Receptors in Disease

Bendall L. Chemokines and their receptors in disease. Histol Histopathol 2005 20(3) 907-926. 

There is now good evidence for a role of presynaptic neuropeptide Y receptors in disease states. As to the cardiovascular system, plasma neuropeptide Y levels are slightly increased in hypertensive patients and to a greater extent in cardiac failure (Morris 2004). An increase in neuropeptide Y levels is even an important prognostic marker for cardiovascular death in hemodialysis patients (Odar-Cederlof et al. 

E2. Ehara, H., Koji, T., Deguchi, T., Yoshii, A., Nakano, M., et al., Expression of estrogen receptor in diseased human prostate assessed by non-radioactive in situ hybridization and immunohistochemistry. Prostate 27, 304-313 (1995). 

GurneU, M., and V. K. Chatteijee. 2004. Nuclear receptors in disease Thyroid receptor beta, peroxisome-prohferators-activated receptor gamma and orphan receptors. Essays in Biochemistry 40 169-190. 

General trends in radiopharmaceutical research emphasize the use of small peptides. These molecules, of which the agents mentioned for thrombosis localization are an example, exhibit rapid and specific binding, and rapid blood clearance, two important parameters for a successflil radiopharmaceutical. Peptides are readily labeled with Tc and lend themselves to formulation as lyophilized kits that can be rapidly and rehably reconstituted. Possible targets for these molecules are quite varied, ranging from atherosclerotic plaque to P-amyloid (for Alzheimer s disease), to a variety of somatic receptors the populations of which are increased or decreased in disease. 

The involvement of serotonin (5-hydroxytryptamine) in disease states has been recognized for several decades. Research on antagonists awaited the recent development of methodology involving serotonin receptors. A thiazolopyrimidone serves as the nucleus for a pair of serotonin antagonists. The key intermediate 118 is in fact simply the lactonized form of 2-hydroxyethyl acetoace-tate. Condensation of this P-keto ester can be visualized to involve initial attack on the reactive... 

Polymorphisms have been described for all (3-adrenergic receptors while initial studies, notably of the (3i-subtype, suggested that these might be predictors of diseases as well as of therapeutic responses, these results have more recently been questioned. Alterations in responsiveness may be limited to certain compounds and a causative role in diseases has not been or remains to be substantiated in larger trials. 

Paschke R, Ludgate M (1997) The thyrotropin receptor in thyroid diseases. N Engl J Med 337 1675-1681... 

Andersen OM, Willnow TE (2006) Lipoprotein receptors in Alzheimer s disease. Trends Neurosci 29 687-694... 

Leger AJ, Covic L, Kuliopulos A (2006) Protease-activated receptors in cardiovascular disease. Circulation 114 1070-1077... 

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