PEPTIDES

One important concept is that the carboxyl carbon is planar, due to the
partial double-bond character of the amide group. That is, the three atoms
bonded with the nitrogen are squashed into the same plane as the nitrogen,
rather than forming a tetrahedonal structure as in the case of the ammonia
molecule. The planar regions in this picture below are shaded.
Peptides
Amino acids are linked together in proteins by a special kind
of bond, the peptide bond
(Videoshow:MCB0301




































































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Peptide
CLASIFICARE
In functie de nr de aminoacizi distingem:
A. Oligopeptide
B. Polippetide

OLIGOPEPTIDE:
Di-peptide (2 aminoacizi)
Tri-peptide (3 aminoacizi)
.
.
.
.
. Deca-peptide (10 aminoacizi)
Peptides
INSULINA: descovered first by the Romanian
biochemist Nicolae Paulescu. For teh Nobel Prize
credit was given to Banting & Best (Canada)
Peptides
INSULINE: First peptide to be sequenced by
SANGER (UK)
Peptides
INSULINE: First peptide to be sequenced by
SANGER (UK)
Peptides
INSULINA: Tridimensional structure




































































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Insulin will lower the glucose levels in the blood.
For this action it needs to bind an insulin receptor




































































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Role of insulin: Patients with defects in insulin receptor will suffer
from type II diabetes (also called insulin resistance)




































































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Type 2 diabetes is a glucose metabolism disorder. On the one hand, body tissue
develops a partial resistance to insulin, one of the bodys own hormones, which is
responsible for metabolizing the dissolved glucose in the blood. On the other hand,
the limited function of the beta cells in the pancreas leads to an insufficient supply of
insulin. The active ingredient metformin hydrochloride corrects the insulin resistance
by making tissues, such as the liver and muscles, receptive to insulin uptake. This
process reduces glucose production in the liver while simultaneously enhancing
glucose uptake in the muscles, where the glucose is stored as glycogen or burned to
produce energy. The result is a restoration of the normal glucose level the most
important objective in treatment of type 2 diabetes. The British UKPDS study has
shown that metformin not only reduces the glucose content in the blood, but that it
also significantly reduces the risk of long-term complications including heart attack or
stroke.
Peptide:
Exemple
Exemple clasice

Hormoni peptidici, exemple
Oxitocina, Vasopresina
Peptide:
Exemple
Cyclic Peptides: VALINOMICINE
Valinomicin: specific for the
potassiumm ion transport
(green)

Used as antibiotic




































































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BIOACTIVE DiPEPTIDES
Carnosine (beta-alanyl-L-histidine)

dipeptide of the amino acids beta-alanine and histidine. It is highly
concentrated excitable tissues such as muscle and brain.




































































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Physiological Functions of Carnosine :
"L-carnosine (beta-alanyl-L-histidine) act as natural antioxidants
with hydroxyl-radical-scavenging and lipid-peroxidase activities"
Carnosine (-alanyl-L-histidine) is present in high
concentrations in human skeletal muscle
Muscle carnosine loading slightly but significantly attenuates fatigue
in repeated bouts of exhaustive dynamic contractions




































































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Anserine
Anserine (beta-alanyl-N-methylhistidine) is a dipeptide found in the
skeletal muscle and brain of mammals,[1] and birds.

Antioxidant (about 5 times that of carnosine) and helps reduce muscle
fatigue




































































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BIOACTIVE Tri-PEPTIDES
Glutathione (GSH)

tripeptide with a gamma peptide linkage between the amine group of
cysteine (which is attached by normal peptide linkage to a glycine)
and the carboxyl group of the glutamate side-chain. It is an
antioxidant, preventing damage to important cellular components
caused by reactive oxygen species such as free radicals and
peroxides




































































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Glutathione exists in reduced (GSH) and oxidized (GSSG) states
In healthy cells and tissue, more than 90% of the total
glutathione pool is in the reduced form (GSH) and less than
10% exists in the disulfide form (GSSG)
An increased GSSG-to-GSH ratio is considered indicative of
oxidative stress.
Glutathione has multiple functions

It is the major endogenous antioxidant produced by the cells

It is used in metabolic and biochemical reactions such as DNA synthesis
and repair, protein synthesis, prostaglandin synthesis, amino acid transport,
and enzyme activation

It has a vital function in iron metabolism
.
BIOACTIVE Tri-PEPTIDES




































































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Thyrotropin-releasing hormone
BIOACTIVE Tri-PEPTIDES




































































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Thyrotropin-releasing hormone (TRH), also called
thyrotropin-releasing factor (TRF), thyroliberin or protirelin,

Tropic, tripeptidal hormone that stimulates the release of TSH
(thyroid-stimulating hormone) and prolactin from the anterior
pituitary. TRH has been used clinically for the treatment of
spinocerebellar degeneration and disturbance of consciousness
in humans




































































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BIOACTIVE Penta-PEPTIDES
Enkephalins

either of two pentapeptides (leu-enkephalin and met-
enkephalin) occurring in the brain and spinal cord and
also in the gastrointestinal tract;


Functions: Enkephalins function as neurotransmitters
or neuromodulators and inhibit neurotransmitters in the
pathway for pain perception, thereby reducing the
emotional as well as the physical impact of pain




































































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BIOACTIVE Penta-PEPTIDES
"endogenous morphine", meaning morphine produced naturally in the body that
function as neurotransmitters
Endorphins
They are produced by the pituitary gland and the hypothalamus in
vertebrates during exercise, excitement, pain, consumption of spicy food,
love and orgasm

they resemble the opiates in their abilities to produce analgesia and a
feeling of well-being.




































































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Oxytocin (Oxt) is a mammalian hormone that acts primarily as a
neuromodulator in the brain
BIOACTIVE Nano-PEPTIDES
Oxytocin is best known for its roles in sexual reproduction, in particular
during and after childbirth. It is released in large amounts after distension
of the cervix and uterus during labor, facilitating birth, and after stimulation
of the nipples, facilitating breastfeeding




































































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BIOACTIVE Nano-PEPTIDES
Oxytocin (Oxt)
Recent studies have begun to investigate oxytocin's role in various behaviors,
including orgasm, social recognition, pair bonding, anxiety, and maternal
behaviors.

For this reason, it is sometimes referred to as the "love hormone". The inability
to secrete oxytocin and feel empathy is linked to sociopathy, psychopathy,
narcissism,

and general manipulativeness.

There is some evidence that oxytocin promotes 'tribal' behaviour, incorporating
the trust and empathy of in-groups with their suspicion and rejection of
outsiders




































































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Vasopressin
BIOACTIVE Nano-PEPTIDES
Arginine vasopressin (AVP), also known as vasopressin, argipressin
or antidiuretic hormone (ADH), is a

neurohypophysial hormone found in most mammals. Vasopressin is
responsible for regulating the body's retention of water by acting to
increase water absorption in the collecting ducts of the kidney nephron
Fig. xxxx: Myofibril contraction
Fig. xxx: Structure of the thick filament
Fig.xx: The myosin molecule
Fig XX: Mechanism of
force generation in
muscle
Fig. XX: Primary and secondary immune response
Fig. XX: Diagram of Immunoglobulin G IgG
Fig. XX; Structure of a mouse Antibody
Influenza peptide bound to an
Antibody;
Note the Ab surrounds the peptide.
Influenza peptide shown with Ab structure
in
the absence of the peptide. Comparison
with
(a) shows how much the Ab conformation
changes when the peptide binds.




































































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