Peptide Drug Discovery refers to the use in human medicine of short chains of amino acids, called polypeptides, that have a biological activity that is therapeutic value in man. Among the best known of the naturally-occurring polypeptides of this nature are enkephalins and endorphins. Synthetic analogues of the substances manufactured within the body have been discovered to have therapeutic value as drugs.
Two of the best known classes of these molecules are the endorphins and enkephalins. These are endogenous opioid peptides that act on the central nervous system where they modulate neurophysiological processes such as responses to pain or stress, motivation and satiation. They are also active in the enteric nervous system in the gut. The term endogenous means they are synthesized in the body. Opiate and opioid drugs aim to mimic the activity of their endogenous counterparts. Opiates are drugs that are derived from the opium plant and include morphine, heroin and codeine. Opioids are synthetic analogues of opiates.
Another major group of molecules of this class are the tachykinins. These include Elediosin, Substance P, Kassinin and Neurokinins B and A. They are around five amino acids long and cause smooth muscle tissue in the digestive system to contract. Another group, the vasoactive intestinal peptides, are 28 AAs long. In this group are growth hormone releasing hormone, secretin, peptide histidine isoleucine, glucagon and pituitary adenylate cyclase activating peptide.
The calcitonin peptides form a fourth group of this type of molecule. These include calcitonin itself, along with AGG01 and Amylin. Within the human body, calcitonin is manufactured in the thyroid gland by the parafollicular cells. It counters the effects of parathyroid hormone by decreasing the amount of circulating calcium ions. Calcitonin derived from salmon is used as a treatment in postmenopausal women for osteoporosis. It is also used in the general population to treat phantom limb pain, bone metastases, Paget's disease and hypercalcemia (elevated plasma calcium levels).
The pancreatic polypeptide-related peptides include neuropeptide Y (NPY), PYY (peptide YY), APP (avian pancreatic polypeptide) and PPY (pancreatic polypeptide). Pancreatic polypeptide consists of about 36 amino acids and has a molecular weight of 4200 Daltons (a dalton is a unit of molecular mass and is equivalent to 1 g/mol).
Pancreatic polypeptide controls hepatic glycogen levels, modulates secretions in the digestive tract and controls the secretory functions in the pancreas. These secretions may be endocrine, acting on the pancreas itself, or exocrine, acting on distant organs. PP is secreted by the pancreas in response to a protein meal, fasting, exercising or during a bad attack of hypoglycemia. Ingesting glucose can reverse these effects.
Two very small groups of therapeutic polypeptides are the lactotripeptides and basic natriuretic peptide (BNP). The lactotripeptides consist of two polypeptides, each only three amino acid residues in length. They occur naturally in milk and have been credited with a possible activity in reducing blood pressure. BNP, also called B-type natriuretic peptide, is made up of 32 amino acids.
Peptide drug discovery has produced many beneficial natural and synthetic drugs. The molecules are all similar in that they are composed of short chains of amino acids, which are the building blocks of proteins. These drugs/molecules function in the central nervous system, the pancreas, thyroid and other human and animal organ systems. A small group called the lactotripeptides, although they are only three amino acid residues in length, may help to control blood pressure.
Two of the best known classes of these molecules are the endorphins and enkephalins. These are endogenous opioid peptides that act on the central nervous system where they modulate neurophysiological processes such as responses to pain or stress, motivation and satiation. They are also active in the enteric nervous system in the gut. The term endogenous means they are synthesized in the body. Opiate and opioid drugs aim to mimic the activity of their endogenous counterparts. Opiates are drugs that are derived from the opium plant and include morphine, heroin and codeine. Opioids are synthetic analogues of opiates.
Another major group of molecules of this class are the tachykinins. These include Elediosin, Substance P, Kassinin and Neurokinins B and A. They are around five amino acids long and cause smooth muscle tissue in the digestive system to contract. Another group, the vasoactive intestinal peptides, are 28 AAs long. In this group are growth hormone releasing hormone, secretin, peptide histidine isoleucine, glucagon and pituitary adenylate cyclase activating peptide.
The calcitonin peptides form a fourth group of this type of molecule. These include calcitonin itself, along with AGG01 and Amylin. Within the human body, calcitonin is manufactured in the thyroid gland by the parafollicular cells. It counters the effects of parathyroid hormone by decreasing the amount of circulating calcium ions. Calcitonin derived from salmon is used as a treatment in postmenopausal women for osteoporosis. It is also used in the general population to treat phantom limb pain, bone metastases, Paget's disease and hypercalcemia (elevated plasma calcium levels).
The pancreatic polypeptide-related peptides include neuropeptide Y (NPY), PYY (peptide YY), APP (avian pancreatic polypeptide) and PPY (pancreatic polypeptide). Pancreatic polypeptide consists of about 36 amino acids and has a molecular weight of 4200 Daltons (a dalton is a unit of molecular mass and is equivalent to 1 g/mol).
Pancreatic polypeptide controls hepatic glycogen levels, modulates secretions in the digestive tract and controls the secretory functions in the pancreas. These secretions may be endocrine, acting on the pancreas itself, or exocrine, acting on distant organs. PP is secreted by the pancreas in response to a protein meal, fasting, exercising or during a bad attack of hypoglycemia. Ingesting glucose can reverse these effects.
Two very small groups of therapeutic polypeptides are the lactotripeptides and basic natriuretic peptide (BNP). The lactotripeptides consist of two polypeptides, each only three amino acid residues in length. They occur naturally in milk and have been credited with a possible activity in reducing blood pressure. BNP, also called B-type natriuretic peptide, is made up of 32 amino acids.
Peptide drug discovery has produced many beneficial natural and synthetic drugs. The molecules are all similar in that they are composed of short chains of amino acids, which are the building blocks of proteins. These drugs/molecules function in the central nervous system, the pancreas, thyroid and other human and animal organ systems. A small group called the lactotripeptides, although they are only three amino acid residues in length, may help to control blood pressure.
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