Aquaporin-7 and glycerol permeability as novel obesity drug-target pathways

2006 ◽  
Vol 27 (7) ◽  
pp. 345-347 ◽  
Author(s):  
G FRUHBECK ◽  
V CATALAN ◽  
J GOMEZAMBROSI ◽  
A RODRIGUEZ
Keyword(s):  
Drug Target ◽  
Aquaporin 7 ◽  
Glycerol Permeability

scholarly journals Aquaporin-7: A Dynamic Aquaglyceroporin With Greater Water and Glycerol Permeability Than Its Bacterial Homolog GlpF

2020 ◽  
Vol 11 ◽  
Author(s):  
Fraser J. Moss ◽  
Paween Mahinthichaichan ◽  
David T. Lodowski ◽  
Thomas Kowatz ◽  
Emad Tajkhorshid ◽  
...  
Keyword(s):  
Aquaporin 7 ◽  
Bacterial Homolog ◽  
Glycerol Permeability

scholarly journals Progressive Adipocyte Hypertrophy in Aquaporin-7-deficient Mice

2005 ◽  
Vol 280 (16) ◽  
pp. 15493-15496 ◽  
Author(s):  
Mariko Hara-Chikuma ◽  
Eisei Sohara ◽  
Tatemitsu Rai ◽  
Masahito Ikawa ◽  
Masaru Okabe ◽  
...  
Keyword(s):  
Body Fat ◽  
Fat Mass ◽  
Body Fat Mass ◽  
Wild Type ◽  
Adipocyte Volume ◽  
Aquaporin 7 ◽  
Adipocyte Hypertrophy ◽  
Adipocyte Plasma Membranes ◽  
Deficient Mice ◽  
Glycerol Permeability

Aquaporin-7 (AQP7) is a water/glycerol transporting protein expressed in adipocyte plasma membranes. We report here remarkable age-dependent hypertrophy in adipocytes in AQP7-deficient mice. Wild type and AQP7 null mice had similar growth at 0–16 weeks as assessed by body weight; however, by 16 weeks AQP7 null mice had 3.7-fold increased body fat mass. Adipocytes from AQP7 null mice of age 16 weeks were greatly enlarged (diameter 118 μm) compared with wild type mice (39 μm). Adipocytes from AQP7 null mice also accumulated excess glycerol (251versus86 nmol/mg of protein) and triglycerides (3.4versus1.7 μmol/mg of protein). In contrast, at age 4 weeks, adipocyte volume and body fat mass were comparable in wild type and AQP7 null mice. To investigate the mechanism(s) responsible for the progressive adipocyte hypertrophy, glycerol permeability and fat metabolism were studied in adipocytes isolated from the younger mice. Plasma membrane glycerol permeability measured by [14C]glycerol uptake was 3-fold reduced in AQP7-deficient adipocytes. However, adipocyte lipolysis, measured by free fatty acid release and hormone-sensitive lipase activity, and lipogenesis, measured by [14C]glucose incorporation into triglycerides, were not affected by AQP7 deletion. These data suggest that adipocyte hypertrophy in AQP7 deficiency results from defective glycerol exit and consequent accumulation of glycerol and triglycerides. Increasing AQP7 expression/function in adipocytes may reduce adipocyte volume and fat mass in obesity.

Memapsin 2, a drug target for Alzheimer's disease

2003 ◽  
Vol 70 ◽  
pp. 213-220 ◽  
Author(s):  
Gerald Koelsch ◽  
Robert T. Turner ◽  
Lin Hong ◽  
Arun K. Ghosh ◽  
Jordan Tang
Keyword(s):  
Crystal Structure ◽  
Alzheimer’S Disease ◽  
Alzheimer's Disease ◽  
Transition State ◽  
Amyloid Precursor Protein ◽  
Therapeutic Target ◽  
Drug Target ◽  
Aspartic Protease ◽  
Precursor Protein ◽  
Memapsin 2

Mempasin 2, a ϐ-secretase, is the membrane-anchored aspartic protease that initiates the cleavage of amyloid precursor protein leading to the production of ϐ-amyloid and the onset of Alzheimer's disease. Thus memapsin 2 is a major therapeutic target for the development of inhibitor drugs for the disease. Many biochemical tools, such as the specificity and crystal structure, have been established and have led to the design of potent and relatively small transition-state inhibitors. Although developing a clinically viable mempasin 2 inhibitor remains challenging, progress to date renders hope that memapsin 2 inhibitors may ultimately be useful for therapeutic reduction of ϐ-amyloid.

CGMP as a New Drug Target in Atrial Fibrillation

2020 ◽  
Author(s):  
N. I. Bork ◽  
N. Grammatika-Pavlidou ◽  
B. Reiter ◽  
E. Girdauskas ◽  
H. Reichenspurner ◽  
...  
Keyword(s):  
Atrial Fibrillation ◽  
Drug Target ◽  
New Drug

Cyclin dependent kinase 4 as promising drug target in adrenocortical carcinoma

2019 ◽  
Author(s):  
Raimunde Liang ◽  
Isabel Weigand ◽  
Silviu Sbiera ◽  
Stefan Kircher ◽  
Juliane Lippert ◽  
...  
Keyword(s):  
Adrenocortical Carcinoma ◽  
Drug Target ◽  
Cyclin Dependent Kinase
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