Purinergic Signaling: Targeting GPCRs, Ion Channels and Enzymes—A Theme Issue in Honor of Dr. Kenneth A. Jacobson

Dear Colleagues,

Dr. K. A. Jacobson is the John W. Daly Distinguished Scientist, Senior Investigator and Chief of the Molecular Recognition Section, Laboratory of Bioorganic Chemistry (NIDDK, NIH, Bethesda, USA). He earned his B.A. from Reed College (1975) and his Ph.D. in Chemistry with Murray Goodman at the University of California, San Diego (1981). He completed postdoctoral studies in organic chemistry at the Weizmann Institute and joined NIH in 1983, subsequently becoming a tenured Research Chemist (1988), Section Chief (since 1993), Senior Investigator (since 2003), and Lab Chief (2008–2018).

Dr. Jacobson is a pioneer in the field of ligand design and pharmacology of adenosine (P1) and P2 receptors. His numerous contributions include the first molecular model of adenosine receptors in 1992 and first publication on modeling the involvement of the 2nd extracellular loop of GPCRs in small molecule recognition. He introduced many of the first selective and high affinity agonists/antagonists (including fluorescent ligands and unique affinity labels) for adenosine, P2Y, and P2X receptors and developed the first selective, competitive antagonists for A₁, A_2B, A₃, P2Y₁, and P2Y₁₃ receptors and positive allosteric modulators (PAMs) for A₃ and P2X1 receptors. More than 36 compounds introduced by Jacobson and coworkers are available commercially as research tools. Five biopharma startups were founded based on the therapeutic potential of compounds from the Jacobson lab. Two selective A₃ adenosine agonists invented by Dr. Jacobson are being developed by the pharmaceutical industry and are in Phase II or III clinical trials for liver cancer, NASH, psoriasis, and other inflammatory diseases. A third A₃ agonist is licensed for pharma development for pain treatment. In collaboration with Ray Stevens (University of Southern California), he also contributed to the determination of the first X-ray crystal structures of P2Y and agonist-bound A_2A receptors.

Dr. Jacobson is a Fellow of the American Chemical Society and served as Chair of the Medicinal Chemistry Div. He mentored approximately 70 postdoctoral fellows throughout his career and authored more than 800 scientific publications (H-index of 109). As inventor of >60 patents on new receptor ligands and analytical methods, filed in the US and other countries, he was highlighted as a Featured NIDDK Innovator from the Office of Technology Transfer and Development.

His numerous awards include the Medicinal Chemistry Hall of Fame (2009), Philip S. Portoghese Medicinal Chemistry Award (2012), and Smissman Award (2017), all from the Medicinal Chemistry Div. of the American Chemical Soc. Other awards include the Sato Memorial International Award of the Pharmaceutical Soc. of Japan (2009), ASPET Goodman and Gilman Award in Drug Receptor Pharmacology (2014), and World’s Most Influential Scientific Minds, Pharmacology and Toxicology (2016, Thomson Reuters).

This Special Issue of Molecules is dedicated to Dr. K. A. Jacobson’s being awarded the first Tu Youyou Award (2017) to honor his great contributions and extraordinary research achievements.

Dr. Anna Junker
Dr. Antonella Ciancetta
Dr. Jinha Yu
Guest Editors

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