干旱区生态环境知识资源中心(Arid): Emerging chemical scaffolds with potential SHP2 phosphatase inhibitory capabilities

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DOI	10.1111/cbdd.13807
	Emerging chemical scaffolds with potential SHP2 phosphatase inhibitory capabilities - A comprehensive review
	Tripathi, Rati Kailash Prasad; Ayyannan, Senthil Raja
通讯作者	Ayyannan, SR
来源期刊	CHEMICAL BIOLOGY & DRUG DESIGN
ISSN	1747-0277
EISSN	1747-0285
英文摘要	The drug discovery panorama is cluttered with promising therapeutic targets that have been deserted because of inadequate authentication and screening failures. Molecular targets formerly tagged as "undruggable" are nowadays being more cautiously cross-examined, and whilst they stay intriguing, numerous targets are emerging more accessible. Protein tyrosine phosphatases (PTPs) excellently exemplifies a class of molecular targets that have transpired as druggable, with several small molecules and antibodies recently turned available for further development. In this respect, SHP2, a PTP, has emerged as one of the potential targets in the current pharmacological research, particularly for cancer, due to its critical role in various signalling pathways. Recently, few molecules with excellent potency have entered clinical trials, but none could reach the clinic. Consequently, search for novel, non-toxic, and specific SHP2 inhibitors are on purview. In this review, general aspects of SHP2 including its structure and mechanistic role in carcinogenesis have been presented. It also sheds light on the development of novel molecular architectures belonging to diverse chemical classes that have been proposed as SHP2-specific inhibitors along with their structure-activity relationships (SARs), stemming from chemical, mechanism-based and computer-aided studies reported since January 2015 to July 2020 (excluding patents), focusing on their potency and selectivity. The encyclopedic facts and discussions presented herein will hopefully facilitate researchers to design new ligands with better efficacy and selectivity against SHP2.
英文关键词	Cancer computational studies protein tyrosine phosphatase SHP2 SHP2 inhibitors structure‐ activity relationship (SAR)
类型	Review ; Early Access
语种	英语
收录类别	SCI-E
WOS记录号	WOS:000592894900001
WOS关键词	PROTEIN-TYROSINE-PHOSPHATASE ; EPITHELIAL-MESENCHYMAL TRANSITION ; ALPHA-LIPOIC ACID ; BREAST-CANCER CELLS ; SOMATIC PTPN11 MUTATIONS ; NOONAN-SYNDROME ; AURINTRICARBOXYLIC ACID ; ALLOSTERIC-INHIBITION ; LEOPARD-SYNDROME ; MOUSE MODEL
WOS类目	Biochemistry & Molecular Biology ; Chemistry, Medicinal
WOS研究方向	Biochemistry & Molecular Biology ; Pharmacology & Pharmacy
资源类型	期刊论文
条目标识符	http://119.78.100.177/qdio/handle/2XILL650/328545
作者单位	[Tripathi, Rati Kailash Prasad] Assam Univ, Dept Pharmaceut Sci, Sushruta Sch Med & Paramed Sci, Silchar, Assam, India; [Tripathi, Rati Kailash Prasad; Ayyannan, Senthil Raja] Banaras Hindu Univ, Pharmaceut Chem Res Lab, Dept Pharmaceut Engn & Technol, Indian Inst Technol, Varanasi 221005, Uttar Pradesh, India
推荐引用方式 GB/T 7714	Tripathi, Rati Kailash Prasad,Ayyannan, Senthil Raja. Emerging chemical scaffolds with potential SHP2 phosphatase inhibitory capabilities - A comprehensive review[J].
APA	Tripathi, Rati Kailash Prasad,&Ayyannan, Senthil Raja.
MLA	Tripathi, Rati Kailash Prasad,et al."Emerging chemical scaffolds with potential SHP2 phosphatase inhibitory capabilities - A comprehensive review".CHEMICAL BIOLOGY & DRUG DESIGN