androgen deficiency or which can be ameliorated by androgen administration, including osteoporesis, periodontal disease, bone fracture, bone damage following bone reconstructive surgery, sarcopenia, frailty, aging skin, male hypogonadism, female sexual dysfunction, post-menopausal symptoms in women, atherosclerosis, hypercholesterolemia, hyperlipidemia, obesity, aplastic anemia and other hematopoietic disorders, pancreatic cancer, renal cancer, prostate cancer, arthritis and joint repair, alone or in combination with other active agents.

Merck &amp; Co., Inc.

17-hydroxy-4-aza-androstan-3-ones as androgen receptor modulators

An extract of Chinese blackberry (Rubus suavissimus) has been found to inhibit angiogenesis, and two active fractions isolated. Gallic acid was shown to be one of the active anti-angiogenic compounds by an in vitro human angiogenesis model. Aqueous extracts from other plants either known or found to have gallic acid were also found to have anti-angiogenic activity. Various derivatives of gallic acid were found to inhibit angiogenesis. The extract from Chinese blackberry also slowed the growth of a pancreatic tumor and of corneal neovascularization in rats. Extracts from pomegranate were shown to inhibit angiogenesis in fat tissue. Extracts from Rubus spp, and other plants with gallic acid, and gallic acid and its derivatives will be useful for treating various diseases associated with neovascularization, including diabetic retinopathy, psoriasis, tumors, obesity, cancer, rheumatoid arthritis, etc.

Board of Supervisors of Louisiana State University And Agricultural and Mechanical College

pancreatic neoplasms/fetma

Plasma membrane biomarkers preferentially expressed in pancreatic beta cells useful in imaging or targeting beta cells

17-hydroxy-4-aza-androstan-3-ones as androgen receptor modulators

Anti-angiogenic extracts from pomegranate

Angiogenic agents from plant extracts, gallic acid, and derivatives

Den mest kompletta databasen med medicinska örter som stöds av vetenskapen