MMP12→Isoquinolines→Nuclear Proteins→poly-ADP-ribose

• 19775099(MMP12): Design, synthesis, biological evaluation, and NMR studies of a new series of arylsulfones as selective and potent matrix metalloproteinase-12 inhibitors.

  We report herein the design , synthesis , and in vitro evaluation of a new series of compounds , possessing an arylsulfonyl scaffold , for their potential as selective inhibitors of MMP-12.

• 18409175(Isoquinolines): On the way to selective PARP-2 inhibitors. Design, synthesis, and preliminary evaluation of a series of isoquinolinone derivatives.

  Among them , we identified the 5-benzoyloxyisoquinolin-1 (2 H) - one derivative as the most selective PARP-2 inhibitor reported so far , with a PARP-2 / PARP-1 selectivity index greater than 60.

• 10364231(Nuclear Proteins): PARP-2, A novel mammalian DNA damage-dependent poly(ADP-ribose) polymerase.

  Poly (ADP-ribose) polymerase which we will now call PARP-1 , has been the only known enzyme of this type for over 30 years.

• 8080500(poly-ADP-ribose): Nitric oxide activation of poly(ADP-ribose) synthetase in neurotoxicity.

  Poly (adenosine 5 ' - diphosphoribose) synthetase (PARS) is a nuclear enzyme which , when activated by DNA strand breaks , adds up to 100 adenosine 5 ' - diphosphoribose (ADP-ribose) units to nuclear proteins such as histones and PARS itself.