A mechanism-aware stoichiometry platform resolves functional viral thresholds and induces antiviral hypersensitivity

Antiviral discovery is frequently hindered by a 'stoichiometric blind spot'-a lack of resolution regarding the functional density of viral enzymes required for replication. Traditional screening pipelines rely on target-based or phenotypic assays that cannot distinguish between simple molecular binding and the crossing of a functional 'stoichiometric cliff.' Here, we present a mechanism-aware platform that resolves these enzymatic requirements with single-virion precision. By integrating quantitative cryo-electron microscopy and genomic validation with Monte Carlo modeling, we map the stoichiometric landscapes of HIV-1 Protease (PR) and Reverse Transcriptase (RT). We uncover a striking disparity in enzymatic demand: a high-redundancy 'buffering capacity' for PR (∼40 monomers) contrasted with a high-threshold requirement for RT (∼95 subunits). We demonstrate that by systematically 'de-buffering' the virion, our platform induces a state of antiviral hypersensitivity, enabling the detection of therapeutic activity in novel and clinical inhibitors that remain invisible to traditional workflows. Furthermore, this multiplexed profiling enables de novo target identification, as inhibitors trigger failure exclusively on their respective stoichiometric arms. This platform provides a deterministic roadmap for de-risking drug discovery and identifying viral sub-stoichiometric vulnerabilities.

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Publication Details

Journal
bioRxiv (Cold Spring Harbor Laboratory)
Published
2026-02-10
DOI
https://doi.org/10.64898/2026.02.09.704886
Primary Topic
HIV/AIDS drug development and treatment
Type
article
Field-Weighted Citation Impact
0.00

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article

A mechanism-aware stoichiometry platform resolves functional viral thresholds and induces antiviral hypersensitivity

Saveez Saffarian, Eric O. Freed, Rodrigo Gallegos, Wiley Peppel et al.
bioRxiv (Cold Spring Harbor Laboratory)
HIV/AIDS drug development and treatment
article

A mechanism-aware stoichiometry platform resolves functional viral thresholds and induces antiviral hypersensitivity

Saveez Saffarian, Eric O. Freed, Rodrigo Gallegos, Wiley Peppel, Brian MacArthur, Haley Durden, Nicole Bohn, Abdul Waheed, Benjamin Preece, Abby Petersen, Gabe Clinger, Ahmet Yildiz, Aaron Daurelle
article en

Abstract

Antiviral discovery is frequently hindered by a 'stoichiometric blind spot'-a lack of resolution regarding the functional density of viral enzymes required for replication. Traditional screening pipelines rely on target-based or phenotypic assays that cannot distinguish between simple molecular binding and the crossing of a functional 'stoichiometric cliff.' Here, we present a mechanism-aware platform that resolves these enzymatic requirements with single-virion precision. By integrating quantitative cryo-electron microscopy and genomic validation with Monte Carlo modeling, we map the stoichiometric landscapes of HIV-1 Protease (PR) and Reverse Transcriptase (RT). We uncover a striking disparity in enzymatic demand: a high-redundancy 'buffering capacity' for PR (∼40 monomers) contrasted with a high-threshold requirement for RT (∼95 subunits). We demonstrate that by systematically 'de-buffering' the virion, our platform induces a state of antiviral hypersensitivity, enabling the detection of therapeutic activity in novel and clinical inhibitors that remain invisible to traditional workflows. Furthermore, this multiplexed profiling enables de novo target identification, as inhibitors trigger failure exclusively on their respective stoichiometric arms. This platform provides a deterministic roadmap for de-risking drug discovery and identifying viral sub-stoichiometric vulnerabilities.

bioRxiv (Cold Spring Harbor Laboratory)
University of Utah (US), National Cancer Institute (US), Center for Cancer Research (US), University of California, Berkeley (US)
National Institutes of Health
Good health and well-being
Openalex Percentile: Top 60%
HIV/AIDS drug development and treatment
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