Entry Database : PDB / ID : 3hc8 Structure visualization Downloads & linksTitle Investigation of Aminopyridiopyrazinones as PDE5 Inhibitors: Evaluation of Modifications to the Central Ring System. ComponentscGMP-specific 3',5'-cyclic phosphodiesterase,cAMP-specific 3',5'-cyclic phosphodiesterase 4A Details Keywords HYDROLASE / PDE5 / PDE-5 / inhibition / Alternative splicing / cAMP / Phosphoprotein / Polymorphism Allosteric enzyme / cGMP / cGMP-binding / Magnesium / Metal-binding / Nucleotide-binding / ZincFunction / homology Function and homology informationFunction Domain/homology Component
regulation of adenylate cyclase-activating G protein-coupled receptor signaling pathway / positive regulation of oocyte development / 3',5'-cyclic-GMP phosphodiesterase / regulation of nitric oxide mediated signal transduction / negative regulation of cardiac muscle contraction / 3',5'-cyclic-AMP phosphodiesterase / regulation of protein kinase A signaling / oocyte development / RHOBTB1 GTPase cycle / relaxation of cardiac muscle ... regulation of adenylate cyclase-activating G protein-coupled receptor signaling pathway / positive regulation of oocyte development / 3',5'-cyclic-GMP phosphodiesterase / regulation of nitric oxide mediated signal transduction / negative regulation of cardiac muscle contraction / 3',5'-cyclic-AMP phosphodiesterase / regulation of protein kinase A signaling / oocyte development / RHOBTB1 GTPase cycle / relaxation of cardiac muscle / extrinsic component of membrane / positive regulation of cardiac muscle hypertrophy / cGMP catabolic process / cGMP effects / cAMP catabolic process / cGMP binding / 3',5'-cyclic-nucleotide phosphodiesterase activity / DARPP-32 events / 3',5'-cyclic-GMP phosphodiesterase activity / 3',5'-cyclic-AMP phosphodiesterase activity / Smooth Muscle Contraction / T cell proliferation / cAMP binding / negative regulation of T cell proliferation / cAMP-mediated signaling / ruffle membrane / sensory perception of smell / cellular response to xenobiotic stimulus / G alpha (s) signalling events / G protein-coupled receptor signaling pathway / perinuclear region of cytoplasm / signal transduction / nucleoplasm / membrane / metal ion binding / nucleus / plasma membrane / cytosol Similarity search - Function Phosphodiesterase 4 upstream conserved regions (UCR) / Phosphodiesterase 4 upstream conserved regions (UCR) / Catalytic domain of cyclic nucleotide phosphodiesterase 4b2b / 3'5'-cyclic nucleotide phosphodiesterase, catalytic domain / 3'5'-cyclic nucleotide phosphodiesterase / GAF domain / 3'5'-cyclic nucleotide phosphodiesterase, catalytic domain / 3'5'-cyclic nucleotide phosphodiesterase, conserved site / 3'5'-cyclic nucleotide phosphodiesterase, catalytic domain superfamily / 3'5'-cyclic nucleotide phosphodiesterase ... Phosphodiesterase 4 upstream conserved regions (UCR) / Phosphodiesterase 4 upstream conserved regions (UCR) / Catalytic domain of cyclic nucleotide phosphodiesterase 4b2b / 3'5'-cyclic nucleotide phosphodiesterase, catalytic domain / 3'5'-cyclic nucleotide phosphodiesterase / GAF domain / 3'5'-cyclic nucleotide phosphodiesterase, catalytic domain / 3'5'-cyclic nucleotide phosphodiesterase, conserved site / 3'5'-cyclic nucleotide phosphodiesterase, catalytic domain superfamily / 3'5'-cyclic nucleotide phosphodiesterase / 3'5'-cyclic nucleotide phosphodiesterase domain signature. / 3'5'-cyclic nucleotide phosphodiesterase domain profile. / Domain present in phytochromes and cGMP-specific phosphodiesterases. / GAF domain / GAF-like domain superfamily / Metal dependent phosphohydrolases with conserved 'HD' motif. / HD/PDEase domain / Orthogonal Bundle / Mainly Alpha Similarity search - Domain/homologyBiological species Homo sapiens (human)Method X-RAY DIFFRACTION / MOLECULAR REPLACEMENT / molecular replacement / Resolution : 1.79 Å DetailsAuthors Hughes, R.O. / Stallings, W.C. / Cubbage, J.W. / Williams, J.M. CitationJournal : Bioorg.Med.Chem.Lett. / Year : 2009Title : Investigation of aminopyridiopyrazinones as PDE5 inhibitors: Evaluation of modifications to the central ring system.Authors: Hughes, R.O. / Walker, J.K. / Cubbage, J.W. / Fobian, Y.M. / Rogier, D.J. / Heasley, S.E. / Blevis-Bal, R.M. / Benson, A.G. / Owen, D.R. / Jacobsen, E.J. / Freskos, J.N. / Molyneaux, J.M. / ... Authors : Hughes, R.O. / Walker, J.K. / Cubbage, J.W. / Fobian, Y.M. / Rogier, D.J. / Heasley, S.E. / Blevis-Bal, R.M. / Benson, A.G. / Owen, D.R. / Jacobsen, E.J. / Freskos, J.N. / Molyneaux, J.M. / Brown, D.L. / Stallings, W.C. / Acker, B.A. / Maddux, T.M. / Tollefson, M.B. / Williams, J.M. / Moon, J.B. / Mischke, B.V. / Rumsey, J.M. / Zheng, Y. / Macinnes, A. / Bond, B.R. / Yu, Y. History Deposition May 5, 2009 Deposition site : RCSB / Processing site : RCSBRevision 1.0 Jul 7, 2009 Provider : repository / Type : Initial releaseRevision 1.1 Jul 13, 2011 Group : Version format complianceRevision 1.2 Jun 21, 2017 Group : Advisory / Database references ... Advisory / Database references / Source and taxonomy / Structure summary Category : entity / entity_name_com ... entity / entity_name_com / entity_src_gen / pdbx_distant_solvent_atoms / struct / struct_ref / struct_ref_seq / struct_ref_seq_dif Item : _entity.pdbx_description / _entity.pdbx_ec ... _entity.pdbx_description / _entity.pdbx_ec / _entity.pdbx_fragment / _entity.pdbx_mutation / _entity_name_com.name / _struct.pdbx_descriptor / _struct_ref.db_code / _struct_ref.pdbx_align_begin / _struct_ref.pdbx_db_accession / _struct_ref.pdbx_db_isoform / _struct_ref_seq.db_align_beg / _struct_ref_seq.db_align_end / _struct_ref_seq.pdbx_db_accession / _struct_ref_seq.pdbx_seq_align_end_ins_code / _struct_ref_seq.seq_align_end / _struct_ref_seq_dif.details Revision 1.3 Nov 1, 2017 Group : Refinement description / Category : softwareRevision 1.4 Jan 24, 2018 Group : Structure summary / Category : audit_author / Item : _audit_author.nameRevision 1.5 Jul 26, 2023 Group : Database references / Derived calculationsCategory : citation / database_2 ... citation / database_2 / pdbx_struct_conn_angle / struct_conn / struct_site Item : _citation.journal_volume / _citation.page_first ... _citation.journal_volume / _citation.page_first / _citation.page_last / _database_2.pdbx_DOI / _database_2.pdbx_database_accession / _pdbx_struct_conn_angle.ptnr1_auth_comp_id / _pdbx_struct_conn_angle.ptnr1_auth_seq_id / _pdbx_struct_conn_angle.ptnr1_label_asym_id / _pdbx_struct_conn_angle.ptnr1_label_atom_id / _pdbx_struct_conn_angle.ptnr1_label_comp_id / _pdbx_struct_conn_angle.ptnr1_label_seq_id / _pdbx_struct_conn_angle.ptnr3_auth_comp_id / _pdbx_struct_conn_angle.ptnr3_auth_seq_id / _pdbx_struct_conn_angle.ptnr3_label_asym_id / _pdbx_struct_conn_angle.ptnr3_label_atom_id / _pdbx_struct_conn_angle.ptnr3_label_comp_id / _pdbx_struct_conn_angle.ptnr3_label_seq_id / _pdbx_struct_conn_angle.value / _struct_conn.pdbx_dist_value / _struct_conn.ptnr1_auth_comp_id / _struct_conn.ptnr1_auth_seq_id / _struct_conn.ptnr1_label_asym_id / _struct_conn.ptnr1_label_atom_id / _struct_conn.ptnr1_label_comp_id / _struct_conn.ptnr1_label_seq_id / _struct_conn.ptnr2_auth_comp_id / _struct_conn.ptnr2_auth_seq_id / _struct_conn.ptnr2_label_asym_id / _struct_conn.ptnr2_label_atom_id / _struct_conn.ptnr2_label_comp_id / _struct_site.pdbx_auth_asym_id / _struct_site.pdbx_auth_comp_id / _struct_site.pdbx_auth_seq_id Revision 1.6 May 22, 2024 Group : Data collection / Category : chem_comp_atom / chem_comp_bond
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