Inhibition of the CDK9‒cyclin T1 protein‒protein interaction as a new approach against triple-negative breast cancer
Sha-Sha Cheng,Yuan-Qing Qu,Jia Wu,Guan-Jun Yang,Guan-Jun Yang,Hao Liu,Wanhe Wang,Wanhe Wang,Qi Huang,Feng Chen,Guodong Li,Chun-Yuen Wong,Vincent Kam Wai Wong,Dik-Lung Ma,Chung-Hang Leung +14 more
Reads0
Chats0
TLDR
In this paper, the authors designed and generated a library of metal complexes bearing the 7-chloro-2-phenylquinoline CˆN ligand and tested their activity against the CDK9-cyclin T1 PPI.About:
This article is published in Acta Pharmaceutica Sinica B.The article was published on 2021-10-30 and is currently open access. It has received 25 citations till now. The article focuses on the topics: Triple-negative breast cancer & Cancer research.read more
Citations
More filters
Journal ArticleDOI
Berberine as a potential agent for breast cancer therapy
Xiaoxiao Zhong,Li-Juan Chen,Xinran Xu,Yan-Jun Liu,Fan Tao,Ming H. Zhu,Chang Li,Dan Zhao,Guan-Jun Yang,Jiong Chen +9 more
TL;DR: The evidence for BBR in BC therapy is provided, its detailed underlying mechanism in BC treatment remains unclear, and the novel BBR-based therapeutic strategies against BC improve biocompatibility and water solubility.
Journal ArticleDOI
Identification of a cytisine-based EED-EZH2 protein-protein interaction inhibitor preventing metastasis in triple-negative breast cancer cells
Sha-Sha Cheng,Guan-Jun Yang,Wanhe Wang,Ying-Qi Song,Chung Ko,Quanbin Han,Dik-Lung Ma,Chung-Hang Leung +7 more
TL;DR: To the authors' knowledge, compound 1 is the first cytisine-based EED-EZH2 PPI inhibitor preventing metastasis in TNBC cells, and may provide a new avenue for the development of more efficacious E ED-EzH 2 PPI inhibitors in T NBC treatment.
Journal ArticleDOI
A state-of-the-art review on LSD1 and its inhibitors in breast cancer: Molecular mechanisms and therapeutic significance
Guan-Jun Yang,Yan-Jun Liu,Lixian Ding,Fan Tao,Ming H. Zhu,Zhenghao Shi,Juan Wen,Mengmeng Niu,Xia Li,Zhancong Xu,Chenjie Fei,Jiong Chen +11 more
TL;DR: This review will provide insight into the overview structure of LSD1, summarize its action mechanisms in BC, describe the therapeutic potential ofLSD1 inhibitors inBC, and prospect the current opportunities and challenges of targeting LSD1 for BC therapy.
Journal ArticleDOI
Targeting PGAM1 in cancer: An emerging therapeutic opportunity.
TL;DR: In this paper , the authors provide insights into structure, function, and regulation of PGAM1, summarizes its mechanism in tumorigenesis, and reviews the advanced status of the PGAM-1 inhibitors in cancer diagnosis and treatment.
Journal ArticleDOI
The anticancer and EGFR-TK/CDK-9 dual inhibitory potentials of new synthetic pyranopyrazole and pyrazolone derivatives: X-ray crystallography, in vitro, and in silico mechanistic investigations.
Arafa Musa,Saleh Ihmaid,David L. Hughes,Musa A. Said,Hamada S. Abulkhair,Ahmed H. El-Ghorab,Mohamed A. Abdelgawad,Khaled Shalaby,Mohamed E. Shaker,Khalid Saad Alharbi,Nasser Hadal Alotaibi,Deborah L. Kays,Laurence J. Taylor,Della Grace Thomas Parambi,Sami I. Alzarea,Ahmed A. Al-Karmalawy,Hany E.A. Ahmed,Ahmed M. El-Agrody +17 more
TL;DR: Sarma et al. as mentioned in this paper reported the synthesis of two new series of suggested anticancer molecules incorporating both heterocycles together with their characterization by IR, 1H NMR, 13C NMR-DEPT, and X-ray diffraction methods.
References
More filters
Journal ArticleDOI
Bipyridine: the most widely used ligand. A review of molecules comprising at least two 2,2'-bipyridine units.
Journal ArticleDOI
Mouse Models of Diabetic Nephropathy
Frank C. Brosius,Charles E. Alpers,Erwin P. Bottinger,Matthew D. Breyer,Thomas M. Coffman,Susan B. Gurley,Raymond C. Harris,Masao Kakoki,Matthias Kretzler,Edward H. Leiter,Moshe Levi,Richard A. McIndoe,Kumar Sharma,Oliver Smithies,Katalin Susztak,Nobuyuki Takahashi,Takamune Takahashi +16 more
TL;DR: This interim report and an online supplement detail the progress made toward a complete murine model of human diabetic kidney disease and the critical analysis of existing murine models, which substantially enhances the understanding of this disease process.
Journal ArticleDOI
Kinase-targeted cancer therapies: progress, challenges and future directions
Khushwant S. Bhullar,Naiara Orrego Lagarón,Eileen M. McGowan,Indu Parmar,Amitabh Jha,Basil P. Hubbard,H.P. Vasantha Rupasinghe +6 more
TL;DR: The human genome encodes 538 protein kinases that transfer a γ-phosphate group from ATP to serine, threonine, or tyrosine residues, which are the second most targeted group of drug targets, after the G-protein-coupled receptors.
Journal ArticleDOI
Targeting oncogenic Myc as a strategy for cancer treatment
Hui Chen,Hudan Liu,Guoliang Qing +2 more
TL;DR: Current strategies include indirectly targeting myc by inhibiting its regulation and stability, and interaction with its partner Max, which is necessary for its regulation of gene expression, which provides promise for effective therapeutics against myc-dependent cancers.
Journal ArticleDOI
Targeting cancer with kinase inhibitors
TL;DR: There are numerous prospects for the discovery of novel kinase targets, and cancer immunotherapy is explored as a new and promising research area for studying kinase biology.
Related Papers (5)
New CDK8 inhibitors as potential anti-leukemic agents - Design, synthesis and biological evaluation.
Design of Novel 3-Pyrimidinylazaindole CDK2/9 Inhibitors with Potent In Vitro and In Vivo Antitumor Efficacy in a Triple-Negative Breast Cancer Model
Umed Singh,Gousia Chashoo,Sameer U. Khan,Priya Mahajan,Amit Nargotra,Girish Badrinath Mahajan,Amarinder Singh,Anjna Sharma,Mubashir J. Mintoo,Santosh Kumar Guru,Hariprasad Aruri,Thanusha Thatikonda,Promod Kumar Sahu,Pankaj Chibber,Vikas Kumar,Sameer Ahmad Mir,Sonali S. Bharate,Sreedhar Madishetti,Utpal Nandi,Gurdarshan Singh,Dilip M. Mondhe,Shashi Bhushan,Fayaz Malik,Serge Mignani,Serge Mignani,Ram A. Vishwakarma,Parvinder Pal Singh +26 more