Eupenicillium shearii

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Eupenicillium shearii is a fungus in the genus Penicillium . The type strain was first isolated in 1931 by Dr. Otto R. Reinking from a soil sample taken in Honduras. It has also been isolated from soil collected in the Democratic Republic of the Congo and near Abidjan. It was named and described in 1967. [1]

E. shearii is of interest to medicinal chemists due to its production of kaitocephalin, a substance that may protect the brain and nervous system. [2] Therefore, kaitocephalin is an attractive scaffold for drug development. Drugs based on this compound may be used to treat neurological conditions including Alzheimer’s, amyotrophic lateral sclerosis (ALS), and stroke. [3]

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Kaitocephalin is a non-selective ionotropic glutamate receptor antagonist, meaning it blocks the action of the neurotransmitter glutamate. It is produced by the fungus Eupenicillium shearii. Although similar molecules have been produced synthetically, kaitocephalin is the only known naturally occurring glutamate receptor antagonist. There is some evidence that kaitocephalin can protect the brain and central nervous system, so it is said to have neuroprotective properties. Kaitocephalin protects neurons by inhibiting excitotoxicity, a mechanism which causes cell death by overloading neurons with glutamate. Because of this, it is of interest as a potential scaffold for drug development. Drugs based on kaitocephalin may be useful in treating neurological conditions, including Alzheimer's, amyotrophic lateral sclerosis (ALS), and stroke.

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References

  1. Amelia C. Stolk and De B. Scott, "Studies on the Genus Eupenicillium Ludwig", Persoonia 4 (1967): 391-405
  2. Yoko Yasuno et al., "(7S)-Kaitocephalin as a potent NMDA receptor selective ligand", Org. Biomol. Chem. 14 (2016): 1206-1210
  3. Philip Garner et al., "A concise [C+NC+CC] coupling-enabled synthesis of kaitocephalin", Chem. Commun. 50 (2014): 4908-4910