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GRP78, therefore, can be not only a biomarker to predict the progression and prognosis of obesity and metabolic diseases but also a potential therapeutic target for anti-obesity treatment. In this paper, GRP78 inhibitors targeting its ATPase domain have been reviewed. Small molecules and proteins that directly bind GRP78 have been described. Putative mechanisms of GRP78 in regulating lipid metabolism were also summarized so as to investigate the role of GRP78 in obesity and other related diseases and provide a theoretical basis for the development and design of anti-obesity drugs targeting GRP78.<\/jats:p>","DOI":"10.3390\/ijerph192315965","type":"journal-article","created":{"date-parts":[[2022,11,30]],"date-time":"2022-11-30T04:32:53Z","timestamp":1669782773000},"page":"15965","update-policy":"https:\/\/doi.org\/10.3390\/mdpi_crossmark_policy","source":"Crossref","is-referenced-by-count":14,"title":["GRP78 Activity Moderation as a Therapeutic Treatment against Obesity"],"prefix":"10.3390","volume":"19","author":[{"ORCID":"https:\/\/orcid.org\/0000-0002-4222-1851","authenticated-orcid":false,"given":"Dongjin","family":"Pan","sequence":"first","affiliation":[{"name":"Institute of Marine Drugs, Guangxi University of Chinese Medicine, Nanning 530200, China"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Yunzhu","family":"Yang","sequence":"additional","affiliation":[{"name":"Institute of Marine Drugs, Guangxi University of Chinese Medicine, Nanning 530200, China"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Aihua","family":"Nong","sequence":"additional","affiliation":[{"name":"Institute of Marine Drugs, Guangxi University of Chinese Medicine, Nanning 530200, China"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-5519-7467","authenticated-orcid":false,"given":"Zhenzhou","family":"Tang","sequence":"additional","affiliation":[{"name":"Institute of Marine Drugs, Guangxi University of Chinese Medicine, Nanning 530200, China"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0003-4589-2869","authenticated-orcid":false,"given":"Qing X.","family":"Li","sequence":"additional","affiliation":[{"name":"Department of Molecular Biosciences and Bioengineering, University of Hawaii at Manoa, 1955 East-West Road, Honolulu, HI 96822, USA"}],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"1968","published-online":{"date-parts":[[2022,11,30]]},"reference":[{"key":"ref_1","unstructured":"WHO (2020). 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