Evidence map›Paper›PMID 30637955›Full record

ArticleChemMedChem2019

Highly Selective and Potent Human β-Secretase 2 (BACE2) Inhibitors against Type 2 Diabetes: Design, Synthesis, X-ray Structure and Structure-Activity Relationship Studies.

Arun K Ghosh, Margherita Brindisi, Yu-Chen Yen, Emma K Lendy, Satish Kovela, Emilio Leal Cárdenas, Bhavanam Sekhara Reddy, Kalapala Venketeswara Rao, Deborah Downs, Xiangping Huang and 2 more

Abstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in ChemMedChem, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 10 papers.

0numbers the graph read from it
0cells of the map it votes in
10citing papers in PubMed
–field-weighted citation impact
1 · What the graph read from it

What it found

Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.

The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.

2 · The registry

The trial behind it

Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.

Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.

3 · Its place in the literature

Who cites it

10 citing papers in PubMed.

  1. Article
  2. Review
  3. Article
  4. Review
  5. Review
  6. Article
  7. The emerging role of β-secretases in cancer.Journal of experimental & clinical cancer research : CR · 2021
    Review
  8. Article
  9. Article
  10. Article
4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

12 authors.

Arun K GhoshDepartment of Chemistry and Department of Medicinal Chemistry and Molecular Pharmacology, Purdue University, West Lafayette, IN, 47907, USA.ORCID 0000-0003-2472-1841
Margherita BrindisiDepartment of Chemistry and Department of Medicinal Chemistry and Molecular Pharmacology, Purdue University, West Lafayette, IN, 47907, USA.
Yu-Chen YenDepartment of Biochemistry, Purdue University, West Lafayette, IN, 47907, USA.
Emma K LendyDepartment of Biochemistry, Purdue University, West Lafayette, IN, 47907, USA.
Satish KovelaDepartment of Chemistry and Department of Medicinal Chemistry and Molecular Pharmacology, Purdue University, West Lafayette, IN, 47907, USA.
Emilio Leal CárdenasDepartment of Chemistry and Department of Medicinal Chemistry and Molecular Pharmacology, Purdue University, West Lafayette, IN, 47907, USA.
Bhavanam Sekhara ReddyDepartment of Chemistry and Department of Medicinal Chemistry and Molecular Pharmacology, Purdue University, West Lafayette, IN, 47907, USA.
Kalapala Venketeswara RaoDepartment of Chemistry and Department of Medicinal Chemistry and Molecular Pharmacology, Purdue University, West Lafayette, IN, 47907, USA.
Deborah DownsProtein Studies Program, Oklahoma Medical Research Foundation, Department of Biochemistry and Molecular Biology, University of Oklahoma Health Science Center, Oklahoma City, OK, 73104, USA.
Xiangping HuangProtein Studies Program, Oklahoma Medical Research Foundation, Department of Biochemistry and Molecular Biology, University of Oklahoma Health Science Center, Oklahoma City, OK, 73104, USA.
Jordan TangProtein Studies Program, Oklahoma Medical Research Foundation, Department of Biochemistry and Molecular Biology, University of Oklahoma Health Science Center, Oklahoma City, OK, 73104, USA.
Andrew D MesecarDepartment of Biochemistry, Purdue University, West Lafayette, IN, 47907, USA.

Funding

Transgenic Mouse Core Facility Shared Resource (TMCF-SR)P30CA023168 · NCI · PURDUE UNIVERSITY WEST LAFAYETTE · PI ANDREW D MESECAR · 1985 to 2026
$43.4M
DESIGN AND SYNTHESIS OF NONPEPTIDE PROTEASE INHIBITORSR01GM053386 · NIGMS · UNIVERSITY OF ILLINOIS AT CHICAGO · PI GHOSH, ARUN K · 1995 to 2010
$3.7M
Design & Synthesis of Nonpeptide Protease InhibitorsR37AI150466 · NIAID · PURDUE UNIVERSITY · PI GHOSH, ARUN K · 2019 to 2020
$969k
NCI NIH HHS P30 CA023168NIAID NIH HHS R37 AI150466NIGMS NIH HHS R01 GM053386
6 · The paper itself

Abstract

Herein we present the design, synthesis, and biological evaluation of potent and highly selective β-secretase 2 (memapsin 1, beta-site amyloid precursor protein cleaving enzyme 2, or BACE 2) inhibitors. BACE2 has been recognized as an exciting new target for type 2 diabetes. The X-ray structure of BACE1 bound to inhibitor 2 a {N

Indexed as

Amyloid Precursor Protein SecretasesAspartic Acid EndopeptidasesBinding SitesCrystallography, X-RayDiabetes Mellitus, Type 2Drug Evaluation, PreclinicalEnzyme InhibitorsEthylaminesHumansHypoglycemic AgentsMolecular Docking SimulationMolecular StructureProtein BindingStructure-Activity RelationshipThermodynamicsAmyloid Precursor Protein SecretasesAspartic Acid EndopeptidasesBACE1 protein, humanBACE2 protein, humanEnzyme InhibitorsEthylaminesHypoglycemic AgentsBACE2 inhibitorsstructure-based designTmem27type 2 diabetesβ-secretase 2

Identifiers

PMID30637955
PMCPMC6637425

What Socratic holds

Textmetadata
LicenceTDM
Read underepoch 390

Registered trials

None linked

Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the Socratic graph.