GRP78/Dna K is a target for Nexavar/Stivarga/Votrient in the treatment of human malignancies, viral infections and bacterial diseases

JL Roberts, M Tavallai, A Nourbakhsh… - Journal of cellular …, 2015 - Wiley Online Library
Prior tumor cell studies have shown that the drugs sorafenib (Nexavar) and regorafenib
(Stivarga) reduce expression of the chaperone GRP78. Sorafenib/regorafenib and the multi …

GRP78/BiP/HSPA5/Dna K is a universal therapeutic target for human disease

L Booth, JL Roberts, DR Cash… - Journal of cellular …, 2015 - Wiley Online Library
The chaperone GRP78/Dna K is conserved throughout evolution down to prokaryotes. The
GRP78 inhibitor OSU‐03012 (AR‐12) interacted with sildenafil (Viagra) or tadalafil (Cialis) …

Vascular targeting and antiangiogenesis agents induce drug resistance effector GRP78 within the tumor microenvironment

D Dong, B Ko, P Baumeister, S Swenson, F Costa… - Cancer research, 2005 - AACR
Therapeutic targeting of the tumor vasculature that destroys preexisting blood vessels of the
tumor and antiangiogenesis therapy capitalize on the requirement of tumor cells on an intact …

Pharmacological effectors of GRP78 chaperone in cancers

C Bailly, MJ Waring - Biochemical Pharmacology, 2019 - Elsevier
The protein chaperone GRP78 is a master regulator of endoplasmic reticulum (ER) functions
and is frequently over-expressed at the surface of cancer cells where it contributes to chemo …

OSU‐03012 and Viagra Treatment Inhibits the Activity of Multiple Chaperone Proteins and Disrupts the Blood–Brain Barrier: Implications for Anti‐Cancer Therapies

L Booth, JL Roberts, M Tavallai… - Journal of cellular …, 2015 - Wiley Online Library
We examined the interaction between OSU‐03012 (also called AR‐12) with
phosphodiesterase 5 (PDE5) inhibitors to determine the role of the chaperone glucose …

[HTML][HTML] Inhibition of colon cancer K-RasG13D mutation reduces cancer cell proliferation but promotes stemness and inflammation via RAS/ERK pathway

Y Qi, H Zou, XH Zhao, J Kapeleris… - Frontiers in …, 2022 - frontiersin.org
K-Ras is a well-studied oncogene, and its mutation is frequently found in epithelial cancers
like pancreas, lung, and colorectal cancers. Cancer cells harboring K-Ras mutations are …

[HTML][HTML] Glucose-related protein 78 expression and its effects on cisplatin-resistance in cervical cancer

C Luo, W Fan, Y Jiang, S Zhou… - Medical Science Monitor …, 2018 - ncbi.nlm.nih.gov
Background GRP78, the 78-kDa glucose-regulated protein, occupies a significant position in
endoplasmic reticulum stress. Emerging evidences have shown that GRP78 induces …

[HTML][HTML] The molecular chaperone GRP78/BiP in the development of chemoresistance: mechanism and possible treatment

C Roller, D Maddalo - Frontiers in pharmacology, 2013 - frontiersin.org
Treatment of several types of cancer such as lung, breast, prostate, and pancreas has
shown notable progresses in the past decades. However, after an initial response, tumors …

GRP-78 secreted by tumor cells blocks the antiangiogenic activity of bortezomib

J Kern, G Untergasser, C Zenzmaier… - Blood, The Journal …, 2009 - ashpublications.org
Antiangiogenic effects of the proteasome inhibitor bortezomib were analyzed on tumor
xenografts in vivo. Bortezomib strongly inhibited angiogenesis and vascularization in the …

GRP78 Protein Expression in Ovarian Cancer Patients and Perspectives for a Drug‐Targeting Approach

F Delie, P Petignat, M Cohen - Journal of oncology, 2012 - Wiley Online Library
Glucose‐regulated protein of 78 kD (GRP78) is a chaperone protein mainly located in the
endoplasmic reticulum (ER). This protein is normally present at low levels in adult cells but …