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bicalutamide-ga - Actavis think smart medicine
... Bicalutamide is a nonsteroidal antiandrogen devoid of other endocrine activity. It binds to androgen receptors without activating gene expression and thus inhibits the androgen stimulus. This inhibition impairs the growth and encourages apoptosis in androgen dependent tumour cells and regression of ...
... Bicalutamide is a nonsteroidal antiandrogen devoid of other endocrine activity. It binds to androgen receptors without activating gene expression and thus inhibits the androgen stimulus. This inhibition impairs the growth and encourages apoptosis in androgen dependent tumour cells and regression of ...
Targeting the androgen receptor in the
... Since the year 2000, tremendous progress has been made in the understanding of castration-resistant prostate cancer (crpc), a disease state now recognized to retain androgen receptor (ar)—dependency in most cases. That understanding led to the rational design of novel therapeutic agents targeting ho ...
... Since the year 2000, tremendous progress has been made in the understanding of castration-resistant prostate cancer (crpc), a disease state now recognized to retain androgen receptor (ar)—dependency in most cases. That understanding led to the rational design of novel therapeutic agents targeting ho ...
FEP-Guidance for Rapid Lead Optimization of Anti-HIV
... Department of Chemistry, Yale University, New Haven, CT 06520-8107 Drug development is being pursued through computer-aided design, synthesis, and assaying. The design begins with use of the BOMB program, which rapidly constructs combinatorial libraries given the structure of the target protein and ...
... Department of Chemistry, Yale University, New Haven, CT 06520-8107 Drug development is being pursued through computer-aided design, synthesis, and assaying. The design begins with use of the BOMB program, which rapidly constructs combinatorial libraries given the structure of the target protein and ...
2009 American Urological Association Abstracts – PCEC
... Abstract: Introduction and Objective: PSA, the standard screening test for prostate cancer (CaP), has low sensitivity/specificity. The PCA3 test is a new diagnostic tool that is increasingly used in clinical practice. Its feasibility and performance has not been evaluated in a true screening populat ...
... Abstract: Introduction and Objective: PSA, the standard screening test for prostate cancer (CaP), has low sensitivity/specificity. The PCA3 test is a new diagnostic tool that is increasingly used in clinical practice. Its feasibility and performance has not been evaluated in a true screening populat ...
Brief Receptor Theory
... agonist causes a maximal effect equal to that of the endogenous ligand (or sometimes another reference compound if the endogenous ligand is not known); a partial agonist causes less than a maximal response. – Intrinsic efficacy (outmoded): the property of how a ligand causes biological responses via ...
... agonist causes a maximal effect equal to that of the endogenous ligand (or sometimes another reference compound if the endogenous ligand is not known); a partial agonist causes less than a maximal response. – Intrinsic efficacy (outmoded): the property of how a ligand causes biological responses via ...
Pharm Test 1
... a2 agonists as smypatholytics stimulation to cause decrease sympathetic outflow (anti-HTN), ↓ TPR methyldopa – prodrug, so must be converted first clonidine – withdrawal, vascular HA, diabetic diarrhea, 2nd line HTN drug side effects – drowsiness, dry mouth Adrenergic Antagonists a1 antagonists – ...
... a2 agonists as smypatholytics stimulation to cause decrease sympathetic outflow (anti-HTN), ↓ TPR methyldopa – prodrug, so must be converted first clonidine – withdrawal, vascular HA, diabetic diarrhea, 2nd line HTN drug side effects – drowsiness, dry mouth Adrenergic Antagonists a1 antagonists – ...
Laparoscopic radical prostatectomy
... 1990's in France and set the benchmark for minimally invasive radical prostatectomy. The operation is extremely difficult to perform because in laparoscopy for all surgical areas the instruments are long, rigid and movements are counterintuitive. ( a bit like shaving left handed in a mirror!) There ...
... 1990's in France and set the benchmark for minimally invasive radical prostatectomy. The operation is extremely difficult to perform because in laparoscopy for all surgical areas the instruments are long, rigid and movements are counterintuitive. ( a bit like shaving left handed in a mirror!) There ...
Definition of the word `Drug`: Drugs are chemicals that prevent
... steric interactions between specific chemical groups of the drug. These sites are termed receptors. Types of Receptors: There are several types of receptors. G-protein coupled receptors, ion-gated channels, enzyme-linked receptors, intracellular receptors. Receptor definition is changing … DNA a ...
... steric interactions between specific chemical groups of the drug. These sites are termed receptors. Types of Receptors: There are several types of receptors. G-protein coupled receptors, ion-gated channels, enzyme-linked receptors, intracellular receptors. Receptor definition is changing … DNA a ...
Neurotransmitter Receptors - VCC Library
... urinating, constipation, potential for diabetes (high glucose concentration from glycogenolysis), and low blood pressure due to dilation of vessels. 2. A 1-antagonist would help decrease the heart rate and force of contraction. Also, an M2-agonist would slow the heart rate to normal. By combining t ...
... urinating, constipation, potential for diabetes (high glucose concentration from glycogenolysis), and low blood pressure due to dilation of vessels. 2. A 1-antagonist would help decrease the heart rate and force of contraction. Also, an M2-agonist would slow the heart rate to normal. By combining t ...
Controversies Surrounding Androgen Deprivation for Prostate Cancer
... the AR is phosphorylated by either protein kinase B (AKT) or mitogen-activated protein kinase (MAPK), resulting in a ligand-independent AR.1 HER-2/neu, a member of the EGF-receptor family of RTKs, deserves special mention. In breast cancer, estrogen independence correlates with HER-2/neu overexpres ...
... the AR is phosphorylated by either protein kinase B (AKT) or mitogen-activated protein kinase (MAPK), resulting in a ligand-independent AR.1 HER-2/neu, a member of the EGF-receptor family of RTKs, deserves special mention. In breast cancer, estrogen independence correlates with HER-2/neu overexpres ...
2nd Lecture 1433
... It must be selective in choosing ligands/drugs to bind To avoid constant activation of the receptor by promiscuous binding of many different ligands It must change its function upon binding in such a way that the function of the biologic system (cell, tissue, etc) is altered This is necessar ...
... It must be selective in choosing ligands/drugs to bind To avoid constant activation of the receptor by promiscuous binding of many different ligands It must change its function upon binding in such a way that the function of the biologic system (cell, tissue, etc) is altered This is necessar ...
Problemset 6
... decreased concentrations of aldosterone. Nevertheless, GCs cause sodium and water retention, and hypertension. Explain! GCs have low affinity for the mineralcorticoid receptors. At physiological GC concentrations, GC display no binding to the aldosterone receptor. However, at elevated GC concentrati ...
... decreased concentrations of aldosterone. Nevertheless, GCs cause sodium and water retention, and hypertension. Explain! GCs have low affinity for the mineralcorticoid receptors. At physiological GC concentrations, GC display no binding to the aldosterone receptor. However, at elevated GC concentrati ...
Receptors and Protein-Protein Interaction ----
... Receptors and Protein-Protein Interaction -----signal transduction proteins Primary messenger ...
... Receptors and Protein-Protein Interaction -----signal transduction proteins Primary messenger ...
File - Introduction
... immobilized in a Civco Vac-Lok cradle (Figure 1). The hands were placed on the chest holding a blue ring. A urethrogram was performed to help visualize the apex of the prostate as there was no magnetic resonance imaging (MRI) study to fuse with the planning CT. Once the patient was immobilized prope ...
... immobilized in a Civco Vac-Lok cradle (Figure 1). The hands were placed on the chest holding a blue ring. A urethrogram was performed to help visualize the apex of the prostate as there was no magnetic resonance imaging (MRI) study to fuse with the planning CT. Once the patient was immobilized prope ...
Molecular Imaging and Prostate Cancer: Get the Facts
... generally not used to image prostate cancer, but some physicians have found PET/CT imaging useful in identifying fast-growing, aggressive tumors. In addition, PET/CT can be used in place of bone scans to painlessly determine whether prostate cancer has spread to the bone, a common occurrence. (For m ...
... generally not used to image prostate cancer, but some physicians have found PET/CT imaging useful in identifying fast-growing, aggressive tumors. In addition, PET/CT can be used in place of bone scans to painlessly determine whether prostate cancer has spread to the bone, a common occurrence. (For m ...
Protein–Ligand Interactions as the Basis for Drug Action
... • Ligand (the key..) is typically flexible • Also protein is adapting a different conformation upon ligand binding • If we know the protein target then “Structure-‐ based design” is used (methods like docking) • It ...
... • Ligand (the key..) is typically flexible • Also protein is adapting a different conformation upon ligand binding • If we know the protein target then “Structure-‐ based design” is used (methods like docking) • It ...
Léčiva působící prostř. histaminu, serotoninu a dopaminu
... (historical example cimetidine) • Antagonists of H3 receptors = betahistin for Meniere disease and problems like tinnitus, hearing loss ...
... (historical example cimetidine) • Antagonists of H3 receptors = betahistin for Meniere disease and problems like tinnitus, hearing loss ...
Drugs and the Brain teaser (PPT)
... Neurotransmitter: A signaling molecule, it crosses the synapse Hormone: Another type of signaling molecule. The border between neurotransmitter and hormone is blurry, many chemicals are both. Receptor: A protein that detects a specific chemical, by binding to it Ligand: A molecule that binds to a re ...
... Neurotransmitter: A signaling molecule, it crosses the synapse Hormone: Another type of signaling molecule. The border between neurotransmitter and hormone is blurry, many chemicals are both. Receptor: A protein that detects a specific chemical, by binding to it Ligand: A molecule that binds to a re ...
T5_a: High resolution copy of the slides of the talk
... What are the cocaine effects ? -Block of catecholam. and 5-HT reuptake (PD) -Increased arousal and performance, decreased fatigue -Inc. BP, heart rate and self-confidence ...
... What are the cocaine effects ? -Block of catecholam. and 5-HT reuptake (PD) -Increased arousal and performance, decreased fatigue -Inc. BP, heart rate and self-confidence ...
351 Pharmacology 3rd sf
... bind To avoid constant activation of the receptor by promiscuous binding of many different ligands It must change its function upon binding in such a way that the function of the biologic system (cell, tissue, etc) is altered This is necessary for the ligand to cause a pharmacologic effect ...
... bind To avoid constant activation of the receptor by promiscuous binding of many different ligands It must change its function upon binding in such a way that the function of the biologic system (cell, tissue, etc) is altered This is necessary for the ligand to cause a pharmacologic effect ...
Healthy lifestyle for men living with hormone therapy for prostate
... associated with progression of bone metastases and reduced overall survival. The exact significance of this is currently unclear as there was no bone scan monitoring in this trial. In addition, a further subanalysis of the one-year study demonstrated a 10 per cent difference in PSA progression, with ...
... associated with progression of bone metastases and reduced overall survival. The exact significance of this is currently unclear as there was no bone scan monitoring in this trial. In addition, a further subanalysis of the one-year study demonstrated a 10 per cent difference in PSA progression, with ...
Case Study: Collaborative Care - American College of Radiology
... software enhancements with dedicated radiology interpretation, enabling the most accurate mapping possible for targeted biopsies; and creative scheduling between centers for optimal efficiency and satisfaction. This collaborative approach is delivering high-value care to Lakeland. Patients are affor ...
... software enhancements with dedicated radiology interpretation, enabling the most accurate mapping possible for targeted biopsies; and creative scheduling between centers for optimal efficiency and satisfaction. This collaborative approach is delivering high-value care to Lakeland. Patients are affor ...
Medicines additional questions LT Scotland
... Identify the pharmacophore that is responsible for the pain killing effect. ...
... Identify the pharmacophore that is responsible for the pain killing effect. ...
Discovery and development of antiandrogens
![](https://commons.wikimedia.org/wiki/Special:FilePath/Androgen_receptor.png?width=300)
In the 1960s, the first antiandrogen, or androgen antagonist, was discovered. Antiandrogens antagonise the androgen receptor (AR) and thereby block the biological effects of testosterone and dihydrotestosterone (DHT). Antiandrogens are important for men with hormonally responsive diseases like prostate cancer, benign prostatic hyperplasia (BHP), acne, seborrhea, hirsutism and androgen alopecia. Antiandrogens are mainly used for the treatment of prostate diseases. Research from 2010 suggests that ARs could be linked to the disease progression of triple-negative breast cancer and that antiandrogens can potentially be used to treat it.As of 2010 antiandrogens are small molecules and can be either steroidal or nonsteroidal depending on ligand chemistry. Steroidal antiandrogens share a similar steroid structure, while nonsteroidal antiandrogens may have structurally distinctive pharmacophores. Only a limited number of compounds are available for clinical use despite the fact that a very large variety of antiandrogen compounds have been discovered and researched.