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A review, discussing antimalarial drug resistance, which has emerged as one of the greatest challenges facing malaria control today, creating an urgent need for new drugs.Accumulating evidence suggests that Plasmodium falciparum (Pf), the causative agent of pernicious malaria, relies heavily on its chaperones and cochaperones for growth and survival in human red blood cells.Underscoring their functional importance, the chaperone genes in fact constitute as much as 2% of the Pf genome.The Hsp90 chaperone holds a special place in all living cells, due to its multiple clients.Given the high degree of sequence homol. between the plasmodial and human Hsp90, and the important role of Hsp90 in both species, it is crucial to develop inhibitors that are specific toward Plasmodium in order to avoid human toxicity.To this end, a highly specific drug-design approach - differential fragment-based screening (DFS) - has been adopted which can be combined with biol. studies and lead optimization to probe the active sites that are different between the Plasmodium and human orthologs.In this chapter, proof-of-concept examples of novel drug-like inhibitors of PfHsp90 that evolved from crystal structure, synthetic chem. and structure-based compound-Hsp90 interaction anal., are presented.The results should form the foundation for the discovery and optimization of highly specific and potent PfHsp90 inhibitors with improved antimalarial efficacy and minimal side effects.

Synthesis and biological evaluation of benzimidazoles as FKBF inhibitors

作者: De, Surya

Neurodegenerative disorders are CNS diseases characterized by synaptic loss, neuronal atrophy, and death as common pathol. hallmarks.Parkinson's disease (PD) is one of the most common neurol. disorders, affecting over 6.3 million people globally, and 1.5 million people in North America.Parkinson's disease (PD) belongs to a group of conditions called motor system disorders, which are the result of the loss of dopamine-producing neurons in the substantia nigra.A hallmark of PD neuronal degeneration is aberrant aggregation of alpha-synuclein (α-SYN).In PD, the protein is present in a fibrillar, aggregated form inside cytoplasmic inclusions called Lewy bodies.Enzymes of the FK506 binding protein (FKBP) family accelerate the aggregation of recombinant α-SYN in vitro and FK506, a specific FKBP inhibitor, abrogates this effect.FKBPs are members of the immunophilin family of proteins.These proteins are enzymes with peptidyl-prolyl cis-trans isomerase (PPIase) activity and bind to immunosuppressants such as FK506.PPIase enzymes catalyze cis-trans isomerization of X-Pro peptide bonds, an essential and rate-limiting step in the process of protein folding.The human FKBP family contains 15 principal members with many different functions.Among these, four members, namely, FKBP12, FKBP38, FKBP52, and FKBP65, are enriched in the human brain.Importantly, numerous clin. and pre-clin. studies have demonstrated that two FKPBs, FKBP12 and FKPB52, are involved in PD pathol.The results of this new series of FKBP 12 and FKBP-52 inhibitors will be presented.

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药物(靶点)	适应症	全球最高研发状态

FKBP inhibitor (Plex Pharma) ( FKBP )	帕金森病更多	临床前
dual HSP90/TRAP1 inhibitors (Plex Pharma) ( HSP90 x TRAP1 )	2型神经纤维瘤病更多	临床前
CAP-1160 ( CRYAB x HSP )	白内障更多	药物发现
Viral Conjunctivitis (Plex Pharma)	病毒性结膜炎更多	药物发现
West Nile (Plex Pharma)	西尼罗河热更多	药物发现