Sequence of KASA_MYCTU

meromycolic acid 3-oxoacyl-(acyl carrier protein) synthase I

P9WQD9

416

43316

944481

Cole S.T.,Brosch R.,Parkhill J.,Garnier T.,Churcher C.M.,Harris D.E.,Gordon S.V.,Eiglmeier K.,Gas S.,Barry C.E. III,Tekaia F.,Badcock K.,Basham D.,Brown D.,Chillingworth T.,Connor R.,Davies R.M.,Devlin K.,Feltwell T.,Gentles S.,Hamlin N.,Holroyd S.,Hornsby T.,Jagels K.,Krogh A.,McLean J.,Moule S.,Murphy L.D.,Oliver S.,Osborne J.,Quail M.A.,Rajandream M.A.,Rogers J.,Rutter S.,Seeger K.,Skelton S.,Squares S.,Squares R.,Sulston J.E.,Taylor K.,Whitehead S.,Barrell B.G.

Deciphering the biology of Mycobacterium tuberculosis from the complete genome sequence.

Nature

393

537-544

1998

944482

Kremer L.,Douglas J.D.,Baulard A.R.,Morehouse C.,Guy M.R.,Alland D.,Dover L.G.,Lakey J.H.,Jacobs W.R. Jr.,Brennan P.J.,Minnikin D.E.,Besra G.S.

Thiolactomycin and related analogues as novel anti-mycobacterial agents targeting KasA and KasB condensing enzymes in Mycobacterium tuberculosis.

J. Biol. Chem.

275

16857-16864

2000

944483

Schaeffer M.L.,Agnihotri G.,Volker C.,Kallender H.,Brennan P.J.,Lonsdale J.T.

Purification and biochemical characterization of the Mycobacterium tuberculosis beta-ketoacyl-acyl carrier protein synthases KasA and KasB.

J. Biol. Chem.

276

47029-47037

2001

944484

Kremer L.,Dover L.G.,Carrere S.,Nampoothiri K.M.,Lesjean S.,Brown A.K.,Brennan P.J.,Minnikin D.E.,Locht C.,Besra G.S.

Mycolic acid biosynthesis and enzymic characterization of the beta-ketoacyl-ACP synthase A-condensing enzyme from Mycobacterium tuberculosis.

Biochem. J.

364

423-430

2002

944485

Slayden R.A.,Barry C.E. III

The role of KasA and KasB in the biosynthesis of meromycolic acids and isoniazid resistance in Mycobacterium tuberculosis.

Tuberculosis

82

149-160

2002

944486

Molle V.,Brown A.K.,Besra G.S.,Cozzone A.J.,Kremer L.

The condensing activities of the Mycobacterium tuberculosis type II fatty acid synthase are differentially regulated by phosphorylation.

J. Biol. Chem.

281

30094-30103

2006

944487

Swanson S.,Gokulan K.,Sacchettini J.C.

KasA, another brick in the mycobacterial cell wall.

Structure

17

914-915

2009

944488

Kelkar D.S.,Kumar D.,Kumar P.,Balakrishnan L.,Muthusamy B.,Yadav A.K.,Shrivastava P.,Marimuthu A.,Anand S.,Sundaram H.,Kingsbury R.,Harsha H.C.,Nair B.,Prasad T.S.,Chauhan D.S.,Katoch K.,Katoch V.M.,Kumar P.,Chaerkady R.,Ramachandran S.,Dash D.,Pandey A.

Proteogenomic analysis of Mycobacterium tuberculosis by high resolution mass spectrometry.

Mol. Cell. Proteomics

10

0-0

2011

944489

Borgaro J.G.,Chang A.,Machutta C.A.,Zhang X.,Tonge P.J.

Substrate recognition by beta-ketoacyl-ACP synthases.

Biochemistry

50

10678-10686

2011

944490

Schaefer B.,Kisker C.,Sotriffer C.A.

Molecular dynamics of Mycobacterium tuberculosis KasA: implications for inhibitor and substrate binding and consequences for drug design.

J. Comput. Aided Mol. Des.

25

1053-1069

2011

944491

Lee W.,Engels B.

The protonation state of catalytic residues in the resting state of KasA revisited: detailed mechanism for the activation of KasA by its own substrate.

Biochemistry

53

919-931

2014

944492

Luckner S.R.,Machutta C.A.,Tonge P.J.,Kisker C.

Crystal structures of Mycobacterium tuberculosis KasA show mode of action within cell wall biosynthesis and its inhibition by thiolactomycin.

Structure

17

1004-1013

2009

944493

Schiebel J.,Kapilashrami K.,Fekete A.,Bommineni G.R.,Schaefer C.M.,Mueller M.J.,Tonge P.J.,Kisker C.

Structural basis for the recognition of mycolic acid precursors by KasA, a condensing enzyme and drug target from Mycobacterium tuberculosis.

J. Biol. Chem.

288

34190-34204

2013

944494

Abrahams K.A.,Chung C.W.,Ghidelli-Disse S.,Rullas J.,Rebollo-Lopez M.J.,Gurcha S.S.,Cox J.A.,Mendoza A.,Jimenez-Navarro E.,Martinez-Martinez M.S.,Neu M.,Shillings A.,Homes P.,Argyrou A.,Casanueva R.,Loman N.J.,Moynihan P.J.,Lelievre J.,Selenski C.,Axtman M.,Kremer L.,Bantscheff M.,Angulo-Barturen I.,Izquierdo M.C.,Cammack N.C.,Drewes G.,Ballell L.,Barros D.,Besra G.S.,Bates R.H.

Identification of KasA as the cellular target of an anti-tubercular scaffold.

Nat. Commun.

7

12581-12581

2016

944495

Cunningham F.,Esquivias J.,Fernandez-Menendez R.,Perez A.,Guardia A.,Escribano J.,Rivero C.,Vimal M.,Cacho M.,de Dios-Anton P.,Martinez-Martinez M.S.,Jimenez E.,Huertas Valentin L.,Rebollo-Lopez M.J.,Lopez-Roman E.M.,Sousa-Morcuende V.,Rullas J.,Neu M.,Chung C.W.,Bates R.H.

Exploring the SAR of the beta-ketoacyl-ACP synthase inhibitor GSK3011724A and optimization around a genotoxic metabolite.

ACS Infect. Dis.

6

1098-1109

2020

944496

Inoyama D.,Awasthi D.,Capodagli G.C.,Tsotetsi K.,Sukheja P.,Zimmerman M.,Li S.G.,Jadhav R.,Russo R.,Wang X.,Grady C.,Richmann T.,Shrestha R.,Li L.,Ahn Y.M.,Ho Liang H.P.,Mina M.,Park S.,Perlin D.S.,Connell N.,Dartois V.,Alland D.,Neiditch M.B.,Kumar P.,Freundlich J.S.

A preclinical candidate targeting Mycobacterium tuberculosis KasA.

Cell Chem. Biol.

27

560-0

2020