pps
... During the optimization from the lead compound to the clinical candidate, molecules are usually becoming larger and more lipophilic (binding pocket is filled better). Thus, following properties are desirable for lead-like compounds: ...
... During the optimization from the lead compound to the clinical candidate, molecules are usually becoming larger and more lipophilic (binding pocket is filled better). Thus, following properties are desirable for lead-like compounds: ...
Symposium Report Role of Nuclear Receptors in Lipid Dysfunction
... pathways in the regulation of body weight and glucose homeostasis, we see the importance of using complementary approaches to elucidate this fascinating network of pathways. The observation that some receptors, like the farnesoid X receptor, can function in a tissue-specific manner via well defined ...
... pathways in the regulation of body weight and glucose homeostasis, we see the importance of using complementary approaches to elucidate this fascinating network of pathways. The observation that some receptors, like the farnesoid X receptor, can function in a tissue-specific manner via well defined ...
Localised prostate cancer
... Prostate cancer is an unusual cancer for a number of reasons: • it usually grows slowly and for many men it may not be a problem • there are often no symptoms in the early stages • treatment can have unwanted effects—especially on your sexual function ‘You don’t ask what the • the choice of treatmen ...
... Prostate cancer is an unusual cancer for a number of reasons: • it usually grows slowly and for many men it may not be a problem • there are often no symptoms in the early stages • treatment can have unwanted effects—especially on your sexual function ‘You don’t ask what the • the choice of treatmen ...
DESIGNING AND COMPUTATIONAL STUDY OF SOME NOVEL LAMIVUDINE ANALOGUES AS
... linkage essential for DNA chain elongation, and therefore, the viral DNA growth is terminated. Lamivudine possess an advantage over other anti HIV agents as it showed no evidence of carcinogenicity or mutagenicity in in vivo studies in mice and rats at doses from 10 to 58 times those used in humans. ...
... linkage essential for DNA chain elongation, and therefore, the viral DNA growth is terminated. Lamivudine possess an advantage over other anti HIV agents as it showed no evidence of carcinogenicity or mutagenicity in in vivo studies in mice and rats at doses from 10 to 58 times those used in humans. ...
Angiogenesis of Breast Cancer
... VEGF-A ligand. It is US Food and Drug Administration–approved for the first-line treatment of metastatic colorectal cancer when given in combination with fluorouracil and irinotecan, based on the demonstration of an overall survival benefit over standard chemotherapy alone.38 Bevacizumab has also demon ...
... VEGF-A ligand. It is US Food and Drug Administration–approved for the first-line treatment of metastatic colorectal cancer when given in combination with fluorouracil and irinotecan, based on the demonstration of an overall survival benefit over standard chemotherapy alone.38 Bevacizumab has also demon ...
Metformin and Cancer: Mounting Evidence Against
... the French lilac, has become the preferred first-line therapy for the treatment of type 2 diabetes (1). This drug is inexpensive, has an excellent safety profile, and can be safely combined with other antidiabetes agents (2). As a result, it has become the most widely prescribed antidiabetes drug worl ...
... the French lilac, has become the preferred first-line therapy for the treatment of type 2 diabetes (1). This drug is inexpensive, has an excellent safety profile, and can be safely combined with other antidiabetes agents (2). As a result, it has become the most widely prescribed antidiabetes drug worl ...
Looking towards label-free biomolecular interaction analysis
... kinetic constants. In total, they ranked almost 200 Fabs by their affinity towards hK1. In addition, SPR measurements were used to classify the Fabs according to their ability to recognize different active sites. ...
... kinetic constants. In total, they ranked almost 200 Fabs by their affinity towards hK1. In addition, SPR measurements were used to classify the Fabs according to their ability to recognize different active sites. ...
065IC Testosterone - American Urological Association
... benefits of male hormone replacement therapy and the relationship of the metabolic syndrome to testosterone deficiency syndrome (TDS) • Understand the scientific basis for androgen replacement therapy • Appraise the controversy regarding testosterone supplementation & prostate cancer • Gain knowledg ...
... benefits of male hormone replacement therapy and the relationship of the metabolic syndrome to testosterone deficiency syndrome (TDS) • Understand the scientific basis for androgen replacement therapy • Appraise the controversy regarding testosterone supplementation & prostate cancer • Gain knowledg ...
Thromboxane Receptors Antagonists and/or Synthase Inhibitors
... antithrombotic effects, depending on the cellular target. Thus, targeting TP receptor, a common downstream pathway for both platelet and extraplatelet TXA2 as well as for endoperoxides and isoprostanes, may be a useful antiatherosclerotic and a more powerful antithrombotic intervention in clinical s ...
... antithrombotic effects, depending on the cellular target. Thus, targeting TP receptor, a common downstream pathway for both platelet and extraplatelet TXA2 as well as for endoperoxides and isoprostanes, may be a useful antiatherosclerotic and a more powerful antithrombotic intervention in clinical s ...
Datasheet - Santa Cruz Biotechnology
... Steroid hormones function as signaling molecules by diffusing into cells and interacting with specific intracellular receptors to regulate gene expression. This superfamily of receptors includes both steroid and nonsteroid receptors. Like many nonsteroid hormone receptors, PXR (Pregnane X Receptor) ...
... Steroid hormones function as signaling molecules by diffusing into cells and interacting with specific intracellular receptors to regulate gene expression. This superfamily of receptors includes both steroid and nonsteroid receptors. Like many nonsteroid hormone receptors, PXR (Pregnane X Receptor) ...
Histamine and Antihistamines
... nausea and vomiting (Promethazine (Phenergan)). Phenergan also inhibits salivary and bronchial secretions and can be used as a local anesthetic. 5. Antiemetic: prevention or treatment of nausea and vomiting (Bendectin, doxylamine with pyridoxine). 6. Hypnotics: limited value. 7. Other uses: a. Reduc ...
... nausea and vomiting (Promethazine (Phenergan)). Phenergan also inhibits salivary and bronchial secretions and can be used as a local anesthetic. 5. Antiemetic: prevention or treatment of nausea and vomiting (Bendectin, doxylamine with pyridoxine). 6. Hypnotics: limited value. 7. Other uses: a. Reduc ...
Drug Effecting Platelet Function
... antiplatelet effects in vitro, but information on their in vivo effect is limited. Verapamil and diltiazem have the most consistent evidence supporting an antiplatelet effect. They inhibit platelet aggregation in whole blood. In a case-control study they were associated with an increased incidence o ...
... antiplatelet effects in vitro, but information on their in vivo effect is limited. Verapamil and diltiazem have the most consistent evidence supporting an antiplatelet effect. They inhibit platelet aggregation in whole blood. In a case-control study they were associated with an increased incidence o ...
NCCN Guidelines for Patients
... Sperm: Cells containing male genes that are needed to make babies Testosterone: A hormone that helps sexual organs in men work Urethra: A tube that expels urine and semen from a man’s body Vagina: The birth canal in women White blood cell: A type of blood cell that fights disease ...
... Sperm: Cells containing male genes that are needed to make babies Testosterone: A hormone that helps sexual organs in men work Urethra: A tube that expels urine and semen from a man’s body Vagina: The birth canal in women White blood cell: A type of blood cell that fights disease ...
GLASS: a comprehensive database for
... Motivation: G protein-coupled receptors (GPCRs) are probably the most attractive drug target membrane proteins, which constitute nearly half of drug targets in the contemporary drug discovery industry. While the majority of drug discovery studies employ existing GPCR and ligand interactions to ident ...
... Motivation: G protein-coupled receptors (GPCRs) are probably the most attractive drug target membrane proteins, which constitute nearly half of drug targets in the contemporary drug discovery industry. While the majority of drug discovery studies employ existing GPCR and ligand interactions to ident ...
Exemestane - BC Cancer Agency
... 3. Kvinnsland S, Anker G, Dirix LY, et al. High activity and tolerability demonstrated for exemestane in postmenopausal women with metastatic breast cancer who had previously failed on tamoxifen treatment. European Journal of Cancer 2000;36(8):976-82. 4. Pharmacia & Upjohn Inc. New drug submission, ...
... 3. Kvinnsland S, Anker G, Dirix LY, et al. High activity and tolerability demonstrated for exemestane in postmenopausal women with metastatic breast cancer who had previously failed on tamoxifen treatment. European Journal of Cancer 2000;36(8):976-82. 4. Pharmacia & Upjohn Inc. New drug submission, ...
KEY Problem Set: Penicillin Concepts Answer the following
... basic amino group (pKa ≈ 9) at the alpha-position of the 6-acylamino side and thus is a zwitterion at pH 7 (amino group predominantly positively ionized, carboxyl group predominately negatively ionized). Other penicillins (D and E) have additional nitrogen functionality in their 6-side chain, but t ...
... basic amino group (pKa ≈ 9) at the alpha-position of the 6-acylamino side and thus is a zwitterion at pH 7 (amino group predominantly positively ionized, carboxyl group predominately negatively ionized). Other penicillins (D and E) have additional nitrogen functionality in their 6-side chain, but t ...
G protein-coupled receptor dimers: Functional
... Kim & Arvan, 1998; Morello et al., 2000). These conditions, which are sometimes referred to as ER storage diseases (Callea et al., 1992), often involve a dominant-negative receptor mutant that effectively prevents surface expression of functional WT receptors, reducing potential binding sites and ab ...
... Kim & Arvan, 1998; Morello et al., 2000). These conditions, which are sometimes referred to as ER storage diseases (Callea et al., 1992), often involve a dominant-negative receptor mutant that effectively prevents surface expression of functional WT receptors, reducing potential binding sites and ab ...
Merck drug finasteride (PROSCAR)
... The development and enlargement of the prostate gland is dependent on the potent androgen, 5α-dihydrotestosterone (DHT). Type II 5α−reductase metabolizes testosterone to DHT in the prostate gland, liver and skin. DHT induces androgenic effects by binding to androgen receptors in the cell nuclei of t ...
... The development and enlargement of the prostate gland is dependent on the potent androgen, 5α-dihydrotestosterone (DHT). Type II 5α−reductase metabolizes testosterone to DHT in the prostate gland, liver and skin. DHT induces androgenic effects by binding to androgen receptors in the cell nuclei of t ...
John Salamone: Dopamine, Motivation and Schizophrenia
... antipsychotics based upon their mesolimbic actions; perhaps antipsychotic effects are due to actions on other systems (e.g. mesocortical DA). • They are related; the core antipsychotic effect could be directly dependent upon the fundamental motivational effects of D2 antagonists, which can be studie ...
... antipsychotics based upon their mesolimbic actions; perhaps antipsychotic effects are due to actions on other systems (e.g. mesocortical DA). • They are related; the core antipsychotic effect could be directly dependent upon the fundamental motivational effects of D2 antagonists, which can be studie ...
Evidence-based treatment for drug misuse, with special reference to
... Only limited international efforts to control abuse of tramadol at an international scale. In 2007, China took vigorous measures against tramadol marketing; this was associated with eventual decreasing levels of misuse in the general population ...
... Only limited international efforts to control abuse of tramadol at an international scale. In 2007, China took vigorous measures against tramadol marketing; this was associated with eventual decreasing levels of misuse in the general population ...
A Multimodal Data Analysis Approach for Targeted Drug Discovery
... against a certain target [8]. Hit identification is currently most often performed by high-throughput screening (HTS), a technique in which hundreds of thousands of compounds are assayed by robotics to determine which have the most significant activity against the target. The libraries that are screen ...
... against a certain target [8]. Hit identification is currently most often performed by high-throughput screening (HTS), a technique in which hundreds of thousands of compounds are assayed by robotics to determine which have the most significant activity against the target. The libraries that are screen ...
From the lead compound to the drug
... Displaced water molecules can form more hydrogen bonds (with other waters) outside the binding pocket. Likewise the dynamic change of H-bonds is simplified in bulk solution. Thus: The ligand should fit more precisely and thoroughly into the binding pocket. Simultaneously, the selectivity is improved ...
... Displaced water molecules can form more hydrogen bonds (with other waters) outside the binding pocket. Likewise the dynamic change of H-bonds is simplified in bulk solution. Thus: The ligand should fit more precisely and thoroughly into the binding pocket. Simultaneously, the selectivity is improved ...
The Value of Phenotypic Screening to Drug Discovery
... • when it works (when the target/MMOA are validated) it provides a ra;onal approach, analogous to engineering. • aligns with the poten;al for gene9cs to inform the cause of disease and provide biomarke ...
... • when it works (when the target/MMOA are validated) it provides a ra;onal approach, analogous to engineering. • aligns with the poten;al for gene9cs to inform the cause of disease and provide biomarke ...
The lead compound
... •Not easy to isolate membrane bound receptors • Carried out on whole cells, tissue cultures, or isolated organs • Affinity - strength with which compounds bind to a receptor • Efficacy - measure of maximum biochemical effect resulting from binding of a compound to a receptor. • Potency - concentrati ...
... •Not easy to isolate membrane bound receptors • Carried out on whole cells, tissue cultures, or isolated organs • Affinity - strength with which compounds bind to a receptor • Efficacy - measure of maximum biochemical effect resulting from binding of a compound to a receptor. • Potency - concentrati ...
Discovery and development of antiandrogens
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.