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Record W2092806574 · doi:10.2174/1381612043384501

Effects of HIV-1 Entry Inhibitors in Combination

2004· review· en· W2092806574 on OpenAlexaff
Cécile Tremblay

Bibliographic record

VenueCurrent Pharmaceutical Design · 2004
Typereview
Languageen
FieldMedicine
TopicHIV/AIDS drug development and treatment
Canadian institutionsHôtel-Dieu de Montréal
Fundersnot available
KeywordsAntagonismDrugPharmacologyEnfuvirtideCCR5 receptor antagonistComputational biologyPharmacokineticsHuman immunodeficiency virus (HIV)BiologyChemokine receptorReceptorVirologyImmunologyBiochemistryChemokine

Abstract

fetched live from OpenAlex

Inhibiting the HIV-1 entry process offer a new therapeutic target and the hope to potentialize our current treatments against wild-type or drug-resistant viruses. Several inhibitors of CD4, co-receptor CCR5 or CXCR4 and fusion are at various levels of clinical development. How best to use this class of drugs in our therapeutic arsenal remains to be defined. It is likely that these compounds will not be used as monotherapy. Therefore, it is important to evaluate how these drugs will interact among themselves as well as with antiretrovirals from other classes. Drug interactions can range from synergy to antagonism depending on factors including binding affinity, drug concentrations, and pharmacokinetics. In the case of entry inhibitors, one must also consider that the entry of HIV-1 into the cell is a multi-step process that involve cumulative events which are interdependent. Furthermore, polymorphism both in the coreceptors and in gp120, the density of coreceptors, and the binding site of the drug may also affect efficacy. Therefore it is difficult to predict how blocking one step of the process will affect the subsequent one without carefully studying interactions of each potential combination in an in vitro system. So far, studies of interactions between fusion inhibitors and coreceptor inhibitors have shown a high level of synergy. Similar studies performed with two co-receptor inhibitors have shown results varying from synergy to high antagonism depending on the viral isolate and the compounds used. In the following chapter, we will review some concepts of mechanisms that may affect these interactions.

Fetched live from OpenAlex and de-inverted. Abstracts are not stored in this database: the inverted indexes are 8.6 GB of the frame’s 9.3 GB of text, and the host has 13 GB free.

How this classification was reachedexpand

Full frame distilled prediction

Teacher imitation

Not calibrated prevalence, not ground truth. Human validation pending. Learned from the 10,348 direct Codex labels and 10,348 direct Gemma labels. Candidate is the union of thresholded teacher heads; consensus is their intersection. These outputs are machine_predicted_unvalidated and are not human labels or direct frontier model labels.

metaresearch head score (Codex)0.000
metaresearch head score (Gemma)0.000
Version: codex-gemma-dda1882f352aValidation status: machine_predicted_unvalidated
Candidate categoriesMeta-epidemiology (narrow)
Consensus categoriesnone
DomainCandidate signal: none · Consensus signal: none
Study designCandidate signal: Other design · Consensus signal: none
GenreCandidate signal: Review · Consensus signal: Review
Teacher disagreement score0.912
Threshold uncertainty score1.000

Codex and Gemma teacher scores by category

CategoryCodexGemma
Metaresearch0.0000.000
Meta-epidemiology (narrow)0.0010.000
Meta-epidemiology (broad)0.0020.000
Bibliometrics0.0010.001
Science and technology studies0.0000.000
Scholarly communication0.0000.000
Open science0.0000.000
Research integrity0.0000.001
Insufficient payload (model declined to judge)0.0000.000

Machine scores (provisional)

The two teacher heads of the student model, read on this work. A score orders the frame for review; it never asserts a category, and the validation status ships verbatim with every row.

Baseline scores from an immature model (maturity gate not passed, 7 training rounds). Scores rank; they never assert a category.

Opus teacher head0.086
GPT teacher head0.403
Teacher spread0.317 · how far apart the two teachers sit on this one work
Validation statusscore_only:v0-immature-baseline · verbatim from the scoring run: score_only means the number may rank works, and no category label ships from it

Classification

machine, unvalidated

Machine predicted; a candidate call from one teacher head, not a consensus.

Study designOther design
Domainnot available
GenreReview

How this classification was reached, model by model and score by score, is at the end of the page under "How this classification was reached".

Quick stats

Citations10
Published2004
Admission routes1
Has abstractyes

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