A rational approach to the design of selective substrates and potent non-transportable inhibitors of the excitatory amino acid transporter EAAC1 (EAAT3): new glutamate and aspartate analogues as potential neuroprotective agents

G Campiani; M De Angelis; S Armaroli; C Fattorusso; B Catalanotti; A Ramunno; V Nacci; C Grewer; D Ionescu; T Rauen; Roger Griffiths

doi:10.1021/jm015509z

A rational approach to the design of selective substrates and potent non-transportable inhibitors of the excitatory amino acid transporter EAAC1 (EAAT3): new glutamate and aspartate analogues as potential neuroprotective agents

G Campiani, M De Angelis, S Armaroli, C Fattorusso, B Catalanotti, A Ramunno, V Nacci, C Grewer, D Ionescu, T Rauen, Roger Griffiths

Research output: Contribution to journal › Article › peer-review

54 Citations (Scopus)

Abstract

Two three-dimensional receptor interaction models for EAAT substrates and nontransportable inhibitors have been developed, and new glutamate (Glu) and aspartate (Asp) analogues have been synthesized. The analogues la and 3 represent novel lead compounds for the development of EAAT substrates and nontransportable inhibitors, selective for EAATs over iGluRs, as possible neuroprotective agents useful to minimize the progression of chronic or acute neurodegenerative diseases, The role played by the protonatable amine function in the interaction with EAATs has been discussed.

Original language	English
Pages (from-to)	2507-2510
Number of pages	4
Journal	Journal of Medicinal Chemistry
Volume	44
DOIs	https://doi.org/10.1021/jm015509z
Publication status	Published - 2 Aug 2001

Keywords

HIGH-AFFINITY
OXIDATIVE STRESS
BRAIN
RECEPTORS
FAMILY

Access to Document

10.1021/jm015509z

Fingerprint

Dive into the research topics of 'A rational approach to the design of selective substrates and potent non-transportable inhibitors of the excitatory amino acid transporter EAAC1 (EAAT3): new glutamate and aspartate analogues as potential neuroprotective agents'. Together they form a unique fingerprint.

Cite this

Campiani, G., De Angelis, M., Armaroli, S., Fattorusso, C., Catalanotti, B., Ramunno, A., Nacci, V., Grewer, C., Ionescu, D., Rauen, T., & Griffiths, R. (2001). A rational approach to the design of selective substrates and potent non-transportable inhibitors of the excitatory amino acid transporter EAAC1 (EAAT3): new glutamate and aspartate analogues as potential neuroprotective agents. Journal of Medicinal Chemistry, 44, 2507-2510. https://doi.org/10.1021/jm015509z

@article{2cccaa4b48534da1ae594d4a795e5ca9,

title = "A rational approach to the design of selective substrates and potent non-transportable inhibitors of the excitatory amino acid transporter EAAC1 (EAAT3): new glutamate and aspartate analogues as potential neuroprotective agents",

abstract = "Two three-dimensional receptor interaction models for EAAT substrates and nontransportable inhibitors have been developed, and new glutamate (Glu) and aspartate (Asp) analogues have been synthesized. The analogues la and 3 represent novel lead compounds for the development of EAAT substrates and nontransportable inhibitors, selective for EAATs over iGluRs, as possible neuroprotective agents useful to minimize the progression of chronic or acute neurodegenerative diseases, The role played by the protonatable amine function in the interaction with EAATs has been discussed.",

keywords = "HIGH-AFFINITY, OXIDATIVE STRESS, BRAIN, RECEPTORS, FAMILY",

author = "G Campiani and {De Angelis}, M and S Armaroli and C Fattorusso and B Catalanotti and A Ramunno and V Nacci and C Grewer and D Ionescu and T Rauen and Roger Griffiths",

note = "This paper is an output from a collaborative, multidisciplinary, transnational CEC Biotech Award. The input is broken down as chemical synthesis and modelling (Italy), electrophysiology (Germany) and biochemical pharmacology (Scotland, St Andrews).",

year = "2001",

month = aug,

day = "2",

doi = "10.1021/jm015509z",

language = "English",

volume = "44",

pages = "2507--2510",

journal = "Journal of Medicinal Chemistry",

issn = "0022-2623",

publisher = "American Chemical Society (ACS)",

}

Campiani, G, De Angelis, M, Armaroli, S, Fattorusso, C, Catalanotti, B, Ramunno, A, Nacci, V, Grewer, C, Ionescu, D, Rauen, T & Griffiths, R 2001, 'A rational approach to the design of selective substrates and potent non-transportable inhibitors of the excitatory amino acid transporter EAAC1 (EAAT3): new glutamate and aspartate analogues as potential neuroprotective agents', Journal of Medicinal Chemistry, vol. 44, pp. 2507-2510. https://doi.org/10.1021/jm015509z

A rational approach to the design of selective substrates and potent non-transportable inhibitors of the excitatory amino acid transporter EAAC1 (EAAT3): new glutamate and aspartate analogues as potential neuroprotective agents. / Campiani, G; De Angelis, M; Armaroli, S et al.
In: Journal of Medicinal Chemistry, Vol. 44, 02.08.2001, p. 2507-2510.

Research output: Contribution to journal › Article › peer-review

TY - JOUR

T1 - A rational approach to the design of selective substrates and potent non-transportable inhibitors of the excitatory amino acid transporter EAAC1 (EAAT3): new glutamate and aspartate analogues as potential neuroprotective agents

AU - Campiani, G

AU - De Angelis, M

AU - Armaroli, S

AU - Fattorusso, C

AU - Catalanotti, B

AU - Ramunno, A

AU - Nacci, V

AU - Grewer, C

AU - Ionescu, D

AU - Rauen, T

AU - Griffiths, Roger

N1 - This paper is an output from a collaborative, multidisciplinary, transnational CEC Biotech Award. The input is broken down as chemical synthesis and modelling (Italy), electrophysiology (Germany) and biochemical pharmacology (Scotland, St Andrews).

PY - 2001/8/2

Y1 - 2001/8/2

N2 - Two three-dimensional receptor interaction models for EAAT substrates and nontransportable inhibitors have been developed, and new glutamate (Glu) and aspartate (Asp) analogues have been synthesized. The analogues la and 3 represent novel lead compounds for the development of EAAT substrates and nontransportable inhibitors, selective for EAATs over iGluRs, as possible neuroprotective agents useful to minimize the progression of chronic or acute neurodegenerative diseases, The role played by the protonatable amine function in the interaction with EAATs has been discussed.

AB - Two three-dimensional receptor interaction models for EAAT substrates and nontransportable inhibitors have been developed, and new glutamate (Glu) and aspartate (Asp) analogues have been synthesized. The analogues la and 3 represent novel lead compounds for the development of EAAT substrates and nontransportable inhibitors, selective for EAATs over iGluRs, as possible neuroprotective agents useful to minimize the progression of chronic or acute neurodegenerative diseases, The role played by the protonatable amine function in the interaction with EAATs has been discussed.

KW - HIGH-AFFINITY

KW - OXIDATIVE STRESS

KW - BRAIN

KW - RECEPTORS

KW - FAMILY

UR - http://www.scopus.com/inward/record.url?scp=0035797358&partnerID=8YFLogxK

U2 - 10.1021/jm015509z

DO - 10.1021/jm015509z

M3 - Article

SN - 0022-2623

VL - 44

SP - 2507

EP - 2510

JO - Journal of Medicinal Chemistry

JF - Journal of Medicinal Chemistry

ER -

Campiani G, De Angelis M, Armaroli S, Fattorusso C, Catalanotti B, Ramunno A et al. A rational approach to the design of selective substrates and potent non-transportable inhibitors of the excitatory amino acid transporter EAAC1 (EAAT3): new glutamate and aspartate analogues as potential neuroprotective agents. Journal of Medicinal Chemistry. 2001 Aug 2;44:2507-2510. doi: 10.1021/jm015509z

A rational approach to the design of selective substrates and potent non-transportable inhibitors of the excitatory amino acid transporter EAAC1 (EAAT3): new glutamate and aspartate analogues as potential neuroprotective agents

Abstract

Keywords

Access to Document

Other files and links

Fingerprint

Cite this