The history, mechanism, and perspectives of nirmatrelvir (PF-07321332): an orally bioavailable main protease inhibitor used in combination with ritonavir to reduce COVID-19-related hospitalizations

Nirmatrelvir/ritonavir use: Managing clinically significant drug‐drug interactions with transplant immunosuppressants

(2022) Nicholas W. Lange et al.   AMERICAN JOURNAL OF TRANSPLANTATION

Emerging COVID-19 variants and their impact on SARS-CoV-2 diagnosis, therapeutics and vaccines

(2022) Queenie Fernandes et al.   ANNALS OF MEDICINE

SARS-CoV-2 Omicron variant is highly sensitive to molnupiravir, nirmatrelvir, and the combination

(2022) Pengfei Li et al.   CELL RESEARCH

Disposition of PF-07321332 (Nirmatrelvir), an Orally Bioavailable Inhibitor of SARS-CoV-2 3CL Protease, across Animals and Humans

(2022) Heather Eng et al.   DRUG METABOLISM AND DISPOSITION

Oral Nirmatrelvir for High-Risk, Nonhospitalized Adults with Covid-19

(2022) Jennifer Hammond et al.   NEW ENGLAND JOURNAL OF MEDICINE

Editorial: Current Status of Oral Antiviral Drug Treatments for SARS-CoV-2 Infection in Non-Hospitalized Patients

(2022) Dinah V. Parums   MEDICAL SCIENCE MONITOR

Oral Nirmatrelvir/Ritonavir Therapy for COVID-19: The Dawn in the Dark?

(2022) Yuan-Pin Hung et al.   Antibiotics-Basel

Main protease mutants of SARS-CoV-2 variants remain susceptible to nirmatrelvir

(2022) Sven Ullrich et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Covalent Reversible Inhibitors of Cysteine Proteases Containing the Nitrile Warhead: Recent Advancement in the Field of Viral and Parasitic Diseases

(2022) Simone Brogi et al.   MOLECULES

Public health actions to control new SARS-CoV-2 variants

(2021) Nathan D. Grubaugh et al.   CELL

Considerations for the Discovery and Development of 3-Chymotrypsin-Like Cysteine Protease Inhibitors Targeting SARS-CoV-2 Infection

(2021) Koen Vandyck et al.   Current Opinion in Virology

Rethinking Remdesivir: Synthesis, Antiviral Activity, and Pharmacokinetics of Oral Lipid Prodrugs

(2021) Robert T. Schooley et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

Characterization of the non-covalent interaction between the PF-07321332 inhibitor and the SARS-CoV-2 main protease

(2021) Marina Macchiagodena et al.   JOURNAL OF MOLECULAR GRAPHICS & MODELLING

Caution required with use of ritonavir-boosted PF-07321332 in COVID-19 management

(2021) Joseph Heskin et al.   LANCET

Heavily mutated Omicron variant puts scientists on alert

(2021) Ewen Callaway   NATURE

An oral SARS-CoV-2 M pro inhibitor clinical candidate for the treatment of COVID-19

(2021) Dafydd R. Owen et al.   SCIENCE

Crystal structure of SARS-CoV-2 main protease in complex with protease inhibitor PF-07321332

(2021) Yao Zhao et al.   Protein & Cell

Validation and invalidation of SARS-CoV-2 main protease inhibitors using the Flip-GFP and Protease-Glo luciferase assays

(2021) Chunlong Ma et al.   Acta Pharmaceutica Sinica B

A new coronavirus associated with human respiratory disease in China

(2020) Fan Wu et al.   NATURE

Structure of Mpro from SARS-CoV-2 and discovery of its inhibitors

(2020) Zhenming Jin et al.   NATURE

Boceprevir, GC-376, and calpain inhibitors II, XII inhibit SARS-CoV-2 viral replication by targeting the viral main protease

(2020) Chunlong Ma et al.   CELL RESEARCH

The SARS-CoV-2 main protease as drug target

(2020) Sven Ullrich et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

SARS-CoV-2 Mpro inhibitors and activity-based probes for patient-sample imaging

(2020) Wioletta Rut et al.   Nature Chemical Biology

Both Boceprevir and GC376 efficaciously inhibit SARS-CoV-2 by targeting its main protease

(2020) Lifeng Fu et al.   Nature Communications

Characterising covalent warhead reactivity

(2019) James S. Martin et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Structure-based design and in vivo anti-arthritic activity evaluation of a potent dipeptidyl cyclopropyl nitrile inhibitor of cathepsin C

(2019) Brice Korkmaz et al.   BIOCHEMICAL PHARMACOLOGY

Pharmacokinetic enhancers (cobicistat/ritonavir) and the potential for drug-drug interactions

(2019) Paul Hollywood et al.   IRISH JOURNAL OF MEDICAL SCIENCE

Emerging and Re-Emerging Warheads for Targeted Covalent Inhibitors: Applications in Medicinal Chemistry and Chemical Biology

(2018) Matthias Gehringer et al.   JOURNAL OF MEDICINAL CHEMISTRY

An Overview of Severe Acute Respiratory Syndrome–Coronavirus (SARS-CoV) 3CL Protease Inhibitors: Peptidomimetics and Small Molecule Chemotherapy

(2016) Thanigaimalai Pillaiyar et al.   JOURNAL OF MEDICINAL CHEMISTRY

Cyanohydrin as an Anchoring Group for Potent and Selective Inhibitors of Enterovirus 71 3C Protease

(2015) Yangyang Zhai et al.   JOURNAL OF MEDICINAL CHEMISTRY

Reversible Cysteine Protease Inhibitors Show Promise for a Chagas Disease Cure

(2013) Momar Ndao et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

3C Protease of Enterovirus 68: Structure-Based Design of Michael Acceptor Inhibitors and Their Broad-Spectrum Antiviral Effects against Picornaviruses

(2013) J. Tan et al.   JOURNAL OF VIROLOGY

Design, synthesis and crystallographic analysis of nitrile-based broad-spectrum peptidomimetic inhibitors for coronavirus 3C-like proteases

(2012) Chi-Pang Chuck et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Discovery of boceprevir, a direct-acting NS3/4A protease inhibitor for treatment of chronic hepatitis C infections

(2012) Srikanth Venkatraman   TRENDS IN PHARMACOLOGICAL SCIENCES

Mutation of Glu-166 Blocks the Substrate-Induced Dimerization of SARS Coronavirus Main Protease

(2010) Shu-Chun Cheng et al.   BIOPHYSICAL JOURNAL