This Special Issue invites contributions that highlight recent innovations in the design, synthesis, and application of macrocycles as therapeutic agents. Submit your manuscript by May 31, 2026.

A close-up image of a molecular structure, representing a chemical compound or a biological macromolecule.

As the need to modulate challenging drug targets grows increasingly urgent, novel approaches to drug discovery are essential. Macrocycles have emerged as a promising class of therapeutic agents, offering a unique combination of adaptability, selectivity, and favorable pharmacological profiles. Despite significant advances in their development, progress is still held back by limitations in synthetic accessibility, structural diversification, and predictive modeling, which collectively slow the efficient exploration of macrocycles as therapeutic modalities.

To highlight the exciting research in this area, the Journal of Medicinal Chemistry is opening submissions for an upcoming Special Issue called “Macrocycles as Therapeutic Modalities for Challenging Drug Targets.”

Read the recent Call for Papers Editorial by guest editor Weibo Yang to learn more about this Special Issue.

Topics include, but are not limited to:

  • Novel macrocyclization reactions and strategies
  • Computational design and modeling of macrocyclic compounds
  • Macrocyclic peptides and peptidomimetics
  • Targeted protein degradation and molecular glues involving macrocycles
  • Macrocyclic inhibitors of protein–protein interactions
  • Strategies to improve cell permeability and oral bioavailability
  • Case studies targeting undruggable proteins (e.g., RAS, c-MYC, transcription factors)
  • Advances in screening technologies for macrocyclic libraries
  • Structural studies and mechanistic insights into macrocycle-target interactions

Organizing Editors

Weibo Yang, Guest Editor
Chinese Academy of Sciences, China

Hiroaki Suga, Guest Editor
University of Tokyo, Japan

Christian Heinis, Guest Editor
EPFL - Swiss Federal Technology Institute of Lausanne, Switzerland

Andrei K. Yudin, Guest Editor
University of Toronto, Canada

Submission Information

We welcome submissions for this Special Issue through May 31, 2026. For more information on submission requirements, please visit the journal’s Author Guidelines page.

Accepted manuscripts for consideration in this Special Issue will include research articles, perspectives, and drug annotations. Papers accepted for publication for this Special Issue will be available ASAP (as soon as publishable) online as soon as they are accepted. After all submissions have been published, they will then be compiled online on a dedicated landing page to form the Special Issue. Manuscripts submitted for consideration will undergo the full rigorous peer review process expected from ACS journals.

How to Submit

  • Log in to the ACS Publishing Center.
  • Select the "Journals" tab.
  • Choose Journal of Medicinal Chemistry
  • Click "Submit."
  • Select your manuscript type, and, under "Special Issue Selection," choose “Macrocycles as Therapeutic Modalities for Challenging Drug Targets."

If you have any general questions regarding submission to this Special Issue, please contact managing.editor@jmedchem.acs.org.

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