HIV‐1 Protease Inhibitors as Antiretroviral Agents

Gulnik, Sergei V.; Afonina, Elena; Eissenstat, Michael A.

doi:10.1002/9780470538951.ch23

Cited by 2 publications

(3 citation statements)

References 279 publications

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“…In fact, more virostatics are available for HIV/AIDS than for all other viruses combined. This exciting endeavor has been extensively reviewed [ 13 – 21 ]. In developed countries, HAART considerably changed the course of HIV infection to a controllable and treatable long-term disease.…”

Section: Inhibitors Currently Used In Clinical Practice: Structure Amentioning

confidence: 99%

“…As mentioned above, important characteristics of any drug that are very relevant for its clinical application are toxicity and undesired side effects. The pathogenesis of some side effects has already been satisfactorily explained (e.g., indinavir nephrolithiasis occasionally caused by indinavir), but pathogenetic mechanisms of numerous side effects (e.g., lipodystrophy syndrome, insulin resistance, inhibition of glucose uptake or disturbances of bone metabolism) is still not entirely elucidated [ 23 – 26 ], reviewed in [ 21 ] .…”

Section: Inhibitors Currently Used In Clinical Practice: Structure Amentioning

confidence: 99%

“…Although the mechanism of P450 inhibition by ritonavir (RTV), originally developed as HIV PR inhibitor, is not fully understood, rational design of cytochrome P450 inhibitors has become a very active research field in current pharmaceutical science [ 31 ] (for recent review see [ 32 , 33 ]). Several promising compounds are currently in various stages of clinical testing (e.g., Gilead Sciences’ GS-9350, SPI-452 from Sequoia Pharmaceuticals, TMC-41629 from Tibotec, PF-03716539 from Pfizer, as well as some others, reviewed in [ 21 , 32 ].…”

Section: Inhibitors Currently Used In Clinical Practice: Structure Amentioning

confidence: 99%

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Current and Novel Inhibitors of HIV Protease

Pokorná

Machala

Řezáčová

et al. 2009

Viruses

100

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The design, development and clinical success of HIV protease inhibitors represent one of the most remarkable achievements of molecular medicine. This review describes all nine currently available FDA-approved protease inhibitors, discusses their pharmacokinetic properties, off-target activities, side-effects, and resistance profiles. The compounds in the various stages of clinical development are also introduced, as well as alternative approaches, aiming at other functional domains of HIV PR. The potential of these novel compounds to open new way to the rational drug design of human viruses is critically assessed.

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Section: Inhibitors Currently Used In Clinical Practice: Structure Amentioning

confidence: 99%

Section: Inhibitors Currently Used In Clinical Practice: Structure Amentioning

confidence: 99%

Section: Inhibitors Currently Used In Clinical Practice: Structure Amentioning

confidence: 99%

See 1 more Smart Citation

Current and Novel Inhibitors of HIV Protease

Pokorná

Machala

Řezáčová

et al. 2009

Viruses

100

View full text Add to dashboard Cite

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Protease Inhibitors: A Review

Sapkale¹,

Jadhav²,

Sable³

2013

IND. DRU.

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HIV protease inhibitors were first invented between 1989 and 1994 by researchers working for the pharmaceutical companies of Hoffmann- La Roche Inc. (in Nutley, New Jersey), Abbott Laboratories and Merck & Co., Inc. HIV protease inhibitors are used in the treatment of patients with AIDS and were considered the first breakthrough in over a decade of AIDS research. Currently, there are five HIV protease inhibitors approved by FDA for the treatment of HIV infection. These drugs work at the final stage of viral replication and attempt to prevent HIV from making new copies of itself by interfering with the HIV protease enzyme. As a result, the new copies of HIV are not able to infect new cells. Occurrence of protease along with structural properties, classification of inhibitors like Saquinavir, Ritonavir, Indinavir, Nelfinavir etc and life cycle of virus confirm the role of protease inhibitor. Other parameters like adverse effect, application, structure activity relationship and dose regime shows need of medication for person suffering from HIV virus.

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HIV‐1 Protease Inhibitors as Antiretroviral Agents

Cited by 2 publications

References 279 publications

Current and Novel Inhibitors of HIV Protease

Current and Novel Inhibitors of HIV Protease

Protease Inhibitors: A Review

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