Synopsis of Some Recent Tactical Application of Bioisosteres in
... CH2 in the context of artificial antigens derived by reacting diazonium ions with proteins, a process that derivatized the ortho position of tyrosine, as summarized in Figure 11,2,4,5 The term “bioisostere” was introduced by Harris Friedman in 1950 who defined it as compounds eliciting a similar biolo ...
... CH2 in the context of artificial antigens derived by reacting diazonium ions with proteins, a process that derivatized the ortho position of tyrosine, as summarized in Figure 11,2,4,5 The term “bioisostere” was introduced by Harris Friedman in 1950 who defined it as compounds eliciting a similar biolo ...
Targeting the Bacterial Division Protein FtsZ
... and polymerization into the Z-ring at mid-cell65 (Figure 2B). In the Gram-positive pathogen Streptococcus pneumoniae, MapZ localizes at the division site prior to FtsZ, interacts directly with FtsZ, and guides positioning of the Z-ring66 (Figure 2B). MapZ is a single-passage transmembrane protein th ...
... and polymerization into the Z-ring at mid-cell65 (Figure 2B). In the Gram-positive pathogen Streptococcus pneumoniae, MapZ localizes at the division site prior to FtsZ, interacts directly with FtsZ, and guides positioning of the Z-ring66 (Figure 2B). MapZ is a single-passage transmembrane protein th ...
ABSTRACT Title of Dissertation: ENERGETICS OF DRUG INTERACTIONS
... Professor Frederick P. Schwarz Center for Advanced Research in Biotechnology, University of Maryland Biotechnology Institute Professor Zvi Kelman Molecular and Cell Biology ...
... Professor Frederick P. Schwarz Center for Advanced Research in Biotechnology, University of Maryland Biotechnology Institute Professor Zvi Kelman Molecular and Cell Biology ...
ERGOLINE ALKALOIDS ERGOT ALKALOIDS ÇAVDAR MAHMUZU
... suspected until the end of the seventeenth century, and it was not demonstrated in animals until one century later. • The fungal nature of ergot was recognized in 1711, but the mystery of its development cycle was not elucidated until ...
... suspected until the end of the seventeenth century, and it was not demonstrated in animals until one century later. • The fungal nature of ergot was recognized in 1711, but the mystery of its development cycle was not elucidated until ...
Overcoming of Vincristine Resistance in P388
... agent might affect the function(s) of mi crotubules or alter the transport function of the drugs through the plasma membrane, resulting in an enhanced cytotoxicity of ' This work was supported by Grant-in-Aid for Cancer Research 40101 7 from the Ministry of Education, Science, and Culture. Japan. 2 ...
... agent might affect the function(s) of mi crotubules or alter the transport function of the drugs through the plasma membrane, resulting in an enhanced cytotoxicity of ' This work was supported by Grant-in-Aid for Cancer Research 40101 7 from the Ministry of Education, Science, and Culture. Japan. 2 ...
Advances in and applications of proteasome inhibitors
... was the first natural non-peptidic proteasome inhibitor [19]. Its low nanomolar reactivity toward the proteasomal b5-subunit is dependent on its transformation to clastolactacystin-b-lactone (omuralide) with concomitant loss of N-acetylcysteine (Figure 2) [20]. Nucleophilic attack of Thr1Og on the b ...
... was the first natural non-peptidic proteasome inhibitor [19]. Its low nanomolar reactivity toward the proteasomal b5-subunit is dependent on its transformation to clastolactacystin-b-lactone (omuralide) with concomitant loss of N-acetylcysteine (Figure 2) [20]. Nucleophilic attack of Thr1Og on the b ...
Structure-based design of hyaluronidase inhibitors
... synthesised by all vertebrates, some Streptococci strains, and viruses. Hyaluronan as an essential structural element in the matrix plays an important role for tissue architecture by immobilising specific proteins (aggrecan, versican, neurocan, brevican, CD44 etc.) in desired locations within the bo ...
... synthesised by all vertebrates, some Streptococci strains, and viruses. Hyaluronan as an essential structural element in the matrix plays an important role for tissue architecture by immobilising specific proteins (aggrecan, versican, neurocan, brevican, CD44 etc.) in desired locations within the bo ...
Strategies for in vitro Transporter Testing and
... – A P-gp inhibitor that meets all of the above criteria has not been identified, due to substantial overlap between different transporters (e.g., cyclosporine is also a potent MRP2 and OATP-C inhibitor; quinidine and verapamil also inhibits various organic cation transporters) – Because of the lack ...
... – A P-gp inhibitor that meets all of the above criteria has not been identified, due to substantial overlap between different transporters (e.g., cyclosporine is also a potent MRP2 and OATP-C inhibitor; quinidine and verapamil also inhibits various organic cation transporters) – Because of the lack ...
An Introduction to Medicinal Chemistry
... These are compounds which are classed according to whether they affect a certain target system in the body—usually involving a neurotransmitter, e.g. antihistamines, cholinergics, etc. This classification is a bit more specific than the first, since it is identifying a system with which the drugs in ...
... These are compounds which are classed according to whether they affect a certain target system in the body—usually involving a neurotransmitter, e.g. antihistamines, cholinergics, etc. This classification is a bit more specific than the first, since it is identifying a system with which the drugs in ...
Granska/Öppna
... transfer. P-gp activity is not likely to modify the placental transfer of quetiapine. Higher P-gp protein expression levels were associated with the variant allele 3435T, but no correlation was found between the TPTAUC % of saquinavir and placental P-gp protein expression. The present results indica ...
... transfer. P-gp activity is not likely to modify the placental transfer of quetiapine. Higher P-gp protein expression levels were associated with the variant allele 3435T, but no correlation was found between the TPTAUC % of saquinavir and placental P-gp protein expression. The present results indica ...
Colchicine for pericarditis: hype or hope? REVIEW Massimo Imazio , Antonio Brucato
... meadow saffron has been reported in the first century AD. Colchicum extracts were first described as a treatment for gout in De Materia Medica by Pedanius Dioscorides in the first century AD. Colchicine was first isolated in 1820 by the two French chemists P.S. Pelletier and J. Caventon. Originally ...
... meadow saffron has been reported in the first century AD. Colchicum extracts were first described as a treatment for gout in De Materia Medica by Pedanius Dioscorides in the first century AD. Colchicine was first isolated in 1820 by the two French chemists P.S. Pelletier and J. Caventon. Originally ...
The Effects of Antibiotics and Cancer
... human malignant neoplasms. Patients being treated with MTX often receive many other pharmacologically active compounds concomitantly. Little work has been done to determine what effect, if any, these other agents have on the transport of MTX into tumor cells and ultimately on its antitumor effect in ...
... human malignant neoplasms. Patients being treated with MTX often receive many other pharmacologically active compounds concomitantly. Little work has been done to determine what effect, if any, these other agents have on the transport of MTX into tumor cells and ultimately on its antitumor effect in ...
Full-Text - Academic Journals
... water-soluble conjugate and excreted through urine. Malaria parasite does not use this pathway for heme metabolism. In the food vacuole, heme is changed into hemozoin, a malaria pigment, which is a dimer of heme units linked through an iron-carboxylate bond (Pagola et al., 2000). Digestion of hemogl ...
... water-soluble conjugate and excreted through urine. Malaria parasite does not use this pathway for heme metabolism. In the food vacuole, heme is changed into hemozoin, a malaria pigment, which is a dimer of heme units linked through an iron-carboxylate bond (Pagola et al., 2000). Digestion of hemogl ...
Cox-2-Selective Inhibitors: The New Super Aspirins
... Nonsteroidal anti-inflammatory drugs (NSAIDs) such as aspirin or ibuprofen are commonly used for the occasional headache or fever or to reduce soreness and inflammation resulting from work or exercise. However, many individuals who have rheumatoid arthritis and osteoarthritis depend on these drugs t ...
... Nonsteroidal anti-inflammatory drugs (NSAIDs) such as aspirin or ibuprofen are commonly used for the occasional headache or fever or to reduce soreness and inflammation resulting from work or exercise. However, many individuals who have rheumatoid arthritis and osteoarthritis depend on these drugs t ...
Targeting proteases: successes, failures and future prospects
... dose per day, although they are only efficacious in a limited number of people and have some side effects, including coughing and angioedema19,23. When the crystal structure of ACE was eventually solved, it revealed that the enzyme is composed of two highly homologous but not identical domains with ...
... dose per day, although they are only efficacious in a limited number of people and have some side effects, including coughing and angioedema19,23. When the crystal structure of ACE was eventually solved, it revealed that the enzyme is composed of two highly homologous but not identical domains with ...
DRUG NAME - BC Cancer Agency
... Vincristine is a naturally occurring vinca alkaloid. Vinca alkaloids act as antimicrotubule agents that block mitosis by ...
... Vincristine is a naturally occurring vinca alkaloid. Vinca alkaloids act as antimicrotubule agents that block mitosis by ...
THESPESIA POPULNEA LINN. Review Article MOHINI A. PHANSE*,
... investigation. The ethanolic extract of T. populnea was administered orally in three doses (100, 200 and 400 mg/kg) for 7 successive days to different groups of young and aged mice and the learning and memory parameters were assessed using elevated plus maze and passive avoidance apparatus. Plant ex ...
... investigation. The ethanolic extract of T. populnea was administered orally in three doses (100, 200 and 400 mg/kg) for 7 successive days to different groups of young and aged mice and the learning and memory parameters were assessed using elevated plus maze and passive avoidance apparatus. Plant ex ...
Aldehyde Oxidase Activity in Donor
... activity and creating a custom high-activity pooled lot of cryopreserved hepatocytes are advised to minimize underpredictions of clearance. ...
... activity and creating a custom high-activity pooled lot of cryopreserved hepatocytes are advised to minimize underpredictions of clearance. ...
C 5 P450
... inhibitors of p38α kinase (p38α MAPK or p38α kinase) and simultaneous structure elucidation by high resolution mass spectrometry (HR-MS) (20). p38α kinase is an important drug target in contemporary drug discovery because it plays a central role in inflammatory cellular signaling processes (21). Sev ...
... inhibitors of p38α kinase (p38α MAPK or p38α kinase) and simultaneous structure elucidation by high resolution mass spectrometry (HR-MS) (20). p38α kinase is an important drug target in contemporary drug discovery because it plays a central role in inflammatory cellular signaling processes (21). Sev ...
Actions of bufalin and cinobufotalin, two bufadienolides respectively
... recently cinobufotalin has been reported to be less active than ouabain on this enzyme [8]. Ouabain is not the most toxic of the cardiac glycosides, but many studies have related activity of other molecules to that of ouabain, especially in relation to inhibition of Na+/K+-ATPase and the inhibition ...
... recently cinobufotalin has been reported to be less active than ouabain on this enzyme [8]. Ouabain is not the most toxic of the cardiac glycosides, but many studies have related activity of other molecules to that of ouabain, especially in relation to inhibition of Na+/K+-ATPase and the inhibition ...
19 Improving the Oral Absorption of S-SEDDS Formulations
... SEDDS and S-SEDDS are self-emulsifying formulations of poorly soluble drugs that contain both a surfactant and lipid, along with a co-solvent, and they are usually formulated in gelatin capsules. Dilution of SEDDS or S-SEDDS formulations with water results in the generation of a microemulsion with a ...
... SEDDS and S-SEDDS are self-emulsifying formulations of poorly soluble drugs that contain both a surfactant and lipid, along with a co-solvent, and they are usually formulated in gelatin capsules. Dilution of SEDDS or S-SEDDS formulations with water results in the generation of a microemulsion with a ...
ANTIFUNGAL AGENTS - Mount Sinai Hospital
... Azoles inhibits cytochrome P450 enzymes in the fungal cell 5FC converts to 5FU, incorporated into RNA, abnormal proteins Griseofulvin binds microtubule proteins, inhibit cell wall synthesis Terbinafine is an ergosterol inhibitor useful for systemic mycosis ...
... Azoles inhibits cytochrome P450 enzymes in the fungal cell 5FC converts to 5FU, incorporated into RNA, abnormal proteins Griseofulvin binds microtubule proteins, inhibit cell wall synthesis Terbinafine is an ergosterol inhibitor useful for systemic mycosis ...
Reaction Phenotyping Methods using Recombinant Enzymes and
... • Mammalian cells – Co-expressed with P450 OR and in some cases with b5 – Reaction phenotyping (EM), DDI, mechanistic studies – Can be useful for studying highly stable compounds (more active than HLM) – Requires RAF or ISEF for comparing to HLM activity ...
... • Mammalian cells – Co-expressed with P450 OR and in some cases with b5 – Reaction phenotyping (EM), DDI, mechanistic studies – Can be useful for studying highly stable compounds (more active than HLM) – Requires RAF or ISEF for comparing to HLM activity ...
The impact of penicillin on therapeutic outcomes
... cancer,autoͲimmunediseases,newvaccines,etc.aredependentonthesamemicrobialstrain selectionandlargeͲscalechemicalengineeringmethodsthatwerefirstpioneeredforpenicillin. • ThedevelopmentofpenicillinduringWorldWarIImarkedafundamentalchangeinthe p p g g relationshipb ...
... cancer,autoͲimmunediseases,newvaccines,etc.aredependentonthesamemicrobialstrain selectionandlargeͲscalechemicalengineeringmethodsthatwerefirstpioneeredforpenicillin. • ThedevelopmentofpenicillinduringWorldWarIImarkedafundamentalchangeinthe p p g g relationshipb ...