As one of the largest and most diverse protein families in nature, the G-protein coupled receptor (GPCR) superfamily play important roles in a variety of biological and pathological processes such as development and proliferation, neuromodulation, angiogenesis, metabolic disorders, inflammation, and viral infection. Not surprisingly, it is one of the most targeted protein families in pharmaceutical research today (Schlyer 2006).
All members of this superfamily share a similar seven transmembrane domain, but are grouped on the basis of shared sequence motifs into the following broad classes:
Class A Rhodopsin-like
Class B Secretin-like
Class C Metabotropic glutamate/pheromone
Class D Fungal pheromone
Class E cAMP receptors
Frizzled/Smoothened
Vomeronasal receptors
Putative/unclassified
The pharmaceutical industry has focused on development of modulators to this protein family, but GPCRs also represent an attractive target as biomarkers. Recent studies have implicated endothelin receptors, chemokine receptors and lysophosphatidic acid receptors in tumorgenesis and metastasis, and a recent in silico analysis found a number of GPCRs that were up-regulated in various cancers which suggests not only targets of therapeutic value, but of diagnostic and prognostic value as well. A summary of these up-regulated receptors is below.
Lung cancer
Edg2, P2Y purinoceptor 6, PAR-2, PAR-3, GPR68
Breast cancer
CCR1, CXCR-4, PAR-2
Prostate cancer
Beta 2 adrenergic receptor, […]
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According to the National Cancer Institute (NCI), prostate cancer is the second most common form of cancer as well as the second leading cause of cancer-related deaths among American men. A prostate specific antigen (PSA) test has been shown to detect prostate cancer in its earliest stages. Even though cancer screenings are very important they are just one health concern when it comes to the prostate. As men get older, the prostate may become a source for many other problems that can, but not necessarily always, include cancer. Since the symptoms of some prostate conditions often mimic cancer, many men who learn they have a problem often immediately assume the worst. Therefore, it is important to understand the prostate and how potential changes might affect your health. Additionally, it is good to know what natural supplements you can take to ensure your prostate ages healthfully.
The prostate is a walnut-shaped gland found only in men just below the bladder and around the urethra, which functions as part of the male reproductive system. Throughout life the prostate continues to grow larger, but only after it becomes too large do problems begin to occur. The most common problem for men under fifty is […]
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The most common reason for exercising is to lose weight and get a thinner body. While this is a great reason to get fit, did you know that there are countless other reasons why you should get fit? We all know that exercise is good for you, but did you know just how good it really was? Exercise can help relieve depression, it can help you decrease your chance of cancer and it can boost your immune system. The best benefit of all is getting a healthy heart. Heart disease is becoming the number one killer in women and exercising can help prolong your life especially if heart disease runs in your family.You do not have to run marathons or spend hours upon hours working out to see the benefits. Most experts say that regular moderate exercise will be fine. Though you will see more benefits from more vigorous exercise included faster weight loss and gaining more endurance. One study has shown that women who followed a vigorous program had lowered their rate of prostate cancer.There have also been studies that have shown that regular […]
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