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Article ; Online: A sulfhydryl blocking reagent BT-4 sensitizes cisplatin-based micelle prodrugs for efficient treatment of breast cancer.

Lin, Congcong / Chen, Yuxiu / Zhu, Mengli / Pei, Junping / Zhou, Yang / Gou, Maling / Ouyang, Liang

2022 Volume 626, Page(s) 122187

Abstract: Detoxification of glutathione (GSH) and insufficient cellular uptake of cisplatin (CDDP) severely compromised the therapeutic efficacy of CDDP. Here, a nano-delivery system (BT-4@PtPPNPs) for CDDP prodrug (C16-Pt(Ⅳ)-PEG) based on a novel sulfhydryl ... ...

Abstract	Detoxification of glutathione (GSH) and insufficient cellular uptake of cisplatin (CDDP) severely compromised the therapeutic efficacy of CDDP. Here, a nano-delivery system (BT-4@PtPPNPs) for CDDP prodrug (C16-Pt(Ⅳ)-PEG) based on a novel sulfhydryl blocking reagent methyl 2-(methylsulfonyl) benzothiazole-6-carboxylate (BT-4) was developed. On the one hand, BT-4 can deplete GSH in tumor cells by directly interacting with reactive sulfhydryl group on GSH, thereby increasing the cytotoxicity of CDDP. On the other hand, the CDDP prodrug carrier C16-Pt(IV)-PEG can promote the distribution of CDDP in tumors, reduce the probability of unexpected inactivation of CDDP, and reduce the content of GSH in tumor cells during the conversion to CDDP, thereby making CDDP more effective for treatment. The results showed that the optimized BT-4@PtPPNPs with a small particle size (130 nm) exhibited notable cytotoxicity and apoptosis of 4T1 cells. BT-4@PtPPNPs not only significantly improved the uptake of drugs by tumor cells, but also rapidly targeted and accumulated in the tumors for a long time. Moreover, in vivo efficacy studies showed that BT-4@PtPPNPs could effectively inhibit tumor growth, inhibiting 60.85 % of tumors in a 4T1 breast cancer mice model, showing superior antitumor activity, which can be attributed to GSH-triggered CDDP tolerance reversal. Overall, this study provides an attractive and simple strategy to combine novel sulfhydryl blockers and CDDP prodrugs to potentiate the efficacy of CDDP in breast cancer.
MeSH term(s)	Animals ; Antineoplastic Agents/pharmacology ; Antineoplastic Agents/therapeutic use ; Benzothiazoles ; Cell Line, Tumor ; Cisplatin/pharmacology ; Cisplatin/therapeutic use ; Glutathione ; Mice ; Micelles ; Neoplasms/drug therapy ; Prodrugs/pharmacology ; Prodrugs/therapeutic use
Chemical Substances	Antineoplastic Agents ; Benzothiazoles ; Micelles ; Prodrugs ; Glutathione (GAN16C9B8O) ; Cisplatin (Q20Q21Q62J)
Language	English
Publishing date	2022-09-12
Publishing country	Netherlands
Document type	Journal Article
ZDB-ID	428962-6
ISSN	1873-3476 ; 0378-5173
ISSN (online)	1873-3476
ISSN	0378-5173
DOI	10.1016/j.ijpharm.2022.122187
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Article ; Online: Design, Synthesis, and Biological Evaluation of Dual Inhibitors of EGFR

Wang, Aoxue / Shuai, Wen / Wu, Chengyong / Pei, Junping / Yang, Panpan / Wang, Xin / Li, Shutong / Liu, Jiaxi / Wang, Yuxi / Wang, Guan / Ouyang, Liang

Journal of medicinal chemistry

2024 Volume 67, Issue 4, Page(s) 2777–2801

Abstract: Activation of the alternative pathways and abnormal signaling transduction are frequently observed in third-generation EGFR-TKIs (epidermal growth factor receptor tyrosine kinase inhibitors)-resistant patients. Wherein, hyperphosphorylation of ACK1 ... ...

Abstract	Activation of the alternative pathways and abnormal signaling transduction are frequently observed in third-generation EGFR-TKIs (epidermal growth factor receptor tyrosine kinase inhibitors)-resistant patients. Wherein, hyperphosphorylation of ACK1 contributes to EGFR-TKIs acquired resistance. Dual inhibition of EGFR
MeSH term(s)	Humans ; Animals ; Mice ; Carcinoma, Non-Small-Cell Lung/pathology ; Lung Neoplasms/pathology ; ErbB Receptors/metabolism ; Drug Resistance, Neoplasm ; Mutation ; Protein Kinase Inhibitors/pharmacology ; Protein Kinase Inhibitors/therapeutic use ; Protein Kinase Inhibitors/chemistry ; Cell Line, Tumor ; Acrylamides ; Aniline Compounds ; Indoles ; Pyrimidines
Chemical Substances	osimertinib (3C06JJ0Z2O) ; ErbB Receptors (EC 2.7.10.1) ; Protein Kinase Inhibitors ; EGFR protein, human (EC 2.7.10.1) ; Acrylamides ; Aniline Compounds ; Indoles ; Pyrimidines
Language	English
Publishing date	2024-02-07
Publishing country	United States
Document type	Journal Article
ZDB-ID	218133-2
ISSN	1520-4804 ; 0022-2623
ISSN (online)	1520-4804
ISSN	0022-2623
DOI	10.1021/acs.jmedchem.3c01934
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Article ; Online: Asymmetric organocatalytic multicomponent reactions for efficient construction of bicyclic compounds bearing bisacetal and isoxazolidine moieties.

Pei, Jun-Ping / Lv, Xue-Jiao / Peng, Chen-Jun / Liu, Yan-Kai

Chemical communications (Cambridge, England)

2020 Volume 56, Issue 84, Page(s) 12765–12768

Abstract: An organocatalytic multicomponent reaction of N-protected hydroxylamines, acrylaldehyde and acetal-containing enones was developed. Bisacetal-containing bicyclic isoxazolidine derivatives bearing four continuous stereocenters were formed with excellent ... ...

Abstract	An organocatalytic multicomponent reaction of N-protected hydroxylamines, acrylaldehyde and acetal-containing enones was developed. Bisacetal-containing bicyclic isoxazolidine derivatives bearing four continuous stereocenters were formed with excellent stereoselectivities. A plausible reaction pathway was proposed based on
Language	English
Publishing date	2020-09-23
Publishing country	England
Document type	Journal Article
ZDB-ID	1472881-3
ISSN	1364-548X ; 1359-7345 ; 0009-241X
ISSN (online)	1364-548X
ISSN	1359-7345 ; 0009-241X
DOI	10.1039/d0cc05099g
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Article ; Online: Targeting Lysosomal Degradation Pathways: New Strategies and Techniques for Drug Discovery.

Pei, Junping / Wang, Guan / Feng, Lu / Zhang, Jifa / Jiang, Tingting / Sun, Qiu / Ouyang, Liang

Journal of medicinal chemistry

2021 Volume 64, Issue 7, Page(s) 3493–3507

Abstract: A series of tools for targeted protein degradation are inspiring scientists to develop new drugs with advantages over traditional small-molecule drugs. Among these tools, proteolysis-targeting chimeras (PROTACs) are most representative of the technology ... ...

Abstract	A series of tools for targeted protein degradation are inspiring scientists to develop new drugs with advantages over traditional small-molecule drugs. Among these tools, proteolysis-targeting chimeras (PROTACs) are most representative of the technology based on proteasomes. However, the proteasome has little degradation effect on certain macromolecular proteins or aggregates, extracellular proteins, and organelles, which limits the application of PROTACs. Additionally, lysosomes play an important role in protein degradation. Therefore, lysosome-induced protein degradation drugs can directly regulate protein levels
MeSH term(s)	Amino Acid Sequence ; Animals ; Autophagosomes/metabolism ; Autophagy/drug effects ; Drug Discovery/methods ; Endocytosis/physiology ; Humans ; Lysosomes/metabolism ; Peptides/chemistry ; Peptides/pharmacology ; Protein Binding ; Proteolysis/drug effects ; Receptor, IGF Type 2/metabolism
Chemical Substances	IGF2R protein, human ; Peptides ; Receptor, IGF Type 2
Language	English
Publishing date	2021-03-25
Publishing country	United States
Document type	Journal Article ; Research Support, Non-U.S. Gov't ; Review
ZDB-ID	218133-2
ISSN	1520-4804 ; 0022-2623
ISSN (online)	1520-4804
ISSN	0022-2623
DOI	10.1021/acs.jmedchem.0c01689
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Article: Asymmetric organocatalytic multicomponent reactions for efficient construction of bicyclic compounds bearing bisacetal and isoxazolidine moieties

Pei, Jun-Ping / Lv, Xue-Jiao / Peng, Chen-Jun / Liu, Yan-Kai

Chemical communications. 2020 Oct. 22, v. 56, no. 84

2020

Abstract	An organocatalytic multicomponent reaction of N-protected hydroxylamines, acrylaldehyde and acetal-containing enones was developed. Bisacetal-containing bicyclic isoxazolidine derivatives bearing four continuous stereocenters were formed with excellent stereoselectivities. A plausible reaction pathway was proposed based on ¹⁸O-labeling control experiments.
Keywords	acrolein ; catalytic activity ; chemical communication ; moieties ; stereoselectivity
Language	English
Dates of publication	2020-1022
Size	p. 12765-12768.
Publishing place	The Royal Society of Chemistry
Document type	Article
ZDB-ID	1472881-3
ISSN	1364-548X ; 1359-7345 ; 0009-241X
ISSN (online)	1364-548X
ISSN	1359-7345 ; 0009-241X
DOI	10.1039/d0cc05099g
Database	NAL-Catalogue (AGRICOLA)

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Article ; Online: Asymmetric Organocatalytic Sequential Reaction of Structurally Complex Cyclic Hemiacetals and Functionalized Nitro-olefins To Synthesize Diverse Heterocycles.

Pei, Jun-Ping / Chen, Ying-Han / Liu, Yan-Kai

Organic letters

2018 Volume 20, Issue 12, Page(s) 3609–3612

Abstract: Structurally complex cyclic hemiacetals bearing a racemic tetrasubstituted stereocenter have been prepared in a concise manner and were successfully used in an organocatalytic enantioselective sequence to react with functionalized nitro-olefins, ... ...

Abstract	Structurally complex cyclic hemiacetals bearing a racemic tetrasubstituted stereocenter have been prepared in a concise manner and were successfully used in an organocatalytic enantioselective sequence to react with functionalized nitro-olefins, providing bicyclic acetal-containing compounds as two separable epimers with excellent stereoselectivity. The reaction showed broad substrate scope, with respect to the starting hemiacetals. Moreover, this protocol allows the synthetic transformation of the products to various interesting heterocyclic compounds with substantial structural diversity and broad functionality.
Language	English
Publishing date	2018--15
Publishing country	United States
Document type	Journal Article ; Research Support, Non-U.S. Gov't
ISSN	1523-7052
ISSN (online)	1523-7052
DOI	10.1021/acs.orglett.8b01386
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Article: Development of small molecule extracellular signal-regulated kinases (ERKs) inhibitors for cancer therapy.

Pan, Xiaoli / Pei, Junping / Wang, Aoxue / Shuai, Wen / Feng, Lu / Bu, Faqian / Zhu, Yumeng / Zhang, Lan / Wang, Guan / Ouyang, Liang

Acta pharmaceutica Sinica. B

2022 Volume 12, Issue 5, Page(s) 2171–2192

Abstract: The mitogen-activated protein kinase (MAPK)/extracellular signal-regulated kinase 1/2 (ERK1/2) signaling pathway is widely activated by a variety of extracellular stimuli, and its dysregulation is associated with the proliferation, invasion, and ... ...

Abstract	The mitogen-activated protein kinase (MAPK)/extracellular signal-regulated kinase 1/2 (ERK1/2) signaling pathway is widely activated by a variety of extracellular stimuli, and its dysregulation is associated with the proliferation, invasion, and migration of cancer cells. ERK1/2 is located at the distal end of this pathway and rarely undergoes mutations, making it an attractive target for anticancer drug development. Currently, an increasing number of ERK1/2 inhibitors have been designed and synthesized for antitumor therapy, among which representative compounds have entered clinical trials. When ERK1/2 signal transduction is eliminated, ERK5 may provide a bypass route to rescue proliferation, and weaken the potency of ERK1/2 inhibitors. Therefore, drug research targeting ERK5 or based on the compensatory mechanism of ERK5 for ERK1/2 opens up a new way for oncotherapy. This review provides an overview of the physiological and biological functions of ERKs, focuses on the structure-activity relationships of small molecule inhibitors targeting ERKs, with a view to providing guidance for future drug design and optimization, and discusses the potential therapeutic strategies to overcome drug resistance.
Language	English
Publishing date	2022-01-04
Publishing country	Netherlands
Document type	Journal Article ; Review
ISSN	2211-3835
ISSN	2211-3835
DOI	10.1016/j.apsb.2021.12.022
Database	MEDical Literature Analysis and Retrieval System OnLINE

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Article ; Online: Unraveling the Design and Discovery of c-Jun N-Terminal Kinase Inhibitors and Their Therapeutic Potential in Human Diseases.

Zhu, Yumeng / Shuai, Wen / Zhao, Min / Pan, Xiaoli / Pei, Junping / Wu, Yongya / Bu, Faqian / Wang, Aoxue / Ouyang, Liang / Wang, Guan

Journal of medicinal chemistry

2022 Volume 65, Issue 5, Page(s) 3758–3775

Abstract: c-Jun N-terminal kinases (JNKs), members of the mitogen-activated protein kinase (MAPK) family, are encoded by three genes: ...

Abstract	c-Jun N-terminal kinases (JNKs), members of the mitogen-activated protein kinase (MAPK) family, are encoded by three genes:
MeSH term(s)	Humans ; JNK Mitogen-Activated Protein Kinases ; MAP Kinase Signaling System ; Neoplasms/drug therapy ; Phosphorylation ; Protein Isoforms/metabolism
Chemical Substances	Protein Isoforms ; JNK Mitogen-Activated Protein Kinases (EC 2.7.11.24)
Language	English
Publishing date	2022-02-24
Publishing country	United States
Document type	Journal Article ; Research Support, Non-U.S. Gov't
ZDB-ID	218133-2
ISSN	1520-4804 ; 0022-2623
ISSN (online)	1520-4804
ISSN	0022-2623
DOI	10.1021/acs.jmedchem.1c01947
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Article ; Online: Emerging strategies to overcome resistance to third-generation EGFR inhibitors.

Shi, Kunyu / Wang, Guan / Pei, Junping / Zhang, Jifa / Wang, Jiaxing / Ouyang, Liang / Wang, Yuxi / Li, Weimin

Journal of hematology & oncology

2022 Volume 15, Issue 1, Page(s) 94

Abstract: Epidermal growth factor receptor (EGFR), the receptor for members of the epidermal growth factor family, regulates cell proliferation and signal transduction; moreover, EGFR is related to the inhibition of tumor cell proliferation, angiogenesis, invasion, ...

Abstract	Epidermal growth factor receptor (EGFR), the receptor for members of the epidermal growth factor family, regulates cell proliferation and signal transduction; moreover, EGFR is related to the inhibition of tumor cell proliferation, angiogenesis, invasion, metastasis, and apoptosis. Therefore, EGFR has become an important target for the treatment of cancer, including non-small cell lung cancer, head and neck cancer, breast cancer, glioma, cervical cancer, and bladder cancer. First- to third-generation EGFR inhibitors have shown considerable efficacy and have significantly improved disease prognosis. However, most patients develop drug resistance after treatment. The challenge of overcoming intrinsic and acquired resistance in primary and recurrent cancer mediated by EGFR mutations is thus driving the search for alternative strategies in the design of new therapeutic agents. In view of resistance to third-generation inhibitors, understanding the intricate mechanisms of resistance will offer insight for the development of more advanced targeted therapies. In this review, we discuss the molecular mechanisms of resistance to third-generation EGFR inhibitors and review recent strategies for overcoming resistance, new challenges, and future development directions.
MeSH term(s)	Antineoplastic Agents/pharmacology ; Antineoplastic Agents/therapeutic use ; Carcinoma, Non-Small-Cell Lung/drug therapy ; Drug Resistance, Neoplasm ; ErbB Receptors ; Humans ; Lung Neoplasms/drug therapy ; Mutation ; Neoplasm Recurrence, Local/drug therapy ; Protein Kinase Inhibitors/pharmacology ; Protein Kinase Inhibitors/therapeutic use
Chemical Substances	Antineoplastic Agents ; Protein Kinase Inhibitors ; EGFR protein, human (EC 2.7.10.1) ; ErbB Receptors (EC 2.7.10.1)
Language	English
Publishing date	2022-07-15
Publishing country	England
Document type	Journal Article ; Review ; Research Support, Non-U.S. Gov't
ZDB-ID	2429631-4
ISSN	1756-8722 ; 1756-8722
ISSN (online)	1756-8722
ISSN	1756-8722
DOI	10.1186/s13045-022-01311-6
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Article ; Online: Design, Synthesis, and Antitumor Activity of Potent and Selective EGFR L858R/T790M Inhibitors and Identification of a Combination Therapy to Overcome Acquired Resistance in Models of Non-small-cell Lung Cancer.

Pei, Junping / Wang, Guan / Wang, Aoxue / Wu, Chengyong / Pan, Xiaoli / Shuai, Wen / Bu, Faqian / Zhu, Yumeng / Wang, Yuxi / Ouyang, Liang / Li, Weimin

Journal of medicinal chemistry

2023 Volume 66, Issue 8, Page(s) 5719–5752

Abstract: Epidermal growth factor receptor (EGFR) is one of the most studied drug targets for the treatment of non-small-cell lung cancer (NSCLC). Here, we report the identification, structure optimization, and structure-activity relationship studies of ... ...

Abstract	Epidermal growth factor receptor (EGFR) is one of the most studied drug targets for the treatment of non-small-cell lung cancer (NSCLC). Here, we report the identification, structure optimization, and structure-activity relationship studies of quinazoline derivatives as novel selective EGFR L858R/T790M inhibitors. The most promising compound,
MeSH term(s)	Humans ; Carcinoma, Non-Small-Cell Lung/drug therapy ; ErbB Receptors/metabolism ; Lung Neoplasms/drug therapy ; Cell Proliferation ; Dasatinib/pharmacology ; Cell Line, Tumor ; Mutation ; Protein Kinase Inhibitors/pharmacology ; Drug Resistance, Neoplasm ; Antineoplastic Agents/pharmacology
Chemical Substances	ErbB Receptors (EC 2.7.10.1) ; Dasatinib (RBZ1571X5H) ; Protein Kinase Inhibitors ; Antineoplastic Agents ; EGFR protein, human (EC 2.7.10.1)
Language	English
Publishing date	2023-04-12
Publishing country	United States
Document type	Journal Article ; Research Support, Non-U.S. Gov't
ZDB-ID	218133-2
ISSN	1520-4804 ; 0022-2623
ISSN (online)	1520-4804
ISSN	0022-2623
DOI	10.1021/acs.jmedchem.3c00027
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