Novel inhibitors of the high-affinity l-proline transporter as potential therapeutic agents for the treatment of cognitive disorders

G. Greg Zipp; Joseph Barbosa; Michael A. Green; Kristen M. Terranova; Cynthia Fink; Xuan Chuan Yu; Amr Nouraldeen; Alan Wilson; Katerina Savelieva; Thomas H. Lanthorn; S. David Kimball

doi:10.1016/j.bmcl.2014.06.049

Novel inhibitors of the high-affinity l-proline transporter as potential therapeutic agents for the treatment of cognitive disorders

G. Greg Zipp
, Joseph Barbosa
, Michael A. Green
, Kristen M. Terranova
, Cynthia Fink
, Xuan Chuan Yu
, Amr Nouraldeen
, Alan Wilson
, Katerina Savelieva
, Thomas H. Lanthorn
, S. David Kimball

Rutgers, The State University

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

4 Scopus citations

Abstract

The incidence of cognitive disorders such as Alzheimer's disease continues to increase unabated. While cures for such diseases have eluded investigators, progress is being made on alleviating certain symptoms of these diseases. Mouse knockouts of the proline transporter (PROT), a high affinity Na ⁺/Cl^--dependent transporter, indicated its potential as a novel therapeutic target for cognition improvement. Herein we report our investigation into a novel class of PROT inhibitors.

Original language	American English
Pages (from-to)	3886-3890
Number of pages	5
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	24
Issue number	16
DOIs	https://doi.org/10.1016/j.bmcl.2014.06.049
State	Published - Aug 15 2014

ASJC Scopus subject areas

Biochemistry
Molecular Medicine
Molecular Biology
Pharmaceutical Science
Drug Discovery
Clinical Biochemistry
Organic Chemistry

Keywords

Acyl piperazine
Alzheimer's disease
Dimentia
Inhibitor
Proline transporter

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10.1016/j.bmcl.2014.06.049

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Zipp, G. G., Barbosa, J., Green, M. A., Terranova, K. M., Fink, C., Yu, X. C., Nouraldeen, A., Wilson, A., Savelieva, K., Lanthorn, T. H., & David Kimball, S. (2014). Novel inhibitors of the high-affinity l-proline transporter as potential therapeutic agents for the treatment of cognitive disorders. Bioorganic and Medicinal Chemistry Letters, 24(16), 3886-3890. https://doi.org/10.1016/j.bmcl.2014.06.049

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abstract = "The incidence of cognitive disorders such as Alzheimer's disease continues to increase unabated. While cures for such diseases have eluded investigators, progress is being made on alleviating certain symptoms of these diseases. Mouse knockouts of the proline transporter (PROT), a high affinity Na +/Cl--dependent transporter, indicated its potential as a novel therapeutic target for cognition improvement. Herein we report our investigation into a novel class of PROT inhibitors.",

keywords = "Acyl piperazine, Alzheimer's disease, Dimentia, Inhibitor, Proline transporter",

author = "Zipp, \{G. Greg\} and Joseph Barbosa and Green, \{Michael A.\} and Terranova, \{Kristen M.\} and Cynthia Fink and Yu, \{Xuan Chuan\} and Amr Nouraldeen and Alan Wilson and Katerina Savelieva and Lanthorn, \{Thomas H.\} and \{David Kimball\}, S.",

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Zipp, GG, Barbosa, J, Green, MA, Terranova, KM, Fink, C, Yu, XC, Nouraldeen, A, Wilson, A, Savelieva, K, Lanthorn, TH & David Kimball, S 2014, 'Novel inhibitors of the high-affinity l-proline transporter as potential therapeutic agents for the treatment of cognitive disorders', Bioorganic and Medicinal Chemistry Letters, vol. 24, no. 16, pp. 3886-3890. https://doi.org/10.1016/j.bmcl.2014.06.049

TY - JOUR

T1 - Novel inhibitors of the high-affinity l-proline transporter as potential therapeutic agents for the treatment of cognitive disorders

AU - Zipp, G. Greg

AU - Barbosa, Joseph

AU - Green, Michael A.

AU - Terranova, Kristen M.

AU - Fink, Cynthia

AU - Yu, Xuan Chuan

AU - Nouraldeen, Amr

AU - Wilson, Alan

AU - Savelieva, Katerina

AU - Lanthorn, Thomas H.

AU - David Kimball, S.

PY - 2014/8/15

Y1 - 2014/8/15

N2 - The incidence of cognitive disorders such as Alzheimer's disease continues to increase unabated. While cures for such diseases have eluded investigators, progress is being made on alleviating certain symptoms of these diseases. Mouse knockouts of the proline transporter (PROT), a high affinity Na +/Cl--dependent transporter, indicated its potential as a novel therapeutic target for cognition improvement. Herein we report our investigation into a novel class of PROT inhibitors.

AB - The incidence of cognitive disorders such as Alzheimer's disease continues to increase unabated. While cures for such diseases have eluded investigators, progress is being made on alleviating certain symptoms of these diseases. Mouse knockouts of the proline transporter (PROT), a high affinity Na +/Cl--dependent transporter, indicated its potential as a novel therapeutic target for cognition improvement. Herein we report our investigation into a novel class of PROT inhibitors.

KW - Acyl piperazine

KW - Alzheimer's disease

KW - Dimentia

KW - Inhibitor

KW - Proline transporter

UR - https://www.scopus.com/pages/publications/84905917524

UR - https://www.scopus.com/pages/publications/84905917524#tab=citedBy

U2 - 10.1016/j.bmcl.2014.06.049

DO - 10.1016/j.bmcl.2014.06.049

M3 - Article

C2 - 25037917

SN - 0960-894X

VL - 24

SP - 3886

EP - 3890

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 16

ER -

Novel inhibitors of the high-affinity l-proline transporter as potential therapeutic agents for the treatment of cognitive disorders

Abstract

ASJC Scopus subject areas

Keywords

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