Results 111 to 120 of about 42,131 (286)

PI5P4K inhibitors: promising opportunities and challenges

The FEBS Journal, EarlyView.
Developing inhibitors is like climbing a steep, challenging mountain. PI5P4K inhibitors hold significant promise for the treatment of cancer, immune disorders, and neurological diseases. However, the path to success is fraught with hurdles, and researchers are therefore required to apply their expertise to overcome critical “checkpoints.” While some ...
Koh Takeuchi, Lisa Nagase, Shun Kageyama, Hirotaka Kanoh, Masashi Oshima, Aki Ogawa‐Iio, Yoshiki Ikeda, Yuki Fujii, Sei Kondo, Natsuki Osaka, Takeshi Masuda, Tsukasa Ishihara, Yoshikazu Nakamura, Yoshihisa Hirota, Takehiko Sasaki, Toshiya Senda, Atsuo T. Sasaki   +16 more
wiley   +1 more source

Heat Shock Protein 20 (HSP20) is a novel substrate for Protein Kinase D1 (PKD1) [PDF]

, 2015
Heat shock protein 20 (HSP20) has cardioprotective qualities, which are triggered by PKA phosphorylation. PKD1 is also a binding partner for HSP20, and this prompted us to investigate whether the chaperone was a substrate for PKD1.
Baillie, George, Sin, Yuan Yan
core   +1 more source

The Molecular Biology of Cyclic Nucleotide Phosphodiesterases

, 1999
Recent progress in the field of cyclic nucleotides has shown that a large array of closely related proteins is involved in each step of the signal transduction cascade. Nine families of adenylyl cyclases catalyze the synthesis of the second messenger cAMP, and protein kinases A, the intracellular effectors of cAMP, are composed of four regulatory and ...
Marco Conti, S.-L. C. Jin
openaire   +3 more sources

A signal transduction blind spot: the function of adenylyl cyclase transmembrane domains

The FEBS Journal, EarlyView.
Transmembrane adenylyl cyclases (tmACs) are essential for synthesising the universal second messenger cyclic AMP. All tmACs share a common topology that includes a large 12‐helix transmembrane (TM) domain. This domain accounts for ~ 35% of the coding sequence but its function is still an open question.
Ryan S. Dowsell, Matthew G. Gold
wiley   +1 more source

To Target or Not to Target Schistosoma mansoni Cyclic Nucleotide Phosphodiesterase 4A? [PDF]

Int J Mol Sci, 2023
Zheng Y, Schroeder S, Kanev GK, Botros SS, William S, Sabra AA, Maes L, Caljon G, Gil C, Martinez A, Salado IG, Augustyns K, Edink E, Sijm M, de Heuvel E, de Esch IJP, van der Meer T, Siderius M, Sterk GJ, Brown D, Leurs R.   +20 more
europepmc   +1 more source

Allosteric modulation of protein kinase A in individuals affected by NLPD‐PKA, a neurodegenerative disease in which the PRKAR1B L50R variant is expressed

The FEBS Journal, EarlyView.
In healthy neurons, Protein kinase A (PKA) forms a tetrameric holoenzyme enabling precise allosteric regulation. We characterized a novel neurodegenerative disease, neuronal loss, and parkinsonism driven by PRKAR1B mutation (NLPD‐PKA), demonstrating disrupted holoenzyme assembly, reduced cooperativity, and increased catalytic subunit nuclear ...
Tal Benjamin‐Zukerman, Valeria Pane, Rania Safadi‐Safa, Meir Solomon, Varda Lev‐Ram, Mohammad Aboraya, Anwar Dakwar, Daniela Bertinetti, Andrew Hoy, Merel O. Mol, John van Swieten, Rodrigo Maillard, Friedrich W. Herberg, Ronit Ilouz   +13 more
wiley   +1 more source

Once upon a Testis: The Tale of Cyclic Nucleotide Phosphodiesterase in Testicular Cancers. [PDF]

Int J Mol Sci, 2023
Campolo F, Assenza MR, Venneri MA, Barbagallo F.   +3 more
europepmc   +1 more source

Posttranslational modifications of phosphodiesterase type 4 enzymes represent novel points for therapeutic targeting

The FEBS Journal, EarlyView.
Enzymes from the phosphodiesterase type 4 family (PDE4) coordinate physiological events driven by the cyclic AMP s(cAMP) signaling pathway by tightly controlling cAMP dynamics in many cell types. Key to this strict regulation is the myriad of posttranslational modifications that alter PDE4 activity, cellular location, and binding partner selection ...
Madihah Hussain, Gonzalo S. Tejeda, George S. Baillie   +2 more
wiley   +1 more source

Cellular Redox Metabolism Is Modulated by the Distinct Localization of Cyclic Nucleotide Phosphodiesterase 5A Isoforms. [PDF]

Int J Mol Sci, 2022
Cardarelli S, Miele AE, Campolo F, Massimi M, Mancini P, Biagioni S, Naro F, Giorgi M, Saliola M.   +8 more
europepmc   +1 more source

Delineation of RAID1, the RACK1 interaction domain located within the unique N-terminal region of the cAMP-specific phosphodiesterase, PDE4D5 [PDF]

, 2002
Background The cyclic AMP specific phosphodiesterase, PDE4D5 interacts with the β-propeller protein RACK1 to form a signaling scaffold complex in cells.
Bolger, G.B., Houslay, M., McCahill, A., Steele, M.R., Warwicker, J., Yarwood, S.   +5 more
core   +3 more sources