Discovery of a novel CDK7 inhibitor YPN-005 in small cell lung cancer

Choi, Yun Jung; Lee, Hyeon-Jeong; Kim, Dasom; Kim, Dong Ha; Kang, Myounghee; Cho, Yong-Hee; Choi, Chang‐Min; Yoo, Jakyung; Lee, Kwang-Ok; Choi, Eun Kyung; Lee, Jae Cheol; Rho, Jin Kyung

doi:10.1016/j.ejphar.2021.174298

Cited by 19 publications

(15 citation statements)

References 22 publications

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“…YPN-005 (C 26 H 28 N 6 O 2 S) and SY1365 were kindly provided from Yungjin Pharm. Co., Ltd (Gyeonggi-do, Korea) ( Choi et al., 2021 ), venetoclax (cat. no.…”

Section: Methodsmentioning

confidence: 99%

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Antileukemic activity of YPN-005, a CDK7 inhibitor, inducing apoptosis through c-MYC and FLT3 suppression in acute myeloid leukemia

Koo

Choi

Hur

et al. 2022

Heliyon

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“…YPN-005 (C 26 H 28 N 6 O 2 S) and SY1365 were kindly provided from Yungjin Pharm. Co., Ltd (Gyeonggi-do, Korea) ( Choi et al., 2021 ), venetoclax (cat. no.…”

Section: Methodsmentioning

confidence: 99%

“…YPN-005, a highly selective CDK7 inhibitor, showed antiproliferative effects in primary sample and drug-resistant lung cancer ( Choi et al., 2021 ). Therefore, in this study, we explored the potential efficacy of YPN-005 in AML cell lines, mouse models, and primary cells from AML patients.…”

Section: Introductionmentioning

confidence: 99%

Antileukemic activity of YPN-005, a CDK7 inhibitor, inducing apoptosis through c-MYC and FLT3 suppression in acute myeloid leukemia

Koo

Choi

Hur

et al. 2022

Heliyon

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“…The mechanism of chemotherapy resistance is complex, and verifying the hypothesis in the new model is necessary [59]. Several compounds were tested in cisplatinresistant lung cancer PDO to restore chemosensitivity, such as YPN-005, which antagonizes CDK7, Solamargine, which blocks the hedgehog signaling pathway, and Halofuginone, which inhibits PI3K/AKT and MAPK signaling pathways [60][61][62].…”

Section: Clinical Research and Drug Screening Based On Lung Cancer Pdomentioning

confidence: 99%

The application of patient-derived organoid in the research of lung cancer

et al. 2023

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Lung cancer is the most common cancer and the leading cause of cancer-related death worldwide. However, mechanisms of its progression remained unclear and new treatments against this disease are rapidly emerging. As a novel preclinical model, patient-derived organoid (PDO) can also be established from the patient’s tumor tissue and cultured in the laboratory, which preserves the key biological characteristics of the original tumor. Compared to the patient-derived xenograft (PDX) model of lung cancer, the culture success rate is improved, and the time and cost of model establishment are largely reduced. PDO is also expected to provide a more individual model to predict the efficacy of anti-cancer treatment in vitro. This paper summarizes the current application of PDO in the translational research of lung cancer.

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“…Rather than the validation of existing drugs in LCOs, Choi et al developed a potent inhibitor of cyclin-dependent kinase 7 called YPN-005 and showed antiproliferative effects in various SCLC cell lines, including those acquiring resistance to cisplatin or etoposide and SCLC patient-derived organoids [59] , providing more robust support for further exploration of this new drug, even though it still requires much validation and further mechanistic research.…”

Section: Drug Screeningmentioning

confidence: 99%