4MAN

Bcl_2-Navitoclax Analog (with Indole) Complex

Replaces:  4LXE

Summary for 4MAN

• Entry DOI: 10.2210/pdb4man/pdb
• Related: 4LVT 4LXD
• Descriptor: Apoptosis regulator Bcl-2, 4-[4-({4'-chloro-3-[2-(dimethylamino)ethoxy]biphenyl-2-yl}methyl)piperazin-1-yl]-2-(1H-indol-5-yloxy)-N-({3-nitro-4-[(tetrahydro-2H-pyran-4-ylmethyl)amino]phenyl}sulfonyl)benzamide (3 entities in total)
• Functional Keywords: 8 helices, apoptosis regulator-inhibitor complex, apoptosis regulator/inhibitor
• Biological source: Homo sapiens (human); More
• Cellular location: Mitochondrion outer membrane ; Single-pass membrane protein : P10415
• Total number of polymer chains: 2
• Total formula weight: 40560.09

Authors

Park, C.H. (deposition date: 2013-08-16, release date: 2014-01-29, Last modification date: 2024-02-28)

• Primary citation: Souers, A.J.,Leverson, J.D.,Boghaert, E.R.,Ackler, S.L.,Catron, N.D.,Chen, J.,Dayton, B.D.,Ding, H.,Enschede, S.H.,Fairbrother, W.J.,Huang, D.C.,Hymowitz, S.G.,Jin, S.,Khaw, S.L.,Kovar, P.J.,Lam, L.T.,Lee, J.,Maecker, H.L.,Marsh, K.C.,Mason, K.D.,Mitten, M.J.,Nimmer, P.M.,Oleksijew, A.,Park, C.H.,Park, C.M.,Phillips, D.C.,Roberts, A.W.,Sampath, D.,Seymour, J.F.,Smith, M.L.,Sullivan, G.M.,Tahir, S.K.,Tse, C.,Wendt, M.D.,Xiao, Y.,Xue, J.C.,Zhang, H.,Humerickhouse, R.A.,Rosenberg, S.H.,Elmore, S.W.; ABT-199, a potent and selective BCL-2 inhibitor, achieves antitumor activity while sparing platelets.; NAT.MED. (N.Y.), 19:202-208, 2013; PubMed: 23291630; DOI: 10.1038/nm.3048

Experimental method

X-RAY DIFFRACTION (2.07 Å)