Small molecule immuno-oncology therapeutic agents

Bioorg Med Chem Lett. 2018 Feb 1;28(3):319-329. doi: 10.1016/j.bmcl.2017.12.044. Epub 2017 Dec 20.

Abstract

Treatment of cancer by activation of an antitumor immune response is now a widely practiced and well-accepted approach to therapy. However, despite dramatic responses in some patients, the high proportion of unresponsive patients points to a considerable unmet medical need. Although antibody therapies have led the way, small molecule immuno-oncology agents are close behind. This perspective provides an overview of some of the many small molecule approaches being explored. It encompasses small molecule modulators of validated targets such as programed cell death 1 (PD-1) as well as novel approaches still to be proven clinically.

Keywords: ARAQTZDRSNRIIK-UHFFFAOYSA-N; BEDXOYXWXUCQNA-IPJVBHEBSA-N; Cancer; FAVUUGQWYAJEGA-UHFFFAOYSA-N; FVWQPAOQPHOQRR-UHFFFAOYSA-N; HUVQZTCJKOXROE-RPXLBNRVSA-N; HWDKOBHGPXRKJJ-HMZIZCGUSA-J; Immuno-oncology; JWVAXOHLLDJSHF-QMJXVMRNSA-N; KRESAFFTFXNKOO-UHFFFAOYSA-N; MFZUODXFGTXTIW-GBEGKXJTSA-N; NINCPJHFIWWUAZ-CDRJQVBSSA-N; RBFLMTFTTMGEPS-UHFFFAOYSA-N; Small molecule; UATCGUSLBHISQR-ALSSIMQBSA-N; UBQQSDUBSSXCEW-DZHBTMGUSA-N; VDNKHSAOWUDCRM-ACSVFZNHSA-N; WUDIWKVIWHAQIO-UHFFFAOYSA-N.

Publication types

  • Review

MeSH terms

  • Animals
  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / pharmacology*
  • Apoptosis / drug effects
  • Cell Cycle Checkpoints / drug effects
  • Cell Proliferation / drug effects
  • Dose-Response Relationship, Drug
  • Drug Screening Assays, Antitumor
  • Humans
  • Immunologic Factors / chemistry
  • Immunologic Factors / pharmacology*
  • Mice
  • Molecular Structure
  • Programmed Cell Death 1 Receptor / antagonists & inhibitors
  • Programmed Cell Death 1 Receptor / metabolism
  • Small Molecule Libraries / chemistry
  • Small Molecule Libraries / pharmacology*
  • Structure-Activity Relationship

Substances

  • Antineoplastic Agents
  • Immunologic Factors
  • PDCD1 protein, human
  • Programmed Cell Death 1 Receptor
  • Small Molecule Libraries