4-1BB agonists(Tumor necrosis factor receptor superfamily member 9 agonists), MSLN inhibitors(Mesothelin inhibitors), ADCC(Antibody-dependent cell-mediated cytotoxicity (ADCC) effects)

+ [1]

Therapeutic Areas

Neoplasms

Active Indication

Solid tumor

Inactive Indication-

Originator Organization

Hefei Hankemaibo Biotechnology Co., Ltd.

Active Organization

Hefei Hankemaibo Biotechnology Co., Ltd.

Inactive Organization-

Drug Highest PhasePreclinical

First Approval Date-

Regulation-

100 Clinical Results associated with HK-013

100 Translational Medicine associated with HK-013

100 Patents (Medical) associated with HK-013

Literatures (Medical) associated with HK-013

27 May 2022·The Journal of BiochemistryQ4 · BIOLOGY

Hybrid molecule between platanic acid and LCL-161 as a yes-associated protein degrader

Q4 · BIOLOGY

Article

Author: Yamazaki, Ryu ; Fukuda, Kazuo ; Okamoto, Iwao ; Itoh, Susumu ; Watanabe, Misao ; Ishikawa, Haruka ; Mori, Alice ; Tashiro, Etsu ; Nakano, Naoko ; Nagano, Waka ; Nakane, Takahisa ; Kawamoto, Rie ; Naito, Mikihiko

AbstractDysregulated yes-associated protein (YAP) is involved in several malignant cancers. However, discovering a druggable YAP inhibitor(s) is difficult because YAP itself does not have any enzymatic activity. In such cases, targeted protein degradation strategies based on hybrid molecules that bind to the target protein and an E3 ubiquitin ligase are useful for suppressing proteins that exhibit aberrant activation and/or excessive expression. Upon screening YAP-interacting small compounds, we identified HK13, a platanic acid, as a novel compound that interacts with YAP. Next, we synthesized hybrid compounds of platanic acid and LCL-161, which reportedly shows a high affinity for cIAP, one of E3 ubiquitin ligases. Among these compounds, HK24 possessed the ability to inhibit the growth of YAP overexpressing NCI-H290 cells. This inhibitory activity may be mediated by YAP degradation, although HK24 exhibited weak YAP degradation. Furthermore, we confirmed involvement of proteasome pathway in HK24-dependent YAP degradation by culturing NCI-H290 cells in the presence of a proteasome inhibitor. Therefore, it is possible that platanic acid is a potential candidate for molecular medicine targeting YAP.

01 Oct 2020·Bioorganic & Medicinal Chemistry LettersQ4 · MEDICINE

Anti-proliferative potential of triphenyl substituted pyrimidines against MDA-MB-231, HCT-116 and HT-29 cancer cell lines

Q4 · MEDICINE

Article

Author: Ranjan Dwivedi, Ashish ; Kumar, Naveen ; Kumar, Vijay ; Kumar, Vinod ; Poduri, Ramarao ; Prakash Yadav, Ravi ; Kaur, Harmeet ; Baranwal, Somesh

A series of triphenyl substituted pyrimidines as analogous of colchicine and combretastatin A-4 was synthesized and evaluated for the antiproliferative potential. The compounds were screened against MDA-MB-231, HCT-116 and HT-29 cell lines using MTT assay. Most of the compounds displayed antiproliferative activity in low to sub micro molar concentration. Amongst the synthesized derivatives, compounds HK-2, HK-10 and HK-13 were found to be effective against all the three cancer cell lines. HK-2 exhibited IC₅₀ values of 3.39 µM, 4.78 µM and 4.23 µM, HK-10 showed IC₅₀ values of 0.81 µM, 5.89 µM, 4.96 µM and HK-13 showed IC₅₀ values 3.24 µM, 4.93 µM and 4.73 µM against MDA-MB-231, HCT-116 and HT-29 cancer cell lines, respectively. HK-10 was found to be the most potent compound in the series with IC₅₀ values of 0.81 µM against MDA-MB-231. In the cell cycle analysis, HK-2 and HK-10 showed cell arrest at G2/M phase of the cell cycle while HK-13 inhibited cell growth at the G1/G0 phase. All the three compounds showed cell death induced through apoptosis. In the docking studies, HK-2, HK-10 and HK-13 were found to fit well in the colchicine binding site of the tubulin. Some of the compounds in the current series were found to be promising against all the three cancer cell lines and may act as potent leads for further development.

01 Oct 2007·Neuroscience LettersQ4 · MEDICINE

Blocking actions of alkylene-tethered bis-neonicotinoids on nicotinic acetylcholine receptors expressed by terminal abdominal ganglion neurons of Periplaneta americana

Q4 · MEDICINE

Article

Author: Shinzo Kagabu ; Chiharu Ishida ; Kazuhiko Matsuda ; Makoto Ihara ; Koichi Hirata

Neonicotinoid insecticides target nicotinic acetylcholine receptors (nAChRs), which, in both vertebrates and invertebrates, mediate fast-acting synaptic neurotransmission in the nervous system. Recently, Kagabu et al. synthesized bis-neonicotinoids. The neural activities of bis-neonicotinoids have been evaluated on the central nerve cord of American cockroaches. However, the action of bis-neonicotinoids on nAChRs expressed by dissociated insect neurons has not yet been studied. Thus, the actions of several alkylene-tethered bis-neonicotinoids on the terminal abdominal ganglion neurons of the American cockroach, Periplaneta americana, were investigated using whole-cell patch-clamp electrophysiology. All of the ligands tested did not induce membrane currents, but reduced the responses to ACh when bath applied prior to co-application with ACh. Of the compounds tested, HK-13, which possesses two imidacloprid units linked with a hexamethylene bridge, had the highest antagonist potency. The antagonist action was reduced, not only by elongating, but also by shortening the linker.

100 Deals associated with HK-013

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Indication	Highest Phase	Country/Location	Organization	Date
Solid tumor	Preclinical	China	Hefei Hankemaibo Biotechnology Co., Ltd.	-

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