Design, Synthesis, and Testing of Potent, Selective Hepsin Inhibitors via Application of an Automated Closed-Loop Optimization Platform-Reference-Cited by-同舟云学术

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Design, Synthesis, and Testing of Potent, Selective Hepsin Inhibitors via Application of an Automated Closed-Loop Optimization Platform

Published:2018-04-27 Issue:10 Volume:61 Page:4335-4347
ISSN:0022-2623
Container-title:Journal of Medicinal Chemistry
language:en
Short-container-title:J. Med. Chem.

Author:

Pant Shishir M.¹,Mukonoweshuro Amanda²,Desai Bimbisar²,Ramjee Manoj K.²,Selway Christopher N.²,Tarver Gary J.²,Wright Adrian G.²,Birchall Kristian³,Chapman Timothy M.³^ORCID,Tervonen Topi A.¹,Klefström Juha¹

Affiliation:

1. Cancer Cell Circuitry Laboratory, Research Programs Unit/Translational Cancer Biology & Medicum, University of Helsinki, P.O. Box 63, Haartmaninkatu 8, 00014 Helsinki, Finland

2. Cyclofluidic Ltd., Biopark, Broadwater Road, Welwyn Garden City, AL7 3AX, U.K.

3. LifeArc, Accelerator Building, Open Innovation Campus, Stevenage, SG1 2FX, U.K.

Funder

UCB

Biomedicum Helsinki-s??ti?

Tekes

Innovate UK

Pfizer

Sy?p?j?rjest?t

Suomen Akatemia

Helsingin Yliopisto

Helsinki Institute of Life Science, Helsingin Yliopisto

Publisher

American Chemical Society (ACS)

Subject

Drug Discovery,Molecular Medicine

Link

https://pubs.acs.org/doi/pdf/10.1021/acs.jmedchem.7b01698

Reference39 articles.

1. The Structure of the Extracellular Region of Human Hepsin Reveals a Serine Protease Domain and a Novel Scavenger Receptor Cysteine-Rich (SRCR) Domain

2. Delineation of prognostic biomarkers in prostate cancer

3. Deregulated hepsin protease activity confers oncogenicity by concomitantly augmenting HGF/MET signalling and disrupting epithelial cohesion

4. Tumor suppressor function of Liver kinase B1 (Lkb1) is linked to regulation of epithelial integrity

5. Clinical and Biological Significance of Hepsin Overexpression in Breast Cancer

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