Non-‘classical’ MEKs: A review of MEK3-7 inhibitors

Ada J. Kwong; Karl A. Scheidt

doi:10.1016/j.bmcl.2020.127203

Non-‘classical’ MEKs: A review of MEK3-7 inhibitors

Ada J. Kwong, Karl A. Scheidt^*

^*Corresponding author for this work

Chemistry

Research output: Contribution to journal › Review article › peer-review

11 Scopus citations

Abstract

The MAPK pathways are an enduring area of interest due to their essential roles in cell processes. Increased expression and activity can lead to a multitude of diseases, sparking research efforts in developing inhibitors against these kinases. Though great strides have been made in developing MEK1/2 inhibitors, there is a notable lack of chemical probes for MEK3-7, given their central role in stimuli response, cell growth, and development. This review summarizes the progress that has been made on developing small molecule probes for MEK3-7, the specific disease states in which they have been studied, and their potential to become novel therapeutics.

Original language	English (US)
Article number	127203
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	30
Issue number	13
DOIs	https://doi.org/10.1016/j.bmcl.2020.127203
State	Published - Jul 1 2020

Funding

Funding for these efforts has been provided by the National Cancer Institute of the National Institutes of Health (NCI; R01CA188015) and Northwestern. AJK is supported by the National Institute of General Medical Sciences of the National Institutes of Health under Award Number T32GM105538. The content is solely the responsibility of the authors and does not necessarily represent the official views of the National Institutes of Health. The authors thank Meghan Orr (NU), Dalton Kim (NU), and David Burke (NU) for manuscript proofreading. Funding for these efforts has been provided by the National Cancer Institute of the National Institutes of Health (NCI; R01CA188015 ) and Northwestern. AJK is supported by the National Institute of General Medical Sciences of the National Institutes of Health under Award Number T32GM105538 . The content is solely the responsibility of the authors and does not necessarily represent the official views of the National Institutes of Health . The authors thank Meghan Orr (NU), Dalton Kim (NU), and David Burke (NU) for manuscript proofreading.

Keywords

Drug discovery
Kinases
Mitogen-activated protein kinases
Small molecule inhibitors
Structure-activity relationships

ASJC Scopus subject areas

Drug Discovery
Molecular Medicine
Molecular Biology
Biochemistry
Clinical Biochemistry
Pharmaceutical Science
Organic Chemistry

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

Access to Document

10.1016/j.bmcl.2020.127203

Cite this

@article{80a4c86a10464dcaa0ea87443746fd5c,

title = "Non-{\textquoteleft}classical{\textquoteright} MEKs: A review of MEK3-7 inhibitors",

abstract = "The MAPK pathways are an enduring area of interest due to their essential roles in cell processes. Increased expression and activity can lead to a multitude of diseases, sparking research efforts in developing inhibitors against these kinases. Though great strides have been made in developing MEK1/2 inhibitors, there is a notable lack of chemical probes for MEK3-7, given their central role in stimuli response, cell growth, and development. This review summarizes the progress that has been made on developing small molecule probes for MEK3-7, the specific disease states in which they have been studied, and their potential to become novel therapeutics.",

keywords = "Drug discovery, Kinases, Mitogen-activated protein kinases, Small molecule inhibitors, Structure-activity relationships",

author = "Kwong, {Ada J.} and Scheidt, {Karl A.}",

note = "Funding Information: Funding for these efforts has been provided by the National Cancer Institute of the National Institutes of Health (NCI; R01CA188015) and Northwestern. AJK is supported by the National Institute of General Medical Sciences of the National Institutes of Health under Award Number T32GM105538. The content is solely the responsibility of the authors and does not necessarily represent the official views of the National Institutes of Health. The authors thank Meghan Orr (NU), Dalton Kim (NU), and David Burke (NU) for manuscript proofreading. Funding Information: Funding for these efforts has been provided by the National Cancer Institute of the National Institutes of Health (NCI; R01CA188015 ) and Northwestern. AJK is supported by the National Institute of General Medical Sciences of the National Institutes of Health under Award Number T32GM105538 . The content is solely the responsibility of the authors and does not necessarily represent the official views of the National Institutes of Health . The authors thank Meghan Orr (NU), Dalton Kim (NU), and David Burke (NU) for manuscript proofreading. Publisher Copyright: {\textcopyright} 2020 Elsevier Ltd",

year = "2020",

month = jul,

day = "1",

doi = "10.1016/j.bmcl.2020.127203",

language = "English (US)",

volume = "30",

journal = "Bioorganic and Medicinal Chemistry Letters",

issn = "0960-894X",

publisher = "Elsevier Ltd",

number = "13",

}

TY - JOUR

T1 - Non-‘classical’ MEKs

T2 - A review of MEK3-7 inhibitors

AU - Kwong, Ada J.

AU - Scheidt, Karl A.

N1 - Funding Information: Funding for these efforts has been provided by the National Cancer Institute of the National Institutes of Health (NCI; R01CA188015) and Northwestern. AJK is supported by the National Institute of General Medical Sciences of the National Institutes of Health under Award Number T32GM105538. The content is solely the responsibility of the authors and does not necessarily represent the official views of the National Institutes of Health. The authors thank Meghan Orr (NU), Dalton Kim (NU), and David Burke (NU) for manuscript proofreading. Funding Information: Funding for these efforts has been provided by the National Cancer Institute of the National Institutes of Health (NCI; R01CA188015 ) and Northwestern. AJK is supported by the National Institute of General Medical Sciences of the National Institutes of Health under Award Number T32GM105538 . The content is solely the responsibility of the authors and does not necessarily represent the official views of the National Institutes of Health . The authors thank Meghan Orr (NU), Dalton Kim (NU), and David Burke (NU) for manuscript proofreading. Publisher Copyright: © 2020 Elsevier Ltd

PY - 2020/7/1

Y1 - 2020/7/1

N2 - The MAPK pathways are an enduring area of interest due to their essential roles in cell processes. Increased expression and activity can lead to a multitude of diseases, sparking research efforts in developing inhibitors against these kinases. Though great strides have been made in developing MEK1/2 inhibitors, there is a notable lack of chemical probes for MEK3-7, given their central role in stimuli response, cell growth, and development. This review summarizes the progress that has been made on developing small molecule probes for MEK3-7, the specific disease states in which they have been studied, and their potential to become novel therapeutics.

AB - The MAPK pathways are an enduring area of interest due to their essential roles in cell processes. Increased expression and activity can lead to a multitude of diseases, sparking research efforts in developing inhibitors against these kinases. Though great strides have been made in developing MEK1/2 inhibitors, there is a notable lack of chemical probes for MEK3-7, given their central role in stimuli response, cell growth, and development. This review summarizes the progress that has been made on developing small molecule probes for MEK3-7, the specific disease states in which they have been studied, and their potential to become novel therapeutics.

KW - Drug discovery

KW - Kinases

KW - Mitogen-activated protein kinases

KW - Small molecule inhibitors

KW - Structure-activity relationships

UR - http://www.scopus.com/inward/record.url?scp=85084408796&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=85084408796&partnerID=8YFLogxK

U2 - 10.1016/j.bmcl.2020.127203

DO - 10.1016/j.bmcl.2020.127203

M3 - Review article

C2 - 32389527

AN - SCOPUS:85084408796

SN - 0960-894X

VL - 30

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 13

M1 - 127203

ER -

Non-‘classical’ MEKs: A review of MEK3-7 inhibitors

Abstract

Funding

Keywords

ASJC Scopus subject areas

UN SDGs

Access to Document

Other files and links

Fingerprint

Cite this