Done for my cell bio class
Tamoxafin by richard logan since its approval in 1998 tamoxifen has been used to treat millions of women and man diagnosed with hormone receptor-positive breast cancer a large proportion of breast cancers expressed the estrogen receptor and the progression is dependent on intact estrogen signaling treatment of er-positive breast cancers usually includes a therapy that
Is designed to block estrogen signaling this is where tamoxifen comes in to describe in a cellular level i made a little video for you on the next slide this is your regular generic cell has a few organelles and a nucleus where dna is kept as you can observe the bigger than usual estrogen receptors now these are where estrogen comes into the cell and binds you see
Right here that turns our bond to each receptor and helps the cell with normal function this is in that healthy cell now in the cancer cells you have a bunch of estrogen bunch of is going to flow into the cell and it’s going to keep and the cells you’re going to keep on accepting it making the cell grow and divide rapidly making the tumor grow bigger and bigger now
The role tamoxifen is there’s a races real quick there’s a coming here and bind to these sites right here there’s tamoxifen you’re gonna bond three sites where the estrogen or nobody come the ex has a cap on the receptors where the extra normally bind now when estrogen tries to come in when tries to come into the cell it’s gonna get stopped by the tamoxifen and bounce
Off and therefore the cell cannot grow into by thus that cancer is stopped so as i said in the last video tamoxifen competitively inhibit the binding edge radio to estrogen receptors thereby preventing the receptor from binding to the estrogen response element on dna tamoxifen is a pro drug with relatively low infinity for the estrogen receptor it undergoes extensive
First-pass oxidative metabolism and two more active metabolites by the cytochrome p450 pathway in addition tamoxifen up regulates the production of transforming growth factor being a factor that hibbott tumor cell growth and down regulates insulin-like growth factor a factor that stimulates breast cancer cell growth tamoxifen has both estrogenic and intelligent ik
Actions depending on the target tissue it is strongly anti trial genacore memory epithelium hence it’s used in both the prevention and treatment of breast cancer it is pros trial jenica on uterine epithelium resulting in the current controversy regarding safety in cancer prevention which i’ll explain the next side this is what we define tamoxifen as a selective
Estrogen receptor modulator meaning is selected either blocks or activates estrogens actions on specific cells for example or tamoxifen blocks estrogens action on breast cells it activates estrogens action and bone and liver cells so they help stop bone loss after menopause and lower cholesterol levels so as i previously stated in the last slide is tamoxifen spro
Estrogenic property on uterine epithelium that have resulted in the current controversy regarding safety in cancer prevention this is due to the dissociation and increased incidence of val endometrial lesions including hyperplasia carcinomas and sarcoma a woman undergoing chronic treatment with tamoxifen with time the risk of endometrial cancer increases jessica
Lee which is a reason tamoxifen is typically recommended for five years but not all of the pro estrogen effects are harmful tamoxifen pro stage and the action is also evident in bone matter where mimics the effects of estrogen and provides the signals required for bone maintenance thereby inhibiting osteo tests and reducing the risk also paralysis and menopausal
Women in particular tamoxifen selective estrogen activation if this can cause some serious side effects as i listed marrying here but i highlight the two main ones that women complain of which are hot flashes in nausea so the question i have for while tamoxifen is commonly known as it estrogen this is not an accurate description of his clinical activity why is that references
Transcribed from video
Tamoxifen By Richard Logan
