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Functional analyses and molecular modeling of two c-Kit mutations
... Figure 2 Molecular modeling of KIT/T670I mutant. The procedure applied in this work has been described in detail in our previous work (Pricl et al., 2005). Accordingly, only a brief outline of the method is reported. All simulations were carried out using the Sander modulus of AMBER 7.0 (Case et al. ...
... Figure 2 Molecular modeling of KIT/T670I mutant. The procedure applied in this work has been described in detail in our previous work (Pricl et al., 2005). Accordingly, only a brief outline of the method is reported. All simulations were carried out using the Sander modulus of AMBER 7.0 (Case et al. ...
Cardiac toxicity hERG
... for their ability to displace the radiolabeled ligand from the hERG channel. This assay is high throughput and low cost. It is suitable for primary screening to identify compounds that have a high affinity for the hERG channel. However, the binding assay has inherent limitations. It is not a functio ...
... for their ability to displace the radiolabeled ligand from the hERG channel. This assay is high throughput and low cost. It is suitable for primary screening to identify compounds that have a high affinity for the hERG channel. However, the binding assay has inherent limitations. It is not a functio ...
Full Text - Molecular Cancer Research
... Therapy The microenvironmental conditions discussed above present unique barriers to specific cancer therapy modalities. For example, hypoxia has long been known to inhibit effective radiation killing in vitro (35). Oxygen is a potent radiosensitizer, with well-oxygenated cells requiring one-third o ...
... Therapy The microenvironmental conditions discussed above present unique barriers to specific cancer therapy modalities. For example, hypoxia has long been known to inhibit effective radiation killing in vitro (35). Oxygen is a potent radiosensitizer, with well-oxygenated cells requiring one-third o ...
Interactions between endothelin-1 and the renin–angiotensin
... jun in the regulatory region of the preproendothelin-1 (ppET-1) gene raised the possibility of its transcriptional regulation by angiotensin II (Ang II). This was confirmed by the finding that stimulation with Ang II of cultured vascular smooth muscle cells (VSMCs) and endothelial cells (ECs) induce ...
... jun in the regulatory region of the preproendothelin-1 (ppET-1) gene raised the possibility of its transcriptional regulation by angiotensin II (Ang II). This was confirmed by the finding that stimulation with Ang II of cultured vascular smooth muscle cells (VSMCs) and endothelial cells (ECs) induce ...
View Prescribing Details
... Hydrochloride) binds selectively and competitively to postsynaptic Alpha1-adrenoreceptors, in particular to subtypes alpha1A and alpha1D. It brings about relaxation of Prostatic and urethral smooth muscle. Tamsulosin increases the maximum urinary flow rate. It relieves obstruction by relaxing smooth ...
... Hydrochloride) binds selectively and competitively to postsynaptic Alpha1-adrenoreceptors, in particular to subtypes alpha1A and alpha1D. It brings about relaxation of Prostatic and urethral smooth muscle. Tamsulosin increases the maximum urinary flow rate. It relieves obstruction by relaxing smooth ...
Cyclodextrins in peptide and protein delivery
... Since safety is a primary concern when considering new excipients intended for use in pharmaceutical formulations, the toxicological issues together with their biological fates must be thoroughly investigated prior to their practical use. The safety status of pharmaceutically useful CDs, including p ...
... Since safety is a primary concern when considering new excipients intended for use in pharmaceutical formulations, the toxicological issues together with their biological fates must be thoroughly investigated prior to their practical use. The safety status of pharmaceutically useful CDs, including p ...
Preclinical Screening and Evaluation of Agents
... screen. The ratio t/c (fractional growth of treated tumor as compared with control) is commonly ...
... screen. The ratio t/c (fractional growth of treated tumor as compared with control) is commonly ...
Salvinorin A, an Active Component of the Hallucinogenic Sage
... protein. Because both methods seemed to yield equivalent results, further studies were performed with Gq-i5. Table 3 shows representative EC50 and Emax values for a variety of KOR agonists using Gq-i5. In these studies, salvinorin A was more potent than any other of the tested KOR agonists (Table 3) ...
... protein. Because both methods seemed to yield equivalent results, further studies were performed with Gq-i5. Table 3 shows representative EC50 and Emax values for a variety of KOR agonists using Gq-i5. In these studies, salvinorin A was more potent than any other of the tested KOR agonists (Table 3) ...
HTA Diagnosis, management and screening of early localised prostate cancer Sara Selley
... he incidence of prostate cancer is rising worldwide, caused mainly by demographic factors, particularly the increasingly elderly population and, more importantly, the increasing number of cases identified following prostate specific antigen (PSA) testing. It is commonly quoted that many more men die ...
... he incidence of prostate cancer is rising worldwide, caused mainly by demographic factors, particularly the increasingly elderly population and, more importantly, the increasing number of cases identified following prostate specific antigen (PSA) testing. It is commonly quoted that many more men die ...
Bioidentical Hormone Therapy
... and progestogens are available in a wide variety of FDAapproved and non–FDA-approved formulations for the treatment of perimenopausal and menopausal symptoms. BIOIDENTICAL HT The term CJPJEFOUJDBMIPSNPOF does not have a standardized definition and thus often confuses patients and practitioners. Wom ...
... and progestogens are available in a wide variety of FDAapproved and non–FDA-approved formulations for the treatment of perimenopausal and menopausal symptoms. BIOIDENTICAL HT The term CJPJEFOUJDBMIPSNPOF does not have a standardized definition and thus often confuses patients and practitioners. Wom ...
mRNA Transcript Diversity Creates New Opportunities for
... CETP inhibitors are currently under development. The first drug candidate acting as a CETP inhibitor (torcetrapib) was withdrawn in late phase III trials because of an unexpected rise in coronary artery disease incidence (Barter et al., 2007), suggesting a complex relationship between HDL, cardiovas ...
... CETP inhibitors are currently under development. The first drug candidate acting as a CETP inhibitor (torcetrapib) was withdrawn in late phase III trials because of an unexpected rise in coronary artery disease incidence (Barter et al., 2007), suggesting a complex relationship between HDL, cardiovas ...
Cyclophosphamide Modulates Rat Hepatic Cytochrome P450 2C11
... mg/kg (single i.p. injection) acrolein decreased testosterone 2a-hydroxylase activity by ~50% and increased steroid 5a-reductase ac tivity by 1.5-fold in isolated liver microsomes. This corresponds to a feminization ratio (defined as the ratio of microsomal steroid 5areductase activity to microsomal ...
... mg/kg (single i.p. injection) acrolein decreased testosterone 2a-hydroxylase activity by ~50% and increased steroid 5a-reductase ac tivity by 1.5-fold in isolated liver microsomes. This corresponds to a feminization ratio (defined as the ratio of microsomal steroid 5areductase activity to microsomal ...
Vascular Targeting 2004
... tissue vessels (e.g., increased proliferation and fragility, and up-regulated proteins). VTAs can kill indirectly the tumor cells that are resistant to conventional antiproliferative cancer therapies, i.e., cells in areas distant from blood vessels where drug penetration is poor, and hypoxia can lea ...
... tissue vessels (e.g., increased proliferation and fragility, and up-regulated proteins). VTAs can kill indirectly the tumor cells that are resistant to conventional antiproliferative cancer therapies, i.e., cells in areas distant from blood vessels where drug penetration is poor, and hypoxia can lea ...
Document
... EC), which interacts with the neuropilin-1 (NRP-1) receptor (17, 19, 20). NRP-1 plays a key role in tumor angiogenesis and can also be engaged by VEGFs that contain an RXXR sequence, also dubbed the C-terminal rule (CendR) motif (18, 21). The transcytosis pathway is not only distinct from other endo ...
... EC), which interacts with the neuropilin-1 (NRP-1) receptor (17, 19, 20). NRP-1 plays a key role in tumor angiogenesis and can also be engaged by VEGFs that contain an RXXR sequence, also dubbed the C-terminal rule (CendR) motif (18, 21). The transcytosis pathway is not only distinct from other endo ...
Serum Creatinine Measuring serum creatinine is a useful and
... The only important pathological condition that causes a significant increase in the serum creatinine level is damage to a large number of nephrons. Unlike the BUN, the serum creatinine level is not affected by hepatic protein metabolism. Tests to measure serum creatinine, urine creatinine, and crea ...
... The only important pathological condition that causes a significant increase in the serum creatinine level is damage to a large number of nephrons. Unlike the BUN, the serum creatinine level is not affected by hepatic protein metabolism. Tests to measure serum creatinine, urine creatinine, and crea ...
affinity biosensor for antitumoral drugs determination
... The DNA- modified electrode can be used for electrochemical determination in serum samples of patients with cancer undergoing treatment with carboplatin. The pharmacokinetics corresponding to the administration of the drug can be followed by electrochemical methods and the detection limit in serum s ...
... The DNA- modified electrode can be used for electrochemical determination in serum samples of patients with cancer undergoing treatment with carboplatin. The pharmacokinetics corresponding to the administration of the drug can be followed by electrochemical methods and the detection limit in serum s ...
Introduction to Fragment-Based Drug Discovery
... smaller compounds should in theory be higher than for larger compounds. This is because as molecules grow larger they grow more complex, and each additional moiety has an increasing probability of interfering with binding. This was demonstrated computationally a decade ago [13], but can be understoo ...
... smaller compounds should in theory be higher than for larger compounds. This is because as molecules grow larger they grow more complex, and each additional moiety has an increasing probability of interfering with binding. This was demonstrated computationally a decade ago [13], but can be understoo ...
Vascular Targeting Agents as Cancer Therapeutics
... tissue vessels (e.g., increased proliferation and fragility, and up-regulated proteins). VTAs can kill indirectly the tumor cells that are resistant to conventional antiproliferative cancer therapies, i.e., cells in areas distant from blood vessels where drug penetration is poor, and hypoxia can lea ...
... tissue vessels (e.g., increased proliferation and fragility, and up-regulated proteins). VTAs can kill indirectly the tumor cells that are resistant to conventional antiproliferative cancer therapies, i.e., cells in areas distant from blood vessels where drug penetration is poor, and hypoxia can lea ...
position statement - Cancer Council Australia
... However the results of secondary end-point analyses support the hypothesis that supplemental selenium may reduce the incidence of cancers at other sites, including prostate and colon-rectum.6, 7 This trial showed a significant protective effect of selenium supplementation on the incidence of prostat ...
... However the results of secondary end-point analyses support the hypothesis that supplemental selenium may reduce the incidence of cancers at other sites, including prostate and colon-rectum.6, 7 This trial showed a significant protective effect of selenium supplementation on the incidence of prostat ...
Schizophrenia and the supersensitive synapse
... disease. (This is a sweeping observation that holds true.) For example, the selective removal or knockout of the metabotropic glutamate-2 or -3 receptor genes leads to animal behavior that is supersensitive to dopamine-like stimulant drugs, accompanied by a marked elevation in the number of D2 recep ...
... disease. (This is a sweeping observation that holds true.) For example, the selective removal or knockout of the metabotropic glutamate-2 or -3 receptor genes leads to animal behavior that is supersensitive to dopamine-like stimulant drugs, accompanied by a marked elevation in the number of D2 recep ...
see p. Rx1 - Viktor`s Notes for the Neurosurgery Resident
... 4. Skeletal muscle relaxant (by increasing presynaptic inhibition in spinal cord) - relax muscle spasticity. ...
... 4. Skeletal muscle relaxant (by increasing presynaptic inhibition in spinal cord) - relax muscle spasticity. ...
Prostate cancer From diagnosis to managing advanced disease
... for men in the European Union and the USA, with 323,790 and 186,320 new cases, respectively and 71,027 and 28,660 deaths in 2008 1. From 28-30 June 2012, a multidisciplinary faculty of almost 50 urologists, radiologists, radiotherapists, medical oncologists and nuclear medicine specialists gathered ...
... for men in the European Union and the USA, with 323,790 and 186,320 new cases, respectively and 71,027 and 28,660 deaths in 2008 1. From 28-30 June 2012, a multidisciplinary faculty of almost 50 urologists, radiologists, radiotherapists, medical oncologists and nuclear medicine specialists gathered ...
Pharmacologic insights into the future of trastuzumab
... (data on file, F. Hoffmann-La Roche Ltd). A minimum available data also indicate that higher doses of trastuserum trough concentration of 10 ug/ml was considered zumab are likely to be well tolerated and could be necessary for a therapeutic response in humans and was administered at longer intervals ...
... (data on file, F. Hoffmann-La Roche Ltd). A minimum available data also indicate that higher doses of trastuserum trough concentration of 10 ug/ml was considered zumab are likely to be well tolerated and could be necessary for a therapeutic response in humans and was administered at longer intervals ...
Management of crizotinib resistance in lung cancer using traditional
... Lung cancer is the major cause of cancer deaths in the world. Lung cancer is broadly categorized into two main types based upon their histology, which are non-small cell lung cancer (NSCLC) and small cell lung cancer (SCLC) [1]. The most common forms of NSCLC are adenocarcinoma (ADC) and squamous ce ...
... Lung cancer is the major cause of cancer deaths in the world. Lung cancer is broadly categorized into two main types based upon their histology, which are non-small cell lung cancer (NSCLC) and small cell lung cancer (SCLC) [1]. The most common forms of NSCLC are adenocarcinoma (ADC) and squamous ce ...
Vinca Alkaloids
... vinca alkaloid, vinflunine that is currently approved in Europe for medicinal treatment.[5,6] ...
... vinca alkaloid, vinflunine that is currently approved in Europe for medicinal treatment.[5,6] ...
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.