Development of Human Carbonic Anhydrase II Heterobifunctional Degraders

Phase 1/2 study of ARV-110, an androgen receptor (AR) PROTAC degrader, in metastatic castration-resistant prostate cancer (mCRPC).

(2022) Xin Gao et al.   JOURNAL OF CLINICAL ONCOLOGY

PROTAC targeted protein degraders: the past is prologue

(2022) Miklós Békés et al.   NATURE REVIEWS DRUG DISCOVERY

Developing Metal-Binding Isosteres of 8-Hydroxyquinoline as Metalloenzyme Inhibitor Scaffolds

(2022) Hyeonglim Seo et al.   INORGANIC CHEMISTRY

Optimization of Class I Histone Deacetylase PROTACs Reveals that HDAC1/2 Degradation is Critical to Induce Apoptosis and Cell Arrest in Cancer Cells

(2022) Joshua P. Smalley et al.   JOURNAL OF MEDICINAL CHEMISTRY

ARV-471, an estrogen receptor (ER) PROTACdegrader, combined with palbociclib in advanced ER+/human epidermal growth factor receptor 2–negative (HER2-) breast cancer: Phase 1b cohort (part C) of a phase 1/2 study.

(2022) Erika P. Hamilton et al.   JOURNAL OF CLINICAL ONCOLOGY

Mutant-selective degradation by BRAF-targeting PROTACs

(2021) Shanique Alabi et al.   Nature Communications

A single–cell type transcriptomics map of human tissues

(2021) Max Karlsson et al.   Science Advances

PROTAC Technology: Opportunities and Challenges

(2020) Hongying Gao et al.   ACS Medicinal Chemistry Letters

Sulfonamide Inhibitors of Human Carbonic Anhydrases Designed through a Three-Tails Approach: Improving Ligand/Isoform Matching and Selectivity of Action

(2020) Alessandro Bonardi et al.   JOURNAL OF MEDICINAL CHEMISTRY

Progress in the development of human carbonic anhydrase inhibitors and their pharmacological applications: Where are we today?

(2020) Chandra B. Mishra et al.   MEDICINAL RESEARCH REVIEWS

Targeted protein degradation as a powerful research tool in basic biology and drug target discovery

(2020) Tao Wu et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

Improved Accuracy for Modeling PROTAC-Mediated Ternary Complex Formation and Targeted Protein Degradation via New In Silico Methodologies

(2020) Michael L. Drummond et al.   Journal of Chemical Information and Modeling

A chemical approach for global protein knockdown from mice to non-human primates

(2019) Xiuyun Sun et al.   Cell Discovery

Carbonic anhydrases as disease markers

(2019) Sabina Zamanova et al.   EXPERT OPINION ON THERAPEUTIC PATENTS

Development of Multifunctional Histone Deacetylase 6 Degraders with Potent Antimyeloma Activity

(2019) Hao Wu et al.   JOURNAL OF MEDICINAL CHEMISTRY

Advances in the structural annotation of human carbonic anhydrases and impact on future drug discovery

(2019) Alessio Nocentini et al.   Expert Opinion on Drug Discovery

Role of Carbonic Anhydrases and Inhibitors in Acid–Base Physiology: Insights from Mathematical Modeling

(2019) Occhipinti et al.   INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES

SAR Exploration of Tight Binding Inhibitors of Influenza Virus PA Endonuclease

(2019) Cy V. Credille et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of New 1,1′-Biphenyl-4-sulfonamides as Selective Subnanomolar Human Carbonic Anhydrase II Inhibitors

(2019) Giuseppe La Regina et al.   ACS Medicinal Chemistry Letters

Development of the first small molecule histone deacetylase 6 (HDAC6) degraders

(2018) Ka Yang et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

A surface proton antenna in carbonic anhydrase II supports lactate transport in cancer cells

(2018) Sina Ibne Noor et al.   eLife

Modulating PCAF/GCN5 Immune Cell Function through a PROTAC Approach

(2018) Zuni I. Bassi et al.   ACS Chemical Biology

Principles of Ubiquitin-Dependent Signaling

(2018) Eugene Oh et al.   Annual Review of Cell and Developmental Biology

Induced protein degradation: an emerging drug discovery paradigm

(2016) Ashton C. Lai et al.   NATURE REVIEWS DRUG DISCOVERY

A supramolecular dissociation strategy for protein sensing

(2015) Hui Wang et al.   CHEMICAL COMMUNICATIONS

Probing the ‘bipolar’ nature of the carbonic anhydrase active site: Aromatic sulfonamides containing 1,3-oxazol-5-yl moiety as picomolar inhibitors of cytosolic CA I and CA II isoforms

(2015) Mikhail Krasavin et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Catalytic in vivo protein knockdown by small-molecule PROTACs

(2015) Daniel P Bondeson et al.   Nature Chemical Biology

Structure of the DDB1–CRBN E3 ubiquitin ligase in complex with thalidomide

(2014) Eric S. Fischer et al.   NATURE

Activity and distribution of intracellular carbonic anhydrase II and their effects on the transport activity of anion exchanger AE1/SLC4A1

(2013) Samer Al-Samir et al.   JOURNAL OF PHYSIOLOGY-LONDON

A Comprehensive Mathematical Model for Three-Body Binding Equilibria

(2013) Eugene F. Douglass et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Structure, function and applications of carbonic anhydrase isozymes

(2012) Md. Imtaiyaz Hassan et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Structural annotation of human carbonic anhydrases

(2012) Mayank Aggarwal et al.   JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY

Glaucoma

(2011) Harry A Quigley   LANCET

Intramolecular proton shuttle supports not only catalytic but also noncatalytic function of carbonic anhydrase II

(2011) H. M. Becker et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Impact of linker length on the activity of PROTACs

(2010) Kedra Cyrus et al.   Molecular BioSystems

Carbonic Anhydrase as a Model for Biophysical and Physical-Organic Studies of Proteins and Protein−Ligand Binding

(2008) Vijay M. Krishnamurthy et al.   CHEMICAL REVIEWS

Carbonic anhydrases: novel therapeutic applications for inhibitors and activators

(2008) Claudiu T. Supuran   NATURE REVIEWS DRUG DISCOVERY