207916-05-0Relevant articles and documents
Targeting prohibitin with small molecules to promote melanogenesis and apoptosis in melanoma cells
Djehal, Amel,Krayem, Mohammad,Najem, Ahmad,Hammoud, Hassan,Cresteil, Thierry,Nebigil, Canan G.,Wang, Dong,Yu, Peng,Bentouhami, Embarek,Ghanem, Ghanem E.,Désaubry, Laurent
, p. 880 - 888 (2018)
Prohibitins 1 and 2 (PHB1/2) are scaffold proteins that are involved in both melanogenesis and oncogenic pathways. We hypothesized that a PHB1 ligand, melanogenin, may display anti-cancer effects in addition to its known melanogenic activity in melanocytes. Here, we disclose a convenient synthesis of melanogenin, and its analogs. We found that, among 57 new melanogenin analogs, two (Mel9 and Mel41) significantly promoted both melanogenesis in melanocytes by activating one of the PHB2-interacting proteins, microtubule-associated protein light chain 3 (LC3), and upregulating the expression of microphthalmia associated transcription factor (MITF). These analogs also activate ERK. Besides, in addition to their promelanogenic activities, we uncovered that melanogenin and its active analogs induce apoptosis in several cancer cell lines, including melanoma cells, and that this effect is caused by an inhibition of AKT survival pathway. Our findings present a new putative function for PHBs as regulators of LC3/ERK/MITF melanogenic signaling, and suggest that Mel9 and Mel41 may provide the basis for the development of new drugs candidates to treat melanoma and other types of cancers.
Influence of supramolecular bonding contacts on the spin crossover behaviour of iron(ii) complexes from 2,2′-dipyridylamino/s-triazine ligands
Wannarit, Nanthawat,Roubeau, Olivier,Youngme, Sujittra,Teat, Simon J.,Gamez, Patrick
, p. 7120 - 7130 (2013/08/25)
Reactions of the related ligands 2-(N,N-bis(2-pyridyl)amino)-4,6- bis(phenoxy)-(1,3,5)triazine (L1) and 2-(N,N-bis(2-pyridyl)amino)-4,6- bis(pentafluorophenoxy)-(1,3,5)triazine (L1F) with iron(ii) thiocyanate produced two spin-crossover coordination compounds with distinct cooperative behaviours. trans-[Fe(L1)2(NCS)2] ·2CH2Cl2 (1) displays a very gradual transition centred at T = 233 K, characterized by a ΔT80 (namely the temperature range within which 80% of the transition considered occurs) of 90 K, while that of fluorinated trans-[Fe(L1F)2(NCS) 2]·2CH3CN (3) is significantly more abrupt (and centred at T = 238 K), with a ΔT80 of 50 K, resulting from supramolecular contacts induced by the fluorinated phenol groups. The coordination compound equivalent to 1 with selenocyanate anions, namely trans-[Fe(L1)2(NCSe)2]·4CH2Cl 2·4CH3OH (2), also exhibits SCO properties centred at T = 238 K, but the transition is very gradual (ΔT80 = 150 K). Light-induced excited spin-state trapping (LIESST) is effective although incomplete for 2 and 3, while it is complete with a TLIESST of 58 K for 1. The Royal Society of Chemistry 2013.
