Therapeutic development in targeting protein–protein interactions with synthetic topological mimetics
Open accessAbstract
Protein-protein interactions lie at the heart of cellular signaling pathways and the deregulation of which has frequently led to diseases. In contrast to inhibitors that bind to distinctive enzyme active sites, molecules targeting protein surface topologies have been underexploited in drug development. The challenges in developing protein surface antagonists or agonists originate from the relatively large and flat surface areas that lack well-defined cavities required for sufficient binding affinity. In the past decade, our understanding of protein recognition has served as solid basis for the design of synthetic mimetics to modulate these protein-protein interactions. Herein, we summarize recent successes in the development of synthetic α-helix mimetics, proteomimetics, and biologics with the therapeutic potentials of inhibiting tumorgenesis or cancer-related viral infections.
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- Authors
- Tsou, L. K., Cheng, Y., & Cheng, Y.-C.
- Affiliations
- Rockefeller University (US)
- Yale University (US)
- Corresponding author
- Cheng, Yung-Chi
- ORCID
- Tsou, Lun K
- Venue
- Current Opinion in Pharmacology
- Publisher
- Elsevier BV
- Published
- 2012-08
- Volume
- 12
- Issue
- 4
- Pages
- 403-407
- ISSN
- 1471-4892 (ISSN-L)
- PMC
- PMC3660839
- OpenAlex
- W2006576925
- Cited by
- 10
- References
- 34
- Citations by year
- 2020: 2 · 2019: 2 · 2017: 2 · 2016: 1 · 2015: 1 · 2013: 2
- FWCI
- 0.09
- Type
- journal article
- Language
- en
- Open access
- green
- europepmc.org
- Locations
- Current Opinion in Pharmacology (publishedVersion)
- PubMed (publishedVersion)
- Europe PMC (PubMed Central) (acceptedVersion)
- PubMed Central (acceptedVersion)
- Funders
- National Cancer Institute (P01CA154295)
- National Institute of Allergy and Infectious Diseases (R56 AI038204, AI 38204, R01AI038204)
- Topics
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Chemical Synthesis and Analysis
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Protein Structure and Dynamics
- Physical Sciences › Materials Science › Biomaterials › Supramolecular Self-Assembly in Materials
- Keywords
- protein-protein interaction, biologics, tumorigenesis inhibition, drug development
- MeSH terms
- Antineoplastic Agents, Antiviral Agents, Biological Products, Humans, Neoplasms, Protein Binding, Proteins, Apoptosis, Receptor Protein-Tyrosine Kinases, Receptors, Death Domain
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