Druq design - Essay Example

Comments (0) Cite this document
The human immunodeficiency virus (HIV) was first discovered in 1985.HIV is most commonly transmitted by sexual contact and needle-sharing due to the exchange of body fluids like blood and semen. The virus damages the body’s immune system resulting in AIDS (acquired immune…
Download full paperFile format: .doc, available for editing
GRAB THE BEST PAPER93.4% of users find it useful
Druq design
Read TextPreview

Extract of sample "Druq design"

Drug Design for HIV Background about HIV The human immunodeficiency virus (HIV) was first discovered in 1985.HIV is most commonly transmitted by sexual contact and needle-sharing due to the exchange of body fluids like blood and semen. The virus damages the body’s immune system resulting in AIDS (acquired immune deficiency syndrome). A worldwide epidemic, 39.5 million individuals were infected with HIV/AIDS in 2006. In the same year, 2.9 million deaths were attributed to AIDS (Cichocki, 2008).
HIV is a retrovirus, which store their genetic information as RNA instead of DNA. HIV enters human immune system CD4 cells through specific receptors in its viral coat. Inside the cell, the HIV reverse transcriptase converts the viral RNA into DNA; this DNA is transported into the cell nucleus where it is inserted into the human genome by the HIV integrase enzyme. The HIV DNA may lie dormant, but is later expressed for the synthesis of new HIV proteins and enzymes. The HIV protease is active at this stage of the life cycle where its role is to cut long protein strands to form viral cores.
The development of the pathogenic effects of HIV is characterized by the interaction between viral and host factors. A broad spectrum of antiviral strategies was developed for each step of the viral replication cycle. Every stage in the life cycle, and every gene product of HIV is a potential target. Host proteins that are recognized to have an essential role in the viral life cycle are also targets of HIV therapy (Nielsen, Pedersen, & Kjems, 2005). As of 2007, more than 20 anti-HIV drugs have been approved (De Clerq, 2007). The drugs block the enzyme activity of any of the enzyme that HIV needs to replicate inside host cells: reverse transcriptase, protease, fusion inhibitors, and lately integrase inhibitors. The norm is to utilize highly active antiretroviral therapy (HAART), which combines two or three drugs to overcome the development of drug resistant targets. Nevertheless, multi-drug resistant HIV continue to develop due to the high viral mutation rates.
Choice of Drug Target
Integrase is the chosen target for the drug to be designed for HIV treatment; it facilitates the insertion of the double-stranded DNA copy of the HIV RNA genome into the host genome, an absolute requirement for viral replication (LaFemina, et al., 1992). Integration of the HIV DNA requires 3 processing of the final two bases of the viral DNA long terminal repeat (LTR), and DNA strand transfer activity. HIV integrase was found to be composed of several multimers with functional domains sufficient for 3 processing and DNA strand transfer (Engelman, Bushman, & Craigie, 1993). The integrase positions the two 3-hydroxyls of its LTRs for nucleophilic attack on the phosphodiester bonds and insertion into the genomic DNA. Gln 148, found in the active site of integrase, was found to have a pivotal role in assembly, strand transfer catalysis, and inhibitor binding (Dicker, et al., 2007).
Proposed Drug Designs
Integrase is an ideal target because it has no known homolog in humans, and therefore strategies can be designed that solely act on it. The designs, which can target the HIV integrase, should consider the known mechanisms for insertion of the viral DNA into the host genome. The catalytic function of integrase can be blocked by inactivating or introducing conformational changes to its binding sites within the viral DNA. Alternatively, the active site of the enzyme or its binding domain can be altered by introducing changes into its structure (Nielsen, Pedersen, & Kjems, 2005). Inhibitory molecules can be oligonucleotides, dinucleotides, and chemical agents (Nair, 2002). The integrase binding site in the LTR region contains the 5-GGAAGGG-3, which can be targeted by oligonucleotide conjugates that complex with the viral DNA and block the catalytic functions of the integrase (Nair, 2002). Some nucleotides also inhibit the integrase by interacting with the catalytic domain.
To determine which compound can work best in inactivating integrase, it is necessary to understand the molecular structure in relation to the catalytic activity of the integrase enzyme. From this, compounds with known molecular structure, or even natural products, can be screened and evaluated in the presence of the integrase, under in vitro conditions. It is only necessary to determine the loss of activity of integrase through spectrophotometric means or by the formation of precipitates (in the case of complex formation). Biochemical studies need to be validated by in vivo experiments after suitable compounds have been selected and characterized.
Cichocki, M 2008, ‘HIV statistics - AIDS data - estimates of the worlds HIV epidemic’, Retrieved March 3, 2009, from worldstats.htm.
De Clerq, E 2007, ‘The design of drugs for HIV and HCV’, Nature Reviews, vol. 6, pp. 1001-1018.
Dicker, I, Samanta, H, Li, Z, Hong, Y, Tian, Y, Banville, J, Remillard, R, Walker, MA, Langley, DR & Krystal, M 2007, ‘Changes to the HIV long terminal repeat and to HIV integrase differentially impact HIV integrase assembly, activity, and the binding of strand transfer inhibitors’, Journal of Biological Chemistry, vol.282, no. 43, pp. 31186-31196.
Engelman, A, Bushman, F & Craigie, R 1993, ‘Identification of discrete functional domains of HIV-1 integrase and their organization within an active multimeric complex’, EMBO Journal, vol. 12, no. 8, pp. 3269-3275.
Havlir, D 2008, ‘HIV integrase inhibitors- out of the pipeline and intothe clinic’, New Engalnd Journal of Medicine, vol. 359, no. 4, pp. 416- 418.
LaFemina, R, Schneider, C, Robbins, H, Callahan, P, LeGrow, K, Roth, E, Schleif, WA & Emini, EA, 1992, ‘Requirement of active human immunodeficiency virus type 1 integrase enzyme for productive infection of human T-lymphoid cells’, Journal of Virology, vol. 66, no. 12, pp. 7414-7419.
Nair, V 2002, ‘HIV integrase as a target for antiviral chemotherapy’, Review of Medical Virology, vol. 12, pp. 179-203.
Nielsen, M, Pedersen, F & Kjems, J 2005, ‘Molecular strategies to inhibit HIV-1 replication’, Retrovirology, vol.2, pp. 10. Read More
Cite this document
  • APA
  • MLA
(“Druq design Essay Example | Topics and Well Written Essays - 500 words”, n.d.)
Druq design Essay Example | Topics and Well Written Essays - 500 words. Retrieved from
(Druq Design Essay Example | Topics and Well Written Essays - 500 Words)
Druq Design Essay Example | Topics and Well Written Essays - 500 Words.
“Druq Design Essay Example | Topics and Well Written Essays - 500 Words”, n.d.
  • Cited: 0 times
Comments (0)
Click to create a comment or rate a document


Design program. It is worth noting that while there is some certainty to both of these sentiments, non-selling HR experts can design actual sales training programs. Designing sales training program entails more than inquiring using standard questions about flaws in the sales team. The role of “internal advisor” will have to be assumed by the HR manager. Furthermore, coordination with the sales management team will be essential to cultivate a relevant and nourishing sales training program. Finally, any training program should present the skills required to be fruitful in a particular job occupation. The difficulty of the sales job, however, can make the skills characterisation more problematic....
4 Pages(1000 words)Essay


...THE CONE CALORIMETER EXPERIMENT The Cone Calorimeter Experiment Fire testing plays a pivotal role in the development of new superior materials as well as enabling fire research engineers study the different effects of fire on materials used for building and construction. The cone calorimeter is one of the most important equipment for performing fire test on the bench. The equipment is used for measuring and testing the heat release rate of a given sample. The instrument has been adapted by the international standard organization (ISO) and other standardizations bodies. It is important to study and understand the fire performance of different PVC materials as they are constituent of the electrical wiring system which may result... CONE...
8 Pages(2000 words)Essay


...and bendable polymer compound - fine particles of polyvinyl chloride (PVC) suspended in plasticizer (DeVoto 1997). Among the advantages of working with this material is a great number of colors and shades provided by the manufacturers. Furthermore, these colors can be blended just like those of painters, to create new, personally designed shades and patterns. There has been developed a great number of special techniques for working with polymer clay, among which some have been inherited from glasswork, textile arts, and sculpture. Such practices as caneworking, marbling, millefiori and others give artists plenty of opportunities to create endless variations of color combinations and even textures. In addition, this kind...
4 Pages(1000 words)Essay


...Academia-Research Kanwal Tariq 6010 Order ID: 753398 Assignment: Education- “Design” Education is a continuous learning process, including the involvement of both the Teacher and Students. Its is very essential for a teacher to have full command on his subject or topic, so that he can explain to the students well and in return help them to understand the lesson. Teacher must have grip on the lesson, should have previously planned lecture that has to deliver the students. During the lesson/lecture the full involvement of not only teacher but also of student is required for the good results. Teacher should ask some questions of previous knowledge from the students in order to judge their interest and involvement. The...
2 Pages(500 words)Assignment


...Design Design Question The learning units of this include utilizing MS Word to create questionnaire or survey, overview of Adobe Acrobat Professional Software, example outcomes and adding interaction (Sypowicz, 2010). The first unit incorporates sections such as exchange introductions, course documents, choices for creating a questionnaire and creating a document. The second unit incorporates sections such as review Adobe Acrobat and Create a sample form. The third unit incorporates sections such as successes and failures, as well as review and repeat steps. Finally, the fourth unit incorporates sections such as review, develop more options, implement, evaluate, as well as additional training. It will be a two-day program whereby... members...
2 Pages(500 words)Assignment

Creational Design Patterns in Detailed Design and Design Logic Patterns

...CREATIONAL DESIGN PATTERNS IN DETAILED DESIGN AND DESIGN LOGIC PATTERNS Software Design Patterns Factory Definition The factory pattern is a creational design software pattern that provides a means to encapsulate a group of individual factories or units sharing common characteristics but without specifying actual classes. A factory is location of real class in the code where objects are constructed. Problem Abstract factory class declares only interface for creating products whereas it is the task of concrete product class to actually create products. This might cause concrete factory to override existing factory methods. Benefit The pattern may...
4 Pages(1000 words)Essay

Causal-Comparative Research Design & Descriptive Design

...1129039 - CAUSAL-COMPARATIVE RESEARCH DESIGN & DESCRIPTIVE DESIGN Casual-comparative research design and descriptive design are sometimes used interchangeably due to the similarities that they have but in actual fact, the two are noted not to be the same thing. The confusion arises because both casual-comparative research design and descriptive design are used to describe conditions that have already taken place (quote). Going close up with the two however, quote (year) explained that casual-comparative research seeks to determine reasons or causes that back the occurrence of existing conditions. In most of the case therefore, there is an identified pre-existing difference between a group of individuals and any subject group... that is of...
1 Pages(250 words)Research Paper


...$ 15,000 Travel and accommodation during field work sessions $ 2,000 Approximate Total $ 45,200 Experience and Delivery Major stakeholders involved within the above labor mobility training program are organizational employees and the management. However, the plan has given an allowance for modification to embrace legal personnel whose mandate would be to ensure that the training is moderated as per the required standards. The training is also designed on a computer based platform, and most notes shall be issued in the form of slides and handouts, but main themes of studies shall be...
2 Pages(500 words)Assignment


...NATUGO Natugo Natugo is a company that provides products that satisfy ostentation desires of humans through production of in-shower moisturizer. Sales pitch of the company is production of moisturizer that is environmentally friendly and free of chemicals (Hartl, 2011). Through their production procedures, products of the company take resemblance to source of the raw material that constitutes largest proportion of the main product (Gibbs, 2010). Design of bottles, therefore, takes resemblance to the raw material thus offering the clients a natural touch, not only in consumption of the end product, but on selection of the product too (Gabriel, 2008). There are three main designs of the bottle, that is,...
2 Pages(500 words)Essay


...Personal Report Personal Report The first thing to consider when handling the design project is to think about the areas that will enhance creativity (Pile, 2009). Additionally, the kind of spaces that people prefer and what is lacking in such spaces must also be taken into consideration. An assessment of various sources has made it possible to formulate various questions that will be useful in the research. Among the questions that are important include: what needs to be accomplish in the research; why the research is important; the values that are critical to the conduct of research; the contribution of the research to the field and to the society; the value of the research to the researcher; and how the research will...
12 Pages(3000 words)Essay
sponsored ads
We use cookies to create the best experience for you. Keep on browsing if you are OK with that, or find out how to manage cookies.

Let us find you another Essay on topic Druq design for FREE!

Contact Us