Evidence map›Paper›PMID 42473948›Full record

ArticleActa crystallographica. Section D, Structural biology2026

Structural basis for a p21-activated kinase 4 and nicotinamide phosphoribosyltransferase dual inhibitor.

Jaehui Park, Hye Rim Hong, Sang Hyun Han, Jinsue Song, Se Young Son, Saehae Choi, Sang Mi Park, Won Kyu Lee, Chimari Jiko, Ji Hun Kim and 4 more

Abstract read
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In one paragraph

Article in Acta crystallographica. Section D, Structural biology, 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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0citing papers in PubMed
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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

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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

0 citing papers in PubMed.

No citing paper in PubMed yet.

4 · The record

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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

14 authors.

Jaehui ParkCollege of Pharmacy, Chungbuk National University, Chungbuk 28160, South Korea.ORCID 0000-0003-1791-8937
Hye Rim HongNew Drug Development Center, Osong Medical Innovation Foundation, Osong Cheongju, Chungbuk 28160, South Korea.
Sang Hyun HanCollege of Pharmacy, Chungbuk National University, Chungbuk 28160, South Korea.
Jinsue SongCollege of Pharmacy, Chungbuk National University, Chungbuk 28160, South Korea.
Se Young SonCollege of Pharmacy, Chungbuk National University, Chungbuk 28160, South Korea.
Saehae ChoiNew Drug Development Center, Osong Medical Innovation Foundation, Osong Cheongju, Chungbuk 28160, South Korea.
Sang Mi ParkCollege of Pharmacy, Chungbuk National University, Chungbuk 28160, South Korea.
Won Kyu LeeClinical Research Center, Masan National Tuberculosis Hospital, Changwon 51755, South Korea.ORCID 0000-0003-4040-1100
Chimari JikoDivision of Radiation Life Science, Institute for Integrated Radiation and Nuclear Science, Kyoto University, Osaka, Japan.ORCID 0009-0009-9880-9804
Ji Hun KimCollege of Pharmacy, Chungbuk National University, Chungbuk 28160, South Korea.
Jun Goo JeeResearch Institute of Pharmaceutical Researches, College of Pharmacy, Kyungpook National University, Daegu 41566, South Korea.
Jeong Kyu BangDivision of Magnetic Resonance, Korea Basic Science Institute (KBSI), Ochang, Chungbuk 28119, South Korea.
Il Yeong ParkCollege of Pharmacy, Chungbuk National University, Chungbuk 28160, South Korea.ORCID 0000-0002-5246-5243
Soo Jae LeeCollege of Pharmacy, Chungbuk National University, Chungbuk 28160, South Korea.ORCID 0000-0002-5524-9802

Funding

Chungbuk National University 2019 Research Year ProgramMinistry of Education 2025-RISE-11-014-05
6 · The paper itself

Abstract

Simultaneous inhibition of oncogenic signaling and metabolic pathways represents a promising approach for cancer therapy. KPT-9274, a clinical stage compound, has been reported as a dual inhibitor of p21-activated kinase 4 (PAK4) and nicotinamide phosphoribosyltransferase (NAMPT), but its structural basis has remained undefined. Here, we present high-resolution crystal structures of PAK4 and NAMPT in complex with KPT-7523, an analog of KPT-9274, determined at 2.20 and 1.45 Å resolution, respectively. In PAK4, the 2-aminopyridine moiety of KPT-7523 enables dual binding, occupying the adenine-binding site for ATP and simultaneously engaging the substrate-binding cleft in the C-lobe, thereby interfering with both catalytic and regulatory functions. In NAMPT, the same scaffold inserts into the NAD

Indexed as

AcrylamidesAminopyridinesCytokinesEnzyme InhibitorsNicotinamide Phosphoribosyltransferasep21-Activated KinasesProtein Kinase InhibitorsCatalytic DomainCrystallography, X-RayHumansModels, MolecularAcrylamidesAminopyridinesCytokinesEnzyme InhibitorsKPT-9274Nicotinamide Phosphoribosyltransferasenicotinamide phosphoribosyltransferase, humanp21-Activated KinasesPAK4 protein, humanProtein Kinase Inhibitors2-aminopyridine pharmacophoredual inhibitionKPT-7523NAMPTPAK4

Identifiers

PMID42473948
PMCPMC13431643

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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.