From Proteopedia

proteopedia linkproteopedia link

This Sandbox is Reserved from 30/01/2013, through 30/12/2013 for use in the course "Biochemistry II" taught by Hannah Tims at the Messiah College. This reservation includes Sandbox Reserved 686 through Sandbox Reserved 700.

To get started: Click the edit this page tab at the top. Save the page after each step, then edit it again. Click the 3D button (when editing, above the wikitext box) to insert Jmol. show the Scene authoring tools, create a molecular scene, and save it. Copy the green link into the page. Add a description of your scene. Use the buttons above the wikitext box for bold, italics, links, headlines, etc. More help: Help:Editing

Contents 1 Complera: Emtricitabine/rilpivirine/tenofovir 1.1 Rilpivirine (RPV) 1.2 Tenofovir (TFV) 1.3 Emtricitabine (ECT)

Complera: Emtricitabine/rilpivirine/tenofovir

• Marketed by: Gilead Sciences and Janssen Therapeutics
• Major Indication: HIV infection
• Drug Class: Combination of nucleoside/tide reverse transcriptase inhibitor and nonnucleoside reverse transcriptase inhibitor
• Date of FDA Approval: August 2011

Upon infection, HIV binds to the CD4 receptor in a helper T cell or other CD4-presenting lymphocyte. The viral envelope is then fused with the cellular membrane allowing intracellular release of viral particles. The utilization of several enzymes helps to solidify the virus’s hold on the cell. HIV reverse transcriptase (RT) works to convert the viral single-stranded RNA (ssRNA) into DNA. HIV integrase then helps to incorporate the newly reverse transcribed DNA into the cellular genome. (Voet et al. 2008)

Rilpivirine (RPV)

spinqualitylabelsall models Crystal structure of HIV-1 reverse transcriptase in complex with rilpivirine Show:Asymmetric Unit Biological Assembly Drag the structure with the mouse to rotate   Export Animated Image

RPV in the In red are the binding pocket residues p66 (Leu-100, Lys-101, Lys-103, Val-106, Thr-107, Val-108, Val-179, Tyr-181, Tyr-188, Val-189, Gly-190, Phe-227, Trp-229, Leu- 234, and Tyr-318) and p51(Glu-138). Singh et al.

Tenofovir (TFV)

spinqualitylabelsall models HIV-1 reverse transcriptase crosslinked to tenofovir terminated template-primer Show:Asymmetric Unit Biological Assembly Drag the structure with the mouse to rotate   Export Animated Image

Reverse Transcriptase:

Emtricitabine (ECT)

Image:Emtricitabine3.png

spinqualitylabelsall models Emtricitabine is an analog of cytidine and functions as antiretroviral drug (NRTI) for the treatment of HIV Show:Asymmetric Unit Biological Assembly Drag the structure with the mouse to rotate   Export Animated Image