Delving into the Latest Updates on Carcinotech Ltd. with Synapse

Overview

Tags

Urogenital Diseases

Endocrinology and Metabolic Disease

Neoplasms

Small molecule drug

Disease domain score

A glimpse into the focused therapeutic areas

Technology Platform

Most used technologies in drug development

Targets

Most frequently developed targets

Disease Domain	Count

Neoplasms	6
Endocrinology and Metabolic Disease	6
Immune System Diseases	1
Hemic and Lymphatic Diseases	1

Top 5 Drug Type	Count

Small molecule drug	6

Top 5 Target	Count

CKAP4(cytoskeleton associated protein 4)	6

While some plant-derived polyphenolic compounds exhibit anticancer activity, their complex mechanism of action is generally hindering the efforts to produce clinically useful derivatives. Here we present several compounds that are, to the best of our knowledge, the first known inhibitors of cytoskeleton associated protein 4 (CKAP4) a transmembrane protein associated with resilient forms of cancer. Since CKAP4 is overexpressed in ovarian cancer the compounds were evaluated in the experimental models below as proof of concept.Target deconvolution using CETSA was followed by spectral shift binding, TRIC and ITC validation. In vitro studies assessed anti-proliferative activity (ATPLite, Revvity), with Oncolines Profiler analysis comparing the IC50 fingerprints with those of 213 pre-profiled reference drugs. Bioprinted human tissue organoids tested the efficacy of the new chemical entities. Tumor microenvironment characterization was performed using immunofluorescence imaging.From our proprietary physical library of 400 new chemical entities SND 106, 108, 562, 581, 584 and 586 were selected based on their strong binding to CKAP4. They were highly active in the ovarian and endometrial cell lines: PA-1, ES-2, AN3-CA, OVCAR-3 with IC50s in the low nanomolar range. Furthermore, the results of the organoid assays showed a significantly improved efficacy of the new compounds compared with the standard of care drug carboplatin.Novel, first-in-class small molecules inhibitors of CKAP4 were discovered, showing strong antitumor activity in ovarian and endometrial cancer. Future studies will determine whether they can be developed into new drugs.Citation Format:Eugenio Gaudio, Viktor Ivasishin, Paulina Biniecka, Christian Kleusch, Cosimo Kropp, Benjamin Zimmer, Kamilla Pawlicka, Helena Almqvist, Alexey Chernobrovkin, Janneke Melis, Guido Zaman, Dan F. Stoicescu. Discovery of first in class, polyphenolic inhibitors of CKAP4 and their antitumor activity in ovarian and endometrial cancer [abstract]. In: Proceedings of the American Association for Cancer Research Annual Meeting 2025; Part 1 (Regular Abstracts); 2025 Apr 25-30; Chicago, IL. Philadelphia (PA): AACR; Cancer Res 2025;85(8_Suppl_1):Abstract nr 4273.

100 Deals associated with Carcinotech Ltd.

Login to view more data

100 Translational Medicine associated with Carcinotech Ltd.

Login to view more data

Corporation Tree

Boost your research with our corporation tree data.

login

or

view full example data

Boost your research with our corporation tree data.

Pipeline

Pipeline Snapshot as of 12 May 2025

The statistics for drugs in the Pipeline is the current organization and its subsidiaries are counted as organizations,Early Phase 1 is incorporated into Phase 1, Phase 1/2 is incorporated into phase 2, and phase 2/3 is incorporated into phase 3

Preclinical

6

Login to view more data

Current Projects

Drug(Targets)	Indications	Global Highest Phase

SND 581 ( CKAP4 )	Endometrial Carcinoma More	Preclinical
SND 108 ( CKAP4 )	Endometrial Carcinoma More	Preclinical
SND 106 ( CKAP4 )	Ovarian Cancer More	Preclinical
SND-562 ( CKAP4 )	Endometrial Carcinoma More	Preclinical
SND 586 ( CKAP4 )	Endometrial Carcinoma More	Preclinical