Selective Inhibitor of Protein Kinase PKN3 Generated by Conjugation of a Structurally Optimized Bumped

Varvara Smorodina, Eva Lea Jääger, Tanel Sõrmus, Ernesto De Jesus Zapata Flores, Erki Enkvist, Asko Uri, Kaido Viht

Abstract read

In one paragraph

Article in Molecules (Basel, Switzerland), 2026. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.

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0 citing papers in PubMed.

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4 · The record

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5 · Who and what money

Authors and funding

7 authors.

Varvara SmorodinaInstitute of Chemistry, University of Tartu, 14A Ravila St., 50411 Tartu, Estonia.ORCID 0000-0003-1635-8886

Eva Lea JäägerInstitute of Chemistry, University of Tartu, 14A Ravila St., 50411 Tartu, Estonia.ORCID 0009-0006-8924-8492

Tanel SõrmusInstitute of Chemistry, University of Tartu, 14A Ravila St., 50411 Tartu, Estonia.ORCID 0000-0001-7238-235X

Ernesto De Jesus Zapata FloresInstitute of Chemistry, University of Tartu, 14A Ravila St., 50411 Tartu, Estonia.ORCID 0000-0002-8802-5071

Erki EnkvistInstitute of Chemistry, University of Tartu, 14A Ravila St., 50411 Tartu, Estonia.ORCID 0000-0001-7375-3765

Asko UriInstitute of Chemistry, University of Tartu, 14A Ravila St., 50411 Tartu, Estonia.ORCID 0000-0001-5436-2427

Kaido VihtInstitute of Chemistry, University of Tartu, 14A Ravila St., 50411 Tartu, Estonia.ORCID 0000-0002-0359-7426

Funding

Estonian Center of Analytical Chemistry TARISTU24-TK15Estonian Research Council PRG454Institute of chemistry, University of Tartu PLTKTARENG21

6 · The paper itself

Abstract

The protein kinase N family belongs to the AGC kinase group and contains three isozymes: PKN1, PKN2, and PKN3. Catalytic domains of PKNs share high sequence similarity, yet the proteins differ in tissue distribution, functions, and involvement in pathological processes. In particular, PKN3 has been implicated in tumor growth and metastatic progression, highlighting the need for isozyme-selective inhibitors as both research tools and therapeutic leads. Here, we report the rational design of selective PKN3 inhibitors based on distinctive structural features of this kinase. Two strategies were applied. First, the smaller threonine gatekeeper residue unique to PKN3 within the AGC group was exploited by derivatization of

Indexed as

ArginineIsoquinolinesProtein Kinase InhibitorsSulfonamidesHumansProtein Kinase CStructure-Activity RelationshipArginineIsoquinolinesProtein Kinase CProtein Kinase Inhibitorsprotein kinase NSulfonamidesgatekeeper residueprotein kinase PKN3selective inhibitor

Identifiers

PMID41752364

DOI10.3390/molecules31040585

PMCPMC12942868

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LicenceCC BY

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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 OpenQuestion graph.