![Etifoxine (Stresam®) for chemotherapy-induced pain?](http://s1.studyres.com/store/data/007845113_1-b11d3bed63b5797d86d172586ab8fc07-300x300.png)
Etifoxine (Stresam®) for chemotherapy-induced pain?
... The majority of patients with cancer suffer from pain, in particular during advanced stages of the disease [6]. The pain can originate from the tumor itself, but in many cases it occurs as a consequence of cancer chemotherapy. In particular vinca alkaloids, taxanes and platinum drugs, which are ofte ...
... The majority of patients with cancer suffer from pain, in particular during advanced stages of the disease [6]. The pain can originate from the tumor itself, but in many cases it occurs as a consequence of cancer chemotherapy. In particular vinca alkaloids, taxanes and platinum drugs, which are ofte ...
Cylene Builds on Success, Presents Second CK2 Inhibitor at AACR
... CX-8184, demonstrating our commitment to exploiting the CK2 target for cancer combination therapy,” commented William G. Rice, Ph.D., President and CEO of Cylene Pharmaceuticals. “As the limitations of suppressing a single target are becoming clear, the need for agents that hit multiple key cancer p ...
... CX-8184, demonstrating our commitment to exploiting the CK2 target for cancer combination therapy,” commented William G. Rice, Ph.D., President and CEO of Cylene Pharmaceuticals. “As the limitations of suppressing a single target are becoming clear, the need for agents that hit multiple key cancer p ...
Investigative study on the angiotensin converting enzyme (ACE
... out by the fact that ACE-LBP maps and proposed pharmacophores were obtained that differed according to resident ligand. This was indicative of the fact that LBP conformation is essentially ligand driven. The fact that for example, ursolic acid had a LBA which was highest when captopril was used as a ...
... out by the fact that ACE-LBP maps and proposed pharmacophores were obtained that differed according to resident ligand. This was indicative of the fact that LBP conformation is essentially ligand driven. The fact that for example, ursolic acid had a LBA which was highest when captopril was used as a ...
Non-depolarizing blocking agents
... motoneurons. At this point, full neuromuscular block has been achieved. The prototypical depolarizing blocking drug is succinylcholine (suxamethonium). It is the only such drug used clinically. It has a rapid onset (30 seconds) but very short duration of action (5–10 minutes) because of hydrolysis b ...
... motoneurons. At this point, full neuromuscular block has been achieved. The prototypical depolarizing blocking drug is succinylcholine (suxamethonium). It is the only such drug used clinically. It has a rapid onset (30 seconds) but very short duration of action (5–10 minutes) because of hydrolysis b ...
Autonomic Nervous System
... cases of bradyasystolic arrest Atropine should be used with extreme caution in the setting of myocardial infarct second-degree type II and 3 degree heart block with wide QRS complexes, transcutaneous pacing is a preferred method of therapy ...
... cases of bradyasystolic arrest Atropine should be used with extreme caution in the setting of myocardial infarct second-degree type II and 3 degree heart block with wide QRS complexes, transcutaneous pacing is a preferred method of therapy ...
citeline Pharma r&d annual review 2015
... which both post double-digit inflations (up 17.9% and 15.1%, respectively). Among the larger groups, Alimentary/Metabolic has the most impressive expansion, with a 9.5% growth in the number of pipeline projects. Note that throughout this section, there can be some double-counting if a drug is under ...
... which both post double-digit inflations (up 17.9% and 15.1%, respectively). Among the larger groups, Alimentary/Metabolic has the most impressive expansion, with a 9.5% growth in the number of pipeline projects. Note that throughout this section, there can be some double-counting if a drug is under ...
Problems in early drug development: PARP inhibitors
... 18 members of PARP super-family identified to date PARP-1 abundant nuclear enzyme activated by and binds with high affinity to DNA single and double strand breaks via zinc fingers PARP-1 essential for the repair of damaged bases and single strand breaks via the Base Excision repair pathway ...
... 18 members of PARP super-family identified to date PARP-1 abundant nuclear enzyme activated by and binds with high affinity to DNA single and double strand breaks via zinc fingers PARP-1 essential for the repair of damaged bases and single strand breaks via the Base Excision repair pathway ...
Dose-Response Concept
... 90 days is the most common test duration but 30 days to 90 days can be used Usually oral administration of the chemical via food; also implant Used to further characterize the specific organs affected by test compound after repeated administration of the chemical ...
... 90 days is the most common test duration but 30 days to 90 days can be used Usually oral administration of the chemical via food; also implant Used to further characterize the specific organs affected by test compound after repeated administration of the chemical ...
Autacoids
... Moreover, concomitant use of these agents with drugs or foods that inhibit their hepatic metabolism (ketonazole, macrolides, & grapefruit juice) is contraindicated because such a combination results in significantly elevated anti-histamine plasma levels. The incidence of arrhythmias was great enough ...
... Moreover, concomitant use of these agents with drugs or foods that inhibit their hepatic metabolism (ketonazole, macrolides, & grapefruit juice) is contraindicated because such a combination results in significantly elevated anti-histamine plasma levels. The incidence of arrhythmias was great enough ...
Antimetastatic Potential of N-Acetylcysteine on Human Prostate
... * Department of Surgery, Faculty of Medicine, Srinakharinwirot University, Nakhon Nayok, Thailand ** Department of Physiology, Faculty of Medicine, Srinakharinwirot University, Bangkok, Thailand Objective: N-acetylcysteine (NAC), is one of the cheapest, safest and widely used over-the-counter-drugs ...
... * Department of Surgery, Faculty of Medicine, Srinakharinwirot University, Nakhon Nayok, Thailand ** Department of Physiology, Faculty of Medicine, Srinakharinwirot University, Bangkok, Thailand Objective: N-acetylcysteine (NAC), is one of the cheapest, safest and widely used over-the-counter-drugs ...
Real-Time Monitoring of Antibody Binding by Parallel MP
... response to injections of MTX, h-IgG and anti-MTX in a broad concentration range, while Figure 3. shows the results for the MP-SPR in parallel with the modulus of the impedance. The results show that a longer equilibration time before the first injection would provide better results. However, the ef ...
... response to injections of MTX, h-IgG and anti-MTX in a broad concentration range, while Figure 3. shows the results for the MP-SPR in parallel with the modulus of the impedance. The results show that a longer equilibration time before the first injection would provide better results. However, the ef ...
Electrochemical behavior and differential pulse voltametric
... The chemical name of bicalutamide is (RS)-N-[4cyano-3-(trifluoromethyl) phenyl]-3-[(4-fluorophenyl) sulfonyl]-2-hydroxy-2-methyl-propanamide, under the trade name of Casodex [1–3]. It belongs to a class of drugs called antiandrogens that includes flutamide (Eulexin) and nilutamide (Nilandron). Andro ...
... The chemical name of bicalutamide is (RS)-N-[4cyano-3-(trifluoromethyl) phenyl]-3-[(4-fluorophenyl) sulfonyl]-2-hydroxy-2-methyl-propanamide, under the trade name of Casodex [1–3]. It belongs to a class of drugs called antiandrogens that includes flutamide (Eulexin) and nilutamide (Nilandron). Andro ...
Biochemistry I (2010) MOED A
... between amino acids and between amino acids and water. d. Secondary structure is formed principally by hydrophobic interactions between amino acids. e. Covalent disulfide bonds are necessary to hold a protein in a rigid conformation. ...
... between amino acids and between amino acids and water. d. Secondary structure is formed principally by hydrophobic interactions between amino acids. e. Covalent disulfide bonds are necessary to hold a protein in a rigid conformation. ...
File
... Not every ligand that binds to a receptor also activates the receptor. The following classes of ligands exist: 1. (Full) agonists are able to activate the receptor and result in a maximal biological response. The natural endogenous ligand with greatest efficacy for a given receptor is by definition ...
... Not every ligand that binds to a receptor also activates the receptor. The following classes of ligands exist: 1. (Full) agonists are able to activate the receptor and result in a maximal biological response. The natural endogenous ligand with greatest efficacy for a given receptor is by definition ...
Effect of Ergot Alkaloids on 3H-Flunitrazepam Binding to Mouse
... in our experimental system. Regarding GABAA re- ceptor related mechanisms, the neurotransmitter site could also be excluded as a possible explanation of the results presented here. Namely, Hruska and Silbergerd reported that ergot alkaloids do not affect 3H-GABA binding to brain GABAA receptors26. T ...
... in our experimental system. Regarding GABAA re- ceptor related mechanisms, the neurotransmitter site could also be excluded as a possible explanation of the results presented here. Namely, Hruska and Silbergerd reported that ergot alkaloids do not affect 3H-GABA binding to brain GABAA receptors26. T ...
Cranberries May Improve Chemotherapy for Ovarian Cancer
... Singh and colleagues believe that the active compounds in the extract are powerful antioxidants called ‘A-type’ proanthocyanidins that are unique to cranberries and not found in other fruits. The researchers add that they do not understand exactly how the cranberry compounds work. However, based on ...
... Singh and colleagues believe that the active compounds in the extract are powerful antioxidants called ‘A-type’ proanthocyanidins that are unique to cranberries and not found in other fruits. The researchers add that they do not understand exactly how the cranberry compounds work. However, based on ...
MA Biotech Thesis Template - Academic Commons
... about the molecules (35). During MRSI studies the concentration of various metabolites can be measured. The current method uses three dimensional 1H MRSI with a volume resolution, referred to as voxel, of 0.24 mm3 or smaller (30). An endorectal MR coil is used to increase the signal to noise ratio a ...
... about the molecules (35). During MRSI studies the concentration of various metabolites can be measured. The current method uses three dimensional 1H MRSI with a volume resolution, referred to as voxel, of 0.24 mm3 or smaller (30). An endorectal MR coil is used to increase the signal to noise ratio a ...
PROSTATE DISEASE CENTER UFPDC_Annual_Report_100410.indd 1
... on the tumor microenvironment, this group works to develop and evaluate novel and targeted treatment strategies with direct clinical applications to cancer management. We are exploring the role of the androgen receptor in prostate cancer progression, and have found that AR S-nitrosylation exerts a n ...
... on the tumor microenvironment, this group works to develop and evaluate novel and targeted treatment strategies with direct clinical applications to cancer management. We are exploring the role of the androgen receptor in prostate cancer progression, and have found that AR S-nitrosylation exerts a n ...
A kalpain enzimrendszer idegrendszeri plaszticitást befolyásoló
... toxin-2 binding site, where VER binds to, are largely overlapping, but not identical (Nau and Wang, 2004). The inverse relationship between the concentration of VER and the potency of TTX, which we found, is in conflict with the observation of some laboratories, but in agreement with those of other ...
... toxin-2 binding site, where VER binds to, are largely overlapping, but not identical (Nau and Wang, 2004). The inverse relationship between the concentration of VER and the potency of TTX, which we found, is in conflict with the observation of some laboratories, but in agreement with those of other ...
patrick_tb_ch05
... Patrick: An Introduction to Medicinal Chemistry 3e which does not activate the receptor. A partial agonist binds but does not activate the receptor to the same extent as a full agonist. An inverse agonist binds to a receptor and stabilises the inactive form of the protein such that the endogenous m ...
... Patrick: An Introduction to Medicinal Chemistry 3e which does not activate the receptor. A partial agonist binds but does not activate the receptor to the same extent as a full agonist. An inverse agonist binds to a receptor and stabilises the inactive form of the protein such that the endogenous m ...
Drug Targets
... • Not all small drug molecules act through specific receptors. • Some small drug molecules interacts non-specifically with lipopolysaccharides, carbohydrates and DNA For example: some group of compound used as narcotics or anaesthetics, the pharmacological effect is mainly related to physical rather ...
... • Not all small drug molecules act through specific receptors. • Some small drug molecules interacts non-specifically with lipopolysaccharides, carbohydrates and DNA For example: some group of compound used as narcotics or anaesthetics, the pharmacological effect is mainly related to physical rather ...
Selective mutation in ATP-binding site reduces affinity of drug to the
... Mutation in protein kinases is very common in cancer and causes constitutive activation of protein kinases resulting in hyper activation of survival pathways. Recent studies suggest that mutation in ATP binding site of kinases confers resistance to the chemotherapy [1]. Thus, understanding how muta ...
... Mutation in protein kinases is very common in cancer and causes constitutive activation of protein kinases resulting in hyper activation of survival pathways. Recent studies suggest that mutation in ATP binding site of kinases confers resistance to the chemotherapy [1]. Thus, understanding how muta ...
Slide ()
... A: The percentage of receptor occupancy resulting from full agonist (present at a single concentration) binding to receptors in the presence of increasing concentrations of a partial agonist. Because the full agonist (filled squares) and the partial agonist (open squares) compete to bind to the same ...
... A: The percentage of receptor occupancy resulting from full agonist (present at a single concentration) binding to receptors in the presence of increasing concentrations of a partial agonist. Because the full agonist (filled squares) and the partial agonist (open squares) compete to bind to the same ...
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.