Discovery and Evaluation of BMS-708163, a Potent, Selective and Orally Bioavailable γ-Secretase Inhibitor (Q33558208)

28 July 2017

title

Discovery and Evaluation of BMS-708163, a Potent, Selective and Orally Bioavailable γ-Secretase Inhibitor (English)

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28 July 2017

John G Houston

17

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author name string

Kevin W Gillman

1

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28 July 2017

John E Starrett

2

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28 July 2017

Michael F Parker

3

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28 July 2017

Kai Xie

4

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Joanne J Bronson

5

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Lawrence R Marcin

6

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Kate E McElhone

7

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Carl P Bergstrom

8

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Robert A Mate

9

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Richard Williams

10

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Jere E Meredith

11

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28 July 2017

Catherine R Burton

12

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Donna M Barten

13

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Jeremy H Toyn

14

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Susan B Roberts

15

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Kimberley A Lentz

16

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Robert Zaczek

18

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Charles F Albright

19

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28 July 2017

Carl P Decicco

20

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28 July 2017

John E Macor

21

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Richard E Olson

22

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28 July 2017

language of work or name

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22 March 2010

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ACS Medicinal Chemistry Letters

28 July 2017

published in

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28 July 2017

volume

1

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28 July 2017

issue

3

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page(s)

120-124

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The amyloid-beta rise and gamma-secretase inhibitor potency depend on the level of substrate expression

28 July 2017

cites work

1 reference

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Deciphering the molecular basis of memory failure in Alzheimer's disease

21 June 2018

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Modulation of notch processing by gamma-secretase inhibitors causes intestinal goblet cell metaplasia and induction of genes known to specify gut secretory lineage differentiation

21 June 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4007960

Chronic treatment with the gamma-secretase inhibitor LY-411,575 inhibits beta-amyloid peptide production and alters lymphopoiesis and intestinal cell differentiation

21 June 2018

1 reference

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Adipsin, a biomarker of gastrointestinal toxicity mediated by a functional gamma-secretase inhibitor

21 June 2018

1 reference

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Alzheimer's disease: genes, proteins, and therapy

21 June 2018

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Notch signaling: a dance of proteins changing partners

21 June 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4007960

Notch signaling: cell fate control and signal integration in development

21 June 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4007960

Novel benzodiazepine receptor partial agonists: oxadiazolylimidazobenzodiazepines

21 June 2018

1 reference

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Synthesis and biological activity of 1,2,4-oxadiazole derivatives: highly potent and efficacious agonists for cortical muscarinic receptors.

21 June 2018

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Studies on the pharmacokinetics and metabolism of a gamma-secretase inhibitor BMS-299897, and exploratory investigation of CYP enzyme induction.

21 June 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4007960

Discovery of begacestat, a Notch-1-sparing gamma-secretase inhibitor for the treatment of Alzheimer's disease

31 October 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4007960

Safety, tolerability, and effects on plasma and cerebrospinal fluid amyloid-beta after inhibition of gamma-secretase

31 October 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4007960

Reductions in beta-amyloid concentrations in vivo by the gamma-secretase inhibitors BMS-289948 and BMS-299897.

31 October 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4007960

Dynamics of {beta}-amyloid reductions in brain, cerebrospinal fluid, and plasma of {beta}-amyloid precursor protein transgenic mice treated with a {gamma}-secretase inhibitor

31 October 2018

1 reference

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Orally active GPIIb/IIIa antagonists: synthesis and biological activities of masked amidines as prodrugs of 2-[(3S)-4.

31 October 2018

1 reference

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Amino-caprolactam derivatives as gamma-secretase inhibitors

31 October 2018

1 reference

PubMed

https://pubmed.ncbi.nlm.nih.gov/24900185

inferred from PubMed ID database lookup

12 December 2020

based on heuristic

Identifiers

DOI

10.1021/ML1000239

1 reference

28 July 2017

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28 July 2017

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