PMID- 36015177 OWN - NLM STAT- PubMed-not-MEDLINE LR - 20230204 IS - 1424-8247 (Print) IS - 1424-8247 (Electronic) IS - 1424-8247 (Linking) VI - 15 IP - 8 DP - 2022 Aug 21 TI - Pharmacological Small Molecules against Prostate Cancer by Enhancing Function of Death Receptor 5. LID - 10.3390/ph15081029 [doi] LID - 1029 AB - Death receptor 5 (DR5) is a membrane protein that mediates exogenous apoptosis. Based on its function, it is considered to be a target for the treatment of cancers including prostate cancer. It is encouraging to note that a number of drugs targeting DR5 are now progressing to different stages of clinical trial studies. We collected 38 active compounds that could produce anti-prostate-cancer effects by modulating DR5, 28 of which were natural compounds and 10 of which were synthetic compounds. In addition, 6 clinically used chemotherapeutic agents have also been shown to promote DR5 expression and thus exert apoptosis-inducing effects in prostate cancer cells. These compounds promote the expression of DR5, thereby enhancing its function in inducing apoptosis. When these compounds were used in combination with the natural ligand of DR5, the number of apoptotic cells was significantly increased. These compounds are all promising for development as anti-prostate-cancer drugs, while most of these compounds are currently being evaluated for their anti-prostate-cancer effects at the cellular level and in animal studies. A great deal of more in-depth research is needed to evaluate whether they can be developed as drugs. We collected literature reports on small molecules against prostate cancer through modulation of DR5 to understand the current dynamics in this field and to evaluate the prospects of small molecules against prostate cancer through modulation of DR5. FAU - Gan, Xia AU - Gan X AD - Guangxi Zhuang Yao Medicine Center of Engineering and Technology, Guangxi University of Chinese Medicine, 13 Wuhe Road, Qingxiu District, Nanning 530200, China. AD - Institute of Marine Drugs, Guangxi University of Chinese Medicine, 13 Wuhe Road, Qingxiu District, Nanning 530200, China. FAU - Liu, Yonghong AU - Liu Y AUID- ORCID: 0000-0001-8327-3108 AD - Institute of Marine Drugs, Guangxi University of Chinese Medicine, 13 Wuhe Road, Qingxiu District, Nanning 530200, China. AD - CAS Key Laboratory of Tropical Marine Bio-Resources and Ecology, Guangdong Key Laboratory of Marine Materia Medica, South China Sea Institute of Oceanology, Chinese Academy of Sciences, Guangzhou 510301, China. FAU - Wang, Xueni AU - Wang X AUID- ORCID: 0000-0001-9884-994X AD - Guangxi Zhuang Yao Medicine Center of Engineering and Technology, Guangxi University of Chinese Medicine, 13 Wuhe Road, Qingxiu District, Nanning 530200, China. AD - CAS Key Laboratory of Tropical Marine Bio-Resources and Ecology, Guangdong Key Laboratory of Marine Materia Medica, South China Sea Institute of Oceanology, Chinese Academy of Sciences, Guangzhou 510301, China. LA - eng GR - AD20159033/Specific Research Project of Guangxi for Research Bases and Talents/ GR - Y.H. Liu/Special Fund for Bagui Scholars of Guangxi/ PT - Journal Article PT - Review DEP - 20220821 PL - Switzerland TA - Pharmaceuticals (Basel) JT - Pharmaceuticals (Basel, Switzerland) JID - 101238453 PMC - PMC9413322 OTO - NOTNLM OT - chemotherapeutic agents OT - death receptor 5 OT - natural compounds OT - prostate cancer OT - synthesized compounds COIS- The authors declare no conflict of interest. EDAT- 2022/08/27 06:00 MHDA- 2022/08/27 06:01 PMCR- 2022/08/21 CRDT- 2022/08/26 01:41 PHST- 2022/07/30 00:00 [received] PHST- 2022/08/15 00:00 [revised] PHST- 2022/08/19 00:00 [accepted] PHST- 2022/08/26 01:41 [entrez] PHST- 2022/08/27 06:00 [pubmed] PHST- 2022/08/27 06:01 [medline] PHST- 2022/08/21 00:00 [pmc-release] AID - ph15081029 [pii] AID - pharmaceuticals-15-01029 [pii] AID - 10.3390/ph15081029 [doi] PST - epublish SO - Pharmaceuticals (Basel). 2022 Aug 21;15(8):1029. doi: 10.3390/ph15081029.