✦ LIBER ✦

Inhibitors of Protein:Farnesyl Transferase and Protein:Geranylgeranyl Transferase I: Synthesis of Homologous Diphosphonate Analogs of Isoprenylated Pyrophosphate

✍ Scribed by Mark Overhand; Hanneke R. Stuivenberg; Elsbet Pieterman; Louis H. Cohen; Rick E.W. van Leeuwen; A.Rob P.M. Valentijn; Herman S. Overkleeft; Gijs A. van der Marel; Jacques H. van Boom

Publisher: Elsevier Science
Year: 1998
Tongue: English
Weight: 297 KB
Volume: 26
Category: Article
ISSN: 0045-2068
DOI: 10.1006/bioo.1998.1101

No coin nor oath required. For personal study only.

✦ Synopsis

Novel diphosphonate homologs 7a-7c, and their cyclic counterparts 8a-8c, of the previously synthesized farnesyl pyrophosphate analogs 1 and 2 were prepared and tested for their inhibition potency and specificity of the enzymes PFT and PGGT-I. Compound 2 was shown to be the most potent inhibitor of PFT (IC 50 ϭ 0.58 Ϯ 0.45 ȐM) in this series. The novel compound 7a, the one carbon homolog of 2, proved to be the most potent inhibitor of PGGT-I (IC 50 ϭ 0.98 Ϯ 0.01 ȐM). The cyclic analogs 8a-8c are generally less biologically active. The compounds 2 and 7a are nonspecific toward inhibition of PFT and PGGT-I and may inhibit both farnesylation and geranylgeranylation processing of oncogenic proteins.

📜 SIMILAR VOLUMES

Synthesis of vinyl pyrophosphonate analo

Synthesis of vinyl pyrophosphonate analogues of farnesyl pyrophosphate: New potential inhibitors of farnesyl protein transferase

✍ Ibrahim Zgani; Chantal Menut; Jean Louis Montéro 📂 Article 📅 2002 🏛 John Wiley and Sons 🌐 English ⚖ 127 KB

## Abstract The synthesis of new bioisosteric analogues of farnesyl pyrophosphate where a vinyl pyrophosphonate replaced the pyrophosphate moiety is described. These compounds have been prepared using a Horner–Wadsworth–Emmons procedure and a modified Michelson reaction. They have been evaluated fo

ChemInform Abstract: Synthesis of Tripho

ChemInform Abstract: Synthesis of Triphosphonate Analogues of Farnesyl Pyrophosphate. Inhibitors of Squalene Synthase and Protein:Farnesyl Transferase.

✍ M. OVERHAND; E. PIETERMAN; L. H. COHEN; A. R. P. M. VALENTIJN; G. A. VAN DER MAR 📂 Article 📅 2010 🏛 John Wiley and Sons ⚖ 23 KB 👁 1 views

Protein isoprenylation regulates secreti

Protein isoprenylation regulates secretion of matrix metalloproteinase 1 from rheumatoid synovial fibroblasts: Effects of statins and farnesyl and geranylgeranyl transferase inhibitors

✍ Aryeh M. Abeles; Nada Marjanovic; Jean Park; Mukundan Attur; Edwin S. Chan; Hayf 📂 Article 📅 2007 🏛 John Wiley and Sons 🌐 English ⚖ 556 KB

Phosphonomethylphosphorylmethyl(oxy)-Ana

Phosphonomethylphosphorylmethyl(oxy)-Analogues of Geranylgeranyl Diphosphate as Stable and Selective Geranylgeranyl Protein Transferase Inhibitors.

✍ Marco Macchia; et al. et al. 📂 Article 📅 2005 🏛 John Wiley and Sons ⚖ 13 KB

ChemInform Abstract: Imidazole-Containin

ChemInform Abstract: Imidazole-Containing Diarylether and Diarylsulfone Inhibitors of Farnesyl-Protein Transferase.

✍ Christopher J. Dinsmore; Theresa M. Williams; Timothy J. O'Neill; Dongming Liu; 📂 Article 📅 2010 🏛 John Wiley and Sons ⚖ 27 KB 👁 1 views

## Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article is trackable v

ChemInform Abstract: Novel Tricyclic Ami

ChemInform Abstract: Novel Tricyclic Aminoacetyl and Sulfonamide Inhibitors of RAS Farnesyl Protein Transferase.

✍ F. G. NJOROGE; B. VIBULBHAN; C. S. ALVAREZ; W. R. BISHOP; J. PETRIN; R. J. DOLL; 📂 Article 📅 2010 🏛 John Wiley and Sons ⚖ 30 KB 👁 2 views

Novel Tricyclic Aminoacetyl and Sulfonamide Inhibitors of RAS Farnesyl Protein Transferase. -It is shown that derivatization of the amino group with a phthaloyl moiety increases inhibitory activity of the title compounds, cf. (IIIc) and (IIId). The potent inhibitors (III) and (V) are non-peptidic,