title: Carbonic anhydrase inhibitors: a review on the progress of patent literature (2011-2016).
abstract: BACKGROUND
  A large area of carbonic anhydrase (CA) research focuses on the inhibition of human CA IX and CA XII, as these isoforms have been designated as biomarkers and therapeutic targets for various cancer types.
  
  
  METHODS
  Recently, the majority of CA inhibitor (CAI) patents cover compound design, synthesis, and delivery methods for the treatment of glaucoma and cancer. The analysis of included patents highlights the need for isoform specific inhibitors. This review covers the patents of medically relevant carbonic anhydrase inhibitors between 2011-2016.
  
  
  CONCLUSIONS
  The improvement of structure-based drug design methods and access to the crystal structures of human CA isoforms have improved inhibitor development. This progress can be observed in relation to the selective inhibition of CA IX for cancer treatments, with one inhibitor in clinical trials. However, the design of nonclassical CAIs is essential to further improve isoform specificity and prevent sulfur allergies.
authors.affiliation: a Department of Biochemistry and Molecular Biology , College of Medicine, University of Florida , Gainesville , FL , USA.
authors.forename: Carrie
authors.initials: C
authors.lastname: Lomelino
authors.affiliation: a Department of Biochemistry and Molecular Biology , College of Medicine, University of Florida , Gainesville , FL , USA.
authors.forename: Robert
authors.initials: R
authors.lastname: McKenna
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000008:administration & dosage / Q000494:pharmacology / Q000627:therapeutic use; D000071231:Carbonic Anhydrase IX / Q000037:antagonists & inhibitors / Q000737:chemistry / Q000378:metabolism; D002257:Carbonic Anhydrase Inhibitors / Q000008:administration & dosage* / Q000494:pharmacology / Q000627:therapeutic use; D002256:Carbonic Anhydrases / Q000737:chemistry / Q000187:drug effects* / Q000378:metabolism; D016503:Drug Delivery Systems; D015195:Drug Design; D005901:Glaucoma / Q000188:drug therapy; D006801:Humans; D009369:Neoplasms / Q000188:drug therapy; D010330:Patents as Topic
chemical_list: D000970:Antineoplastic Agents; D002257:Carbonic Anhydrase Inhibitors; D000071231:Carbonic Anhydrase IX; D002256:Carbonic Anhydrases; C477378:carbonic anhydrase XII
keywords: CA IX; cancer; carbonic anhydrase (CA); carbonic anhydrase inhibitors (CAIs); glaucoma; isoform specificity