Javascript must be enabled to continue!
Design of a First-in-Class homoPROTAC to Induce ICP0 Degradation in Human Herpes Simplex Virus 1
View through CrossRef
Background/Objectives: Human Herpes Simplex Virus 1 (HSV-1) is a common pathogen that establishes lifelong latent infections. The emergence of drug resistance necessitates novel therapeutic strategies. This study introduces a novel antiviral approach: a bivalent degrader designed to induce the degradation of an essential protein. Methods: A structural model of ICP0, generated via the Chai-1 AI platform, was analyzed with fpocket, P2Rank, and KVFinder to identify a superior allosteric target site. An iterative de novo design workflow with CReM-dock then yielded a lead scaffold based on its predicted affinity and drug-like properties. This selected “warhead” was used to rationally design the final bivalent degrader, ICP0-deg-01, for the ICP0 dimer model. Results: The generative process yielded a lead chemical scaffold that was selected based on its predicted binding affinity and favorable drug-like properties. This scaffold was used to rationally design a single candidate bivalent degrader, ICP0-deg-01. Our structural model predicts that ICP0-deg-01 can successfully bridge two ICP0 protomers, forming an energetically favorable ternary complex. Conclusions: This work provides a computational proof-of-concept for a novel class of anti-herpetic agents and identifies a lead candidate for future molecular dynamics simulations and experimental validation.
Title: Design of a First-in-Class homoPROTAC to Induce ICP0 Degradation in Human Herpes Simplex Virus 1
Description:
Background/Objectives: Human Herpes Simplex Virus 1 (HSV-1) is a common pathogen that establishes lifelong latent infections.
The emergence of drug resistance necessitates novel therapeutic strategies.
This study introduces a novel antiviral approach: a bivalent degrader designed to induce the degradation of an essential protein.
Methods: A structural model of ICP0, generated via the Chai-1 AI platform, was analyzed with fpocket, P2Rank, and KVFinder to identify a superior allosteric target site.
An iterative de novo design workflow with CReM-dock then yielded a lead scaffold based on its predicted affinity and drug-like properties.
This selected “warhead” was used to rationally design the final bivalent degrader, ICP0-deg-01, for the ICP0 dimer model.
Results: The generative process yielded a lead chemical scaffold that was selected based on its predicted binding affinity and favorable drug-like properties.
This scaffold was used to rationally design a single candidate bivalent degrader, ICP0-deg-01.
Our structural model predicts that ICP0-deg-01 can successfully bridge two ICP0 protomers, forming an energetically favorable ternary complex.
Conclusions: This work provides a computational proof-of-concept for a novel class of anti-herpetic agents and identifies a lead candidate for future molecular dynamics simulations and experimental validation.
Related Results
Design of a First-in-Class homoPROTAC to Induce ICP0 Degradation in Human Herpes Simplex Virus 1
Design of a First-in-Class homoPROTAC to Induce ICP0 Degradation in Human Herpes Simplex Virus 1
Background/Objectives: Human Herpes Simplex Virus 1 (HSV-1) is a pervasive pathogen that establishes lifelong latent infections, and the emergence of drug resistance necessitates n...
STAT-1- and IRF-3-Dependent Pathways Are Not Essential for Repression of ICP0-Null Mutant Herpes Simplex Virus Type 1 in Human Fibroblasts
STAT-1- and IRF-3-Dependent Pathways Are Not Essential for Repression of ICP0-Null Mutant Herpes Simplex Virus Type 1 in Human Fibroblasts
ABSTRACT
Efficient herpes simplex virus type 1 (HSV-1) infection of human fibroblasts (HFs) is highly dependent on the viral immediate-early regulatory protein ICP0 unles...
APLICAÇÃO DA TERAPIA FOTODINÂMICA ANTIMICROBIANA EM LESÕES DE HERPES LABIAL
APLICAÇÃO DA TERAPIA FOTODINÂMICA ANTIMICROBIANA EM LESÕES DE HERPES LABIAL
Introdução: O herpes simples é uma doença viral recorrente que afeta grande parte da população mundial. As lesões de herpes são comumente dolorosas e podem ter impactos na qualidad...
Benchmarking Bayesian methods for spectroscopy
Benchmarking Bayesian methods for spectroscopy
<p class="p1"><span class="s1"><strong>Introduction:</strong></span>&l...
Herpesviruses (Human)
Herpesviruses (Human)
Abstract
Human herpesviruses are a family of eight
deoxyribonucleic acid
(DNA) viruses. There are thr...
Perinatal HIV infection and opportunistic infectious pathology: morphological features of the placenta
Perinatal HIV infection and opportunistic infectious pathology: morphological features of the placenta
Opportunistic infections account for more than 90% of all deaths associated with immunosuppression resulting from exposure to the human immunodeficiency virus (HIV). Fatal opportun...
Fuze Well Mechanical Interface
Fuze Well Mechanical Interface
<div class="section abstract">
<div class="htmlview paragraph">This interface standard applies to fuzes used in airborne weapons that use a 3-Inch Fuze Well. It defin...

