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Last update 08 May 2025

HASPIN

Last update 08 May 2025

Basic Info

Synonyms

germ cell associated 2 (haspin), Germ cell-specific gene 2 protein, GSG2

+ [5]

Introduction

Serine/threonine-protein kinase that phosphorylates histone H3 at 'Thr-3' (H3T3ph) during mitosis. May act through H3T3ph to both position and modulate activation of AURKB and other components of the chromosomal passenger complex (CPC) at centromeres to ensure proper chromatid cohesion, metaphase alignment and normal progression through the cell cycle.

Drugs associated with HASPIN

FM-301(Future Medicine)

Target

HASPIN

Mechanism

HASPIN inhibitors

Active Org.

Future Medicine Co., Ltd.

Originator Org.

Future Medicine Co., Ltd.

Active Indication

Pancreatic Cancer

Inactive Indication-

Drug Highest PhasePreclinical

First Approval Ctry. / Loc.-

First Approval Date20 Jan 1800

HSK-205

Target

FLT3 x HASPIN

Mechanism

FLT3 inhibitors [+1]

Active Org.

Purdue University

Originator Org.

Purdue University

Active Indication

Acute Myeloid Leukemia

Inactive Indication-

Drug Highest PhasePreclinical

First Approval Ctry. / Loc.-

First Approval Date20 Jan 1800

LDN-1929660

Target

HASPIN

Mechanism

HASPIN inhibitors

Active Org.

University of Basilicata

Originator Org.

University of Basilicata

Active Indication

Neoplasms

Inactive Indication-

Drug Highest PhaseDiscovery

First Approval Ctry. / Loc.-

First Approval Date20 Jan 1800

100 Clinical Results associated with HASPIN

100 Translational Medicine associated with HASPIN

0 Patents (Medical) associated with HASPIN

187

Literatures (Medical) associated with HASPIN

01 Jun 2025·Bioorganic & Medicinal Chemistry

Synthesis and biological activity of 1H-pyrrolo[3,2-g]isoquinolines as Haspin kinase inhibitors

Article

Author: Josselin, Béatrice ; Giraud, Francis ; Moreau, Pascale ; Malosse, Killian ; Anizon, Fabrice ; Ruchaud, Sandrine ; Robert, Thomas ; Doula, Marie Ben

Based on previous results, new 1H-pyrrolo[3,2-g]isoquinolines were synthesized and evaluated for their ability to inhibit Haspin. Considering that analogues methylated at the indole nitrogen could retain their Haspin inhibitory potency, conjugates that could be suitable for a use in a PROTAC approach were prepared by N-alkylation. In addition, based on the Haspin inhibitory potency of 1H-pyrrolo[3,2-g]isoquinoline-3-carbaldehyde analogue, an additional PROTAC candidate was synthesized by carbonylation at the 3-position. Unfortunately, none of these conjugates exhibited Haspin inhibitory potency. Nevertheless, N-methylated derivative 10 bearing a pyridin-4-yl substituent at the 3-position is the best selective Haspin inhibitor identified to date in these series, with an IC₅₀ value of 23.6 nM and a selectivity index superior to 14 compared to other protein kinases tested. Additionally, this compound showed both interesting effects on cell viability of various human cell lines and significant inhibitory properties on cellular Haspin kinase.

02 Jan 2025·Angewandte Chemie International Edition

Thieno[3,2‐b]pyridine: Attractive scaffold for highly selective inhibitors of underexplored protein kinases with variable binding mode

Article

Author: Kubina, Tadeáš ; Souček, Karel ; Knapp, Stefan ; Chaikuad, Apirat ; Paruch, Kamil ; Skočková, Veronika ; Krämer, Andreas ; Moyano, Paula Martín ; Suchánková, Tereza ; Šmída, Michal ; Kuster, Bernhard ; Jarošková, Aneta ; Paruch, Štěpán Owen ; Ovesná, Petra ; Prokofeva, Polina ; Novotný, Jan

AbstractProtein kinases are key regulators of numerous biological processes and aberrant kinase activity can cause various diseases, particularly cancer. Herein, we report the identification of new series of highly selective kinase inhibitors based on the thieno[3,2‐b]pyridine scaffold. The weak interaction of the thieno[3,2‐b]pyridine core with the kinase hinge region allows for profoundly different binding modes all of which maintain high kinome‐wide selectivity, as illustrated by the isomers MU1464 and MU1668. Thus, this core structure provides a template of ATP‐competitive but not ATP‐mimetic inhibitors that are anchored at the kinase back pocket. Mapping the chemical space around the central thieno[3,2‐b]pyridine pharmacophore afforded highly selective inhibitors of the kinase Haspin, exemplified by the compound MU1920 that fulfils criteria for a quality chemical probe and is suitable for use in in vivo applications. However, despite the role of Haspin in mitosis, the inhibition of Haspin alone was not sufficient to elicit cytotoxic effect in cancer cells. The thieno[3,2‐b]pyridine scaffold can be used in a broader context, as a basis of inhibitors targeting other underexplored protein kinases, such as CDKLs.

31 Dec 2024·Nucleus

Nuclear functions regulated by the VRK1 kinase

Review

Author: Lazo, Pedro A.

In the nucleus, the VRK1 Ser-Thr kinase is distributed in nucleoplasm and chromatin, where it has different roles. VRK1 expression increases in response to mitogenic signals. VRK1 regulates cyclin D1 expression at G0 exit and facilitates chromosome condensation at the end of G2 and G2/M progression to mitosis. These effects are mediated by the phosphorylation of histone H3 at Thr3 by VRK1, and later in mitosis by haspin. VRK1 regulates the apigenetic patterns of histones in processes requiring chromating remodeling, such as transcription, replication and DNA repair. VRK1 is overexpressed in tumors, facilitating tumor progression and resistance to genotoxic treatments. VRK1 also regulates the organization of Cajal bodies assembled on coilin, which are necessary for the assembly of different types of RNP complexes. VRK1 pathogenic variants cuase defects in Cajal bodies, functionally altering neurons with long axons and leading to neurological diseases, such as amyotrophic laterla sclerosis, spinal muscular atrophy, distal hereditay motor neuropathies and Charcot-Marie-Tooth.

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