41373-29-9Relevant academic research and scientific papers
Novel Furan-2-yl-1 H-pyrazoles Possess Inhibitory Activity against α-Synuclein Aggregation
Ryan, Philip,Xu, Mingming,Jahan, Kousar,Davey, Andrew K.,Bharatam, Prasad V.,Anoopkumar-Dukie, Shailendra,Kassiou, Michael,Mellick, George D.,Rudrawar, Santosh
, p. 2303 - 2315 (2020)
A series of novel furan-2-yl-1H-pyrazoles and their chemical precursors were synthesized and evaluated for their effectiveness at disrupting α-synuclein (α-syn) aggregation in vitro. The compounds were found to inhibit α-syn aggregation with efficacy comp
Identification of a small molecule inhibitor that stalls splicing at an early step of spliceosome activation
Sidarovich, Anzhalika,Will, Cindy L.,Anokhina, Maria M.,Ceballos, Javier,Sievers, Sonja,Agafonov, Dmitry E.,Samatov, Timur,Bao, Penghui,Kastner, Berthold,Urlaub, Henning,Waldmann, Herbert,Lührmann, Reinhard
, (2017/03/23)
Small molecule inhibitors of pre-mRNA splicing are important tools for identifying new spliceosome assembly intermediates, allowing a finer dissection of spliceosome dynamics and function. Here, we identified a small molecule that inhibits human pre-mRNA splicing at an intermediate stage during conversion of pre-catalytic spliceosomal B complexes into activated Bact complexes. Characterization of the stalled complexes (designated B028) revealed that U4/U6 snRNP proteins are released during activation before the U6 Lsm and B-specific proteins, and before recruitment and/or stable incorporation of Prp19/CDC5L complex and other Bact complex proteins. The U2/U6 RNA network in B028 complexes differs from that of the Bact complex, consistent with the idea that the catalytic RNA core forms stepwise during the B to Bact transition and is likely stabilized by the Prp19/CDC5L complex and related proteins. Taken together, our data provide new insights into the RNP rearrangements and extensive exchange of proteins that occurs during spliceosome activation.
Rhodanine-based tau aggregation inhibitors in cell models of tauopathy
Bulic, Bruno,Pickhardt, Marcus,Khlistunova, Inna,Biernat, Jacek,Mandelkow, Eva-Maria,Mandelkow, Eckhard,Waldmann, Herbert
, p. 9215 - 9219 (2008/12/22)
Breaking up the crowd: The pathological aggregation of tau protein correlates closely with the progression of Alzheimer's disease. Rhodanine-based inhibitors of tau aggregation (e.g. 1) have been identified, and it has been shown that tau aggregation in a
Dantrolene analogues revisited: General synthesis and specific functions capable of discriminating two kinds of Ca2+ release from sarcoplasmic reticulum of mouse skeletal muscle
Hosoya, Takamitsu,Aoyama, Hiroshi,Ikemoto, Takaaki,Kihara, Yasutaka,Hiramatsu, Toshiyuki,Endo, Makoto,Suzuki, Masaaki
, p. 663 - 673 (2007/10/03)
The general synthesis of dantrolene analogues with various substituents on its phenyl ring has been developed via palladium-catalyzed cross-coupling reactions, the Stille or Suzuki reaction, as the key step. The effects of synthesized analogues have been evaluated by two kinds of Ca2+ release modes from sarcoplasmic reticulum (SR) of mouse skeletal muscle fibers based on: (1) the measurement of twitch contraction caused by the physiological Ca2+ release (PCR) of intact skeletal muscle and (2) the rate of Ca2+-induced Ca2+ release (CICR) in saponin-treated skinned muscle fibers. Although dantrolene, a lead compound, inhibits both twitch contraction and CICR, some structurally modified analogues exhibit one or the other of these effects. The methoxy congener, GIF-0185, potently inhibits the twitch contraction without affecting the CICR, while GIF-0166 and GIF-0248, the ortho-nitro regioisomer and ortho, ortho-dinitro substituted analogues, respectively, doubly potentiate the CICR exclusively.
Preparation of 5-aryl furfurals and aryl thiophene-2-carboxaldehydes via palladium-catalyzed C-C bond formation in aqueous media
Bussolari, Jacqueline C.,Rehborn, Diana C.
, p. 965 - 967 (2008/02/09)
(matrix presented) A series of 5-aryl furfurals and aryl thiophene-2-carboxaldehydes was synthesized. To this end, efficient and effective palladium-catalyzed C-C bond-forming reactions were carried out at room temperature in aqueous media. This mild proc
