Publications

2nd International Symposium on the Chaperone Code, 2023.

Buchner J, Alasady MJ, Backe SJ, Blagg BS, Carpenter RL, Colombo G, Gelis I, Gewirth DT, Gierasch LM, Houry WA, Johnson JL, Kang BH, Kao AW, LaPointe P, Mattoo S, McClellan AJ, Neckers LM, Prodromou C, Rasola A, Sager RA, Theodoraki MA, Truman AW, Truttman MC, Zachara NE, Bourboulia D, Mollapour M, Woodford MR

Cell Stress Chaperones. 2024 Feb 3:S1355-8145(24)00043-9. doi: 10.1016/j.cstres.2024.01.003. Online

Targeting the Mitochondrial Chaperone TRAP1 Alleviates Vascular Pathologies in Ischemic Retinopathy

Kim SY, Yoon NG, Im JY, Lee JH, Kim J, Jeon Y, Choi YJ, Lee JH, Uemura A, Park DH, Kang BH

Adv Sci (Weinh). 2023 Nov 20:e2302776. doi: 10.1002/advs.202302776. Online ahead of print.

Structure, Function, and Inhibitors of the Mitochondrial Chaperone TRAP1

Kang S and Kang BH

J Med Chem. 2022 Dec 12; 65(24): 16155-16172.

TonEBP in Myeloid Cells Promotes Obesity-Induced Insulin Resistance and Inflammation Through Adipose Tissue Remodeling.

Lee HH, Jeong GW, Ye BJ, Yoo EJ, Son KS, Kim DK, Park HK, Kang BH, Lee-Kwon W, Kwon HM, Choi SY.

Diabetes. 2022 Dec 1;71(12):2557-2571

Triphenylphosphonium conjugation to a TRAP1 inhibitor, 2-amino-6-chloro-7,9-dihydro-8H-purin-8-one increases antiproliferative activity.

Yang S#, Yoon NG#, Park MA#, Yun J, Im JY, Kang BH*, Kang S*.

Bioorg Chem. 2022 Sep 20;126:105856. doi: 10.1016/j.bioorg.2022.105856.

Quaternary ammonium-based mitochondria targeting anticancer agents with high water solubility

Kim S#, Yoon NG#, Jana B, Kang BH*, Ryu JH*. 

Bull. Kor. Chem. Soc. 2022 March 21; 43(3): 391-395.

Mitoquinone Inactivates Mitochondrial Chaperone TRAP1 by Blocking the Client Binding Site.

Yoon NG, Lee H, Kim SY, Hu S, Kim D, Yang S, Hong KB, Lee JH, Kang S, Kim BG, Myung K, Lee C*, Kang BH*.

J Am Chem Soc. 2021 Dec 1;143(47):19684-19696. (Cover)

Design and Synthesis of TRAP1 Selective Inhibitors: H-Bonding with Asn171 Residue in TRAP1 Increases Paralog Selectivity.

Yang S#, Yoon NG#, Kim D#, Park E, Kim SY, Lee JH, Lee C, Kang BH, Kang S.

ACS Med Chem Lett. 2021 Jun 16;12(7):1173-1180.

Development of pyrazolo[3,4-d]pyrimidine-6-amine-based TRAP1 inhibitors that demonstrate in vivo anticancer activity in mouse xenograft models.

Kim D, Kim SY, Kim D, Yoon NG, Yun J, Hong KB, Lee C*, Lee JH*, Kang BH*, Kang S*.

Bioorg Chem. 2020 Jun 15;101:103901. 

Flightless-1 inhibits ER stress-induced apoptosis in colorectal cancer cells by regulating Ca(2+) homeostasis.

Choi SS, Lee SK, Kim JK, Park HK, Lee E, Jang J, Lee YH, Khim KW, Hyun JM, Eom HJ, Lee S, Kang BH, Chae YC, Myung K, Myung SJ, Park CY, Choi JH.

Exp Mol Med. 2020 Jun;52(6):940-950.

Dual Binding to Orthosteric and Allosteric Sites Enhances the Anticancer Activity of a TRAP1-Targeting Drug.

Hu S, Ferraro M, Thomas AP, Chung JM, Yoon NG, Seol JH, Kim S, Kim HU, An MY, Ok H, Jung HS*, Ryu JH*, Colombo G*, Kang BH*.

J Med Chem. 2020 Mar 26;63(6):2930-2940.

Unleashing the full potential of Hsp90 inhibitors as cancer therapeutics through simultaneous inactivation of Hsp90, Grp94, and TRAP1.

Park HK, Yoon NG, Lee JE, Hu S, Yoon S, Kim SY, Hong JH, Nam D, Chae YC, Park JB, Kang BH.

Exp Mol Med. 2020 Jan;52(1):79-91. 

Discovery of 2-((4-resorcinolyl)-5-aryl-1,2,3-triazol-1-yl)acetates as potent Hsp90 inhibitors with selectivity over TRAP1.

Jung S#, Yoon NG#, Yang S, Kim D, Lee WS, Hong KB, Lee C, Kang BH*, Lee JH*, Kang S*.

Bioorg Med Chem Lett. 2020 Jan; 30(2): 126809

Mitochondrial heat shock protein-guided photodynamic therapy.

Thomas AP#, Lee AJ#, Palanikumar L, Jana B, Kim K, Kim S, Ok H, Seol J, Kim D, Kang BH*, Ryu JH*.

Chem Commun. 2019 Oct; 55(84):12631-12634

Interplay between TRAP1 and sirtuin-3 modulates mitochondrial respiration and oxidative stress to maintain stemness of glioma stem cells

Park HK#, Hong JH#, Oh YT, Kim SS, Yin J, Lee AJ, Chae YC, Kim JH, Park SH, Park CK, Park MJ, Park JB*, Kang BH*

Cancer Res. 2019 Apr;79(7):1369-1382

TRAP1 Inhibition Increases Glutamine Synthetase Activity in Glutamine Auxotrophic Non-small Cell Lung Cancer Cells.

Vo VTA, Choi JW, Phan ANH, Hua TNM, Kim MK, Kang BH, Jung SH, Yong SJ, Jeong Y.

Anticancer Res. 2018 Apr;38(4):2187-2193

The novel resveratrol derivative 3,5-diethoxy-3',4'-dihydroxy-trans-stilbene induces mitochondrial ROS-mediated ER stress and cell death in human hepatoma cells in vitro

Park JW, Choi WG, Lee PJ, Chung SW, Kim BS, Chung HT, Cho S, Kim JH, Kang BH, Kim H, Kim HP, Back SH.

Acta Pharmacol. Sin. 2017 Nov;38(11):1486-1500

Paralog Specificity Determines Subcellular Distribution, Action Mechanism, and Anticancer Activity of TRAP1 Inhibitors.

Park HK, Jeong H, Ko E, Lee G, Lee JE, Lee SK, Lee AJ, Im JY, Hu S, Kim SH, Lee JH, Lee C, KangS, Kang BH.

J. Med. Chem. 2017 Aug 30; 60(17): 7569-78

Development of a mitochondria-targeted Hsp90 inhibitor based on the crystal structures of human TRAP1.

Lee C, Park HK, Jeong H, Lim J, Lee AJ, Cheon KY, Kim CS, Thomas AP, Bae B, Kim ND, Kim SH, Suh PG, Ryu JH, Kang BH.

J Am Chem Soc. 2015 Apr 8;137(13):4358-67

Hepatoprotective and anticancer activities of Allomyrina dichotoma larvae.

Lee JE, Jo DE, Lee AJ, Park HK, Youn K, Yun EY, Hwang JS, Jun M, Kang BH

J Life Sci. 2015 Mar 31; 25(3):307-16

Cytotoxic Effects of Tenebrio molitor Larval Extracts against Hepatocellular Carcinoma

Lee JE, Lee AJ, Jo DE, Cho JH, Youn K, Yun EY, Hwang JS, Jun M, Kang BH

J Korean Soc Food Sci Nutr. 2015 Feb 28; 44(2):200-7

Crystallization and preliminary X-ray diffraction analysis of Trap1 complexed with Hsp90 inhibitors.

Jeong H, Kang BH, Lee C.

Acta Crystallogr F Struct Biol Commun. 2014 Dec 1;70(Pt 12):1683-7.

Hepatoprotective and antineoplastic properties of Protaetia brevitarsis larvae.

Lee JE, Jo DE, Lee AJ, Park HK, Youn K, Yun EY, Hwang JS, Jun M, Kang BH.

Entomol Res. 2014 Nov 30; 44(6):244-53. 

OGA heterozygosity suppresses intestinal tumorigenesis in Apc(min/+) mice.

Yang YR, Jang HJ, Yoon S, Lee YH, Nam D, Kim IS, Lee H, Kim H, Choi JH, Kang BH, Ryu SH, Suh PG.

Oncogenesis. 2014 Jul 7;3:e109

Combination treatment with doxorubicin and gamitrinib synergistically augments anticancer activity through enhanced activation of Bim.

Park HK, Lee JE, Lim J, Jo DE, Park SA, Suh PG, Kang BH.

BMC Cancer. 2014 Jun 13;14(1):431.

Mitochondrial Hsp90s suppress calcium-mediated stress signals propagating from mitochondria to the ER in cancer cells.

Park HK, Lee JE, Lim J, Kang BH.

Mol Cancer. 2014 Jun 12;13(1):148.

PDZ domain-containing 1 (PDZK1) protein regulates phospholipase C-β3 (PLC-β3)-specific activation of somatostatin by forming a ternary complex with PLC-β3 and somatostatin receptors.

Kim JK, Kwon O, Kim J, Kim EK, Park HK, Lee JE, Kim KL, Choi JW, Lim S, Seok H, Lee-Kwon W, Choi JH, Kang BH, Kim S, Ryu SH, Suh PG.

J Biol Chem. 2012 Jun 15;287(25):21012-24.

TRAP1 regulation of mitochondrial life or death decision in cancer cells and mitochondria-targeted TRAP1 inhibitors.

Kang BH.

BMB Rep. 2012 Jan;45(1):1-6. 

Developmental control of apoptosis by the immunophilin aryl hydrocarbon receptor-interacting protein (AIP) involves mitochondrial import of the survivin protein.

Kang BH, Xia F, Pop R, Dohi T, Socolovsky M, Altieri DC.

J Biol Chem. 2011 May 13;286(19):16758-67.

Targeted inhibition of mitochondrial Hsp90 suppresses localised and metastatic prostate cancer growth in a genetic mouse model of disease.

Kang BH, Tavecchio M, Goel HL, Hsieh CC, Garlick DS, Raskett CM, Lian JB, Stein GS, Languino LR, Altieri DC.

Br J Cancer. 2011 Feb 15;104(4):629-34

Preclinical Characterization of Mitochondria-Targeted Small Molecule Hsp90 Inhibitors, Gamitrinibs, in Advanced Prostate Cancer.

Kang BH, Siegelin MD, Plescia J, Raskett CM, Garlick DS, Dohi T, Lian JB, Stein GS, Languino LR, Altieri DC.

Clin Cancer Res. 2010 Oct 1; 16(19):4779-88. (selected as a cover article)

Compartmentalized cancer drug discovery targeting mitochondrial Hsp90 chaperones.

Kang BH, Altieri DC.

Oncogene. 2009 Oct 22;28(42):3681-8.

Combinatorial drug design targeting multiple cancer signaling networks controlled by mitochondrial Hsp90.

Kang BH, Plescia J, Song HY, Meli M, Colombo G, Beebe K, Scroggins B, Neckers L, Altieri DC.

J Clin Invest. 2009 Mar;119(3):454-64. (selected as a cover article)

Hsp60 regulation of tumor cell apoptosis.

Ghosh JC, Dohi T, Kang BH, Altieri DC.

J Biol Chem. 2008 Feb 22;283(8):5188-94.

Regulation of tumor cell mitochondrial homeostasis by an organelle-specific Hsp90 chaperone network.

Kang BH, Plescia J, Dohi T, Rosa J, Doxsey SJ, Altieri DC.

Cell. 2007 Oct 19;131(2):257-70.

Regulation of survivin stability by the aryl hydrocarbon receptor-interacting protein.

Kang BH, Altieri DC.

J Biol Chem. 2006 Aug 25;281(34):24721-7.