The relationship between the chemistry and biological activity of the bisphosphonates

FH Ebetino, AML Hogan, S Sun, MK Tsoumpra, X Duan… - Bone, 2011 - Elsevier
The ability of bisphosphonates ((HO) 2 P (O) CR 1 R 2 P (O)(OH) 2) to inhibit bone
resorption has been known since the 1960s, but it is only recently that a detailed molecular …

Molecular mechanisms of action of bisphosphonates: current status

AJ Roelofs, K Thompson, S Gordon, MJ Rogers - Clinical Cancer Research, 2006 - AACR
Purpose: Bisphosphonates are currently the most important class of antiresorptive agents
used in the treatment of metabolic bone diseases, including tumor-associated osteolysis and …

Recent advances in understanding the mechanism of action of bisphosphonates

FP Coxon, K Thompson, MJ Rogers - Current opinion in pharmacology, 2006 - Elsevier
Bisphosphonates (BPs) are widely used in the treatment of diseases associated with
excessive osteoclast-mediated bone resorption, such as osteoporosis. Although several …

Targeting small GTPases: emerging grasps on previously untamable targets, pioneered by KRAS

G Yin, J Huang, J Petela, H Jiang, Y Zhang… - Signal transduction and …, 2023 - nature.com
Abstract Small GTPases including Ras, Rho, Rab, Arf, and Ran are omnipresent molecular
switches in regulating key cellular functions. Their dysregulation is a therapeutic target for …

Fluorescent risedronate analogues reveal bisphosphonate uptake by bone marrow monocytes and localization around osteocytes in vivo

AJ Roelofs, FP Coxon, FH Ebetino… - Journal of Bone and …, 2010 - academic.oup.com
Bisphosphonates are effective antiresorptive agents owing to their bone‐targeting property
and ability to inhibit osteoclasts. It remains unclear, however, whether any non‐osteoclast …

Drugging the small GTPase pathways in cancer treatment: promises and challenges

N Prieto-Dominguez, C Parnell, Y Teng - Cells, 2019 - mdpi.com
Small GTPases are a family of low molecular weight GTP-hydrolyzing enzymes that cycle
between an inactive state when bound to GDP and an active state when associated to GTP …

[HTML][HTML] Onco-Golgi: is fragmentation a gate to cancer progression?

A Petrosyan - Biochemistry & molecular biology journal, 2015 - ncbi.nlm.nih.gov
The Golgi apparatus-complex is a highly dynamic organelle which is considered the “heart”
of intracellular transportation. Since its discovery by Camillo Golgi in 1873, who described it …

Osteoclasts in multiple myeloma are derived from Gr-1+ CD11b+ myeloid-derived suppressor cells

J Zhuang, J Zhang, ST Lwin, JR Edwards… - PloS one, 2012 - journals.plos.org
Osteoclasts play a key role in the development of cancer-associated osteolytic lesions. The
number and activity of osteoclasts are often enhanced by tumors. However, the origin of …

Biological activity of aminophosphonic acids and their short peptides

B Lejczak, P Kafarski - Phosphorous Heterocycles I, 2009 - Springer
The biological activity and natural occurrence of the aminophosphonic acids were described
half a century ago. Since then the chemistry and biology of this class of compounds have …

The bisphosphonate zoledronic acid has antimyeloma activity in vivo by inhibition of protein prenylation

A Guenther, S Gordon, M Tiemann… - … Journal of Cancer, 2010 - Wiley Online Library
Nitrogen‐containing bisphosphonates (N‐BPs) are effective antiosteolytic agents in patients
with multiple myeloma. Preclinical studies have also demonstrated that these agents have …